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Staurosporine (STS) 단백질 키나아제 억제제

Name: Staurosporine (STS)
Brand: Selleck Chemicals
SKU: S1421
Rating: 5 (189 reviews)

제품 번호S1421

Staurosporine (STS)은 세포 자유 분석에서 PKCα, PKCγ 및 PKCη에 대한 강력한 PKC 억제제이며 IC50은 각각 2 nM, 5 nM 및 4 nM이며, PKCδ (20 nM), PKCε (73 nM)에는 덜 강력하고 PKCζ (1086 nM)에는 거의 활성이 없습니다. 이 화합물은 또한 PKA, PKG, S6K, CaMKII 등 다른 키나아제에 대한 억제 활성을 보입니다. 3상.

Staurosporine (STS) Antineoplastic and Immunosuppressive Antibiotics 억제제 Chemical Structure

화학 구조

분자량: 466.53

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품질 관리

배치: 순도: 99.61%

99.61

함께 자주 사용되는 제품 Staurosporine (STS)

Z-VAD-FMK

Z-VAD-FMK inhibits cell death induced by this compound in SJG2/MT330 cells.

관련 타겟	TGF-beta/Smad PKC ROCK Bcr-Abl
기타 Antineoplastic and Immunosuppressive Antibiotics 억제제	Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Cephalomannine Pirarubicin

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
human colon carcinoma cell line HCT116	Function assay			Concentration required for growth inhibition of human colon carcinoma cell line HCT116, IC50=6 nM.	15537345
human PBMC	Function assay		24 h	Suppression of IL2 production in human PBMC after 24 hrs by ELISA, IC50=16 nM.	18585046
endothelial cells	Function assay			Effective dose against plasminogen activator activity stimulated by phorbol ester in endothelial cells, ED50 = 7.5 μM.	8709095
Sf9 insect cells	Function assay			Inhibition of protein kinase C(1:1mixture of PKC alpha & beta) expressed in Sf9 insect cells, IC50 = 0.02 μM.	9873605
LoVo cells	Antiproliferative activity assay			Antiproliferative activity against human colon cancer cell line (LoVo cells) using MTT assay, IC50 = 0.001 μM.	11591505
umbilical vein endothelial cells	Antiproliferative activity assay			Antiproliferative activity against human umbilical vein endothelial cells (HUVECs) using MTT assay, IC50 = 0.004 μM.	11591505
ST-486 cells	Antiproliferative activity assay			Antiproliferative activity against burkit lymphoma cell line (ST-486 cells) using MTT assay, IC50 = 0.007 μM.	11591505
DLD-1 cells	Antiproliferative activity assay			Antiproliferative activity against human colon cancer cell line (DLD-1 cells) using MTT assay, IC50 = 0.009 μM.	11591505
HEK293 cells	Function assay			Inhibition of PKC-beta II mediated IL-8 release from HEK293 cells by ELISA, IC50 = 0.077 μM.	12941331
P19 cells	Function assay			Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM.	15771419
P19 cells	Function assay			Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM.	15771419
P19 cells	Function assay			Inhibition of Protein Kinase A in P19 cells, IC50 = 0.004 μM.	15771419
P19 cells	Function assay			Inhibition of Calcium/calmodulin-dependent protein kinase type II in P19 cells, IC50 = 0.006 μM.	15771419
P19 cells	Function assay			Inhibition of Cyclin-dependent kinase 1 in P19 cells, IC50 = 0.008 μM.	15771419
P19 cells	Function assay			Inhibition of Vascular endothelial growth factor receptor in P19 cells, IC50 = 0.014 μM.	15771419
HEK293 cells	Function assay			Inhibition of IL-8 release by HEK293 cells expressing PKC-beta2, IC50 = 0.077 μM.	15771419
P19 cells	Function assay			Inhibition of Insulin receptor kinase in P19 cells, IC50 = 0.2 μM.	15771419
P19 cells	Function assay			Inhibition of Casein kinase 1 in P19 cells, IC50 = 1.4 μM.	15771419
FL5.12-Akt1 cells	Antiproliferative activity assay			Antiproliferative activity against FL5.12-Akt1 cells by MTT assay, IC50 = 0.29 μM.	16403626
MiaPaCa-2 cells	Antiproliferative activity assay			Antiproliferative activity against MiaPaCa-2 cells by MTT assay, IC50 = 0.37 μM.	16403626
FL5.12-Akt1 cells	Function assay			Activity against GSK3 in FL5.12-Akt1 cells, EC50 = 0.46 μM.	16403626
MiaPaCa-2 cells	Antiproliferative activity assay			Antiproliferative activity against human MiaPaCa-2 cells, IC50 = 0.37 μM.	16413780
FL5.12-Akt1 cells	Function assay			Activity against GSK3 phosphorylation in FL5.12-Akt1 cells, EC50 = 0.46 μM.	16413780
Sf21 cells	Function assay			Inhibition of JAK3 expressed in Sf21 cells, IC50 = 0.006 μM.	17088059
U937 cells	Cytotoxicity assay			Cytotoxicity against human U937 cells, IC50 = 2 μM.	17088067
Sf9 cells	Function assay		1 min	Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 1 umol/L ATP, IC50 = 0.005 μM.	17315853
Sf9 cells	Function assay		20 mins	Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 1 umol/L ATP, IC50 = 0.015 μM.	17315853
Sf9 cells	Function assay		1 min	Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 10 umol/L ATP, IC50 = 0.036 μM.	17315853
Sf9 cells	Function assay		20 mins	Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 10 umol/L ATP, IC50 = 0.083 μM.	17315853
Sf9 cells	Function assay		1 min	Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 100 umol/L ATP, IC50 = 0.27 μM.	17315853
Sf9 cells	Function assay		20 mins	Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 100 umol/L ATP, IC50 = 0.51 μM.	17315853
A549 cells	Cytotoxicity assay		72 h	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0024 μM.	18484775
MDA-MB-231 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0071 μM.	18484775
HT29 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HT29 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0109 μM.	18484775
MCF7 cells	Function assay			Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, Ki = 0.005 μM.	18656369
MCF7 cells	Function assay			Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, IC50 = 2 μM.	18656369
Sf9 cells	Function assay			Inhibition of human Syk expressed in Sf9 cells, IC50 = 0.003 μM.	18823784
Sf9 cells	Function assay			Inhibition of human ZAP70 expressed in Sf9 cells, IC50 = 0.053 μM.	18823784
insect cells	Function assay			Inhibition of human recombinant Pim1 expressed in insect cells by HTRF, IC50 = 0.01 μM.	19179076
HT-29 cells	Apoptosis assay		2 h	Induction of apoptosis in human HT-29 cells assessed as change in mitochondrial transmembrane potential after 2 hrs by JC1 staining based fluorescence assay, ED50 = 0.0026 μM.	19422206
insect Sf21 cells	Function assay			Inhibition of JAK3 expressed in insect Sf21 cells assessed as inhibition of biotinylated substrate phosphorylation, IC50 = 0.006 μM.	19427203
Jurkat cells	Antiproliferative activity assay			Antiproliferative activity against JAK3 expressing IL2-stimulated human Jurkat cells, IC50 = 0.071 μM.	19427203
Jurkat cells	Antiproliferative activity assay			Antiproliferative activity against JAK3 expressing human resting Jurkat cells, IC50 = 0.311 μM.	19427203
HUE cells	Function assay		90 mins	Inhibition of VEGFR2 in HUE cells assessed as inhibition of VEGF-induced autophosphorylation treated for 90 mins before VEGF challenge by ELISA, IC50 = 0.07 μM.	20170163
Sf9 cells	Function assay		60 mins	Inhibition of human recombinant GST-fused NIK expressed in Sf9 cells after 60 mins by radiometric protein kinase assay, IC50 = 2.3 μM.	20580552
Sf21 cells	Function assay	30 uM		Inhibition of human CHK2 kinase expressed in insect Sf21 cells using phospho-CREBtide as substrate at 30 uM, IC50 = 0.027 μM.	21334796
Sf21 cells	Function assay	30 uM		Inhibition of human recombinant IKK-alpha expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.039 μM.	21334796
Sf21 cells	Function assay	30 uM		Inhibition of human recombinant IKK-beta expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.49 μM.	21334796
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM.	21388191
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM.	21388191
HT-29 cells	Function assay		2 h	Effect on mitochondrial membrane potential in human HT-29 cells after 2 hrs using JC-1 staining by fluorescence assay, IC50 = 0.002 μM.	21428375
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM.	21488655
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM.	21488655
HT-29 cells	Function assay			Inhibition of mitochondrial membrane potential in human HT-29 cells using JC1 dye staining by fluorescence plate reader assay, IC50 = 0.0025 μM.	21513293
SF268 cells	Cytotoxicity assay		48 h	Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50 = 0.044 μM.	21513294
CHOK1 cells	Cytotoxicity assay		48 h	Cytotoxicity against human CHOK1 cells after 48 hrs by SRB assay, GI50 = 0.13 μM.	21513294
H460 cells	Cytotoxicity assay		48 h	Cytotoxicity against human H460 cells after 48 hrs by SRB assay, GI50 = 3.6 μM.	21513294
HT-29 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HT-29 cells after 48 hrs by SRB assay, GI50 = 3.6 μM.	21513294
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 11 μM.	21513294
SW1116 cells	Function assay		24 h	Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.32 μM.	21962523
HT-29 cells	Apoptosis assay		2 h	Induction of apoptosis in human HT-29 cells assessed reduction of mitochondrial membrane potential after 2 hrs by using JC1 staining by fluorescence cell-based assay, ED50 = 0.0026 μM.	21973101
LoVo cells	Antiproliferative activity assay		48 to 72 h	Antiproliferative activity against human LoVo cells after 48 to 72 hrs by MTT assay, IC50 = 0.001 μM.	22182929
ST486 cells	Antiproliferative activity assay		48 to 72 h	Antiproliferative activity against human ST486 cells after 48 to 72 hrs by MTT assay, IC50 = 0.007 μM.	22182929
DLD1 cells	Antiproliferative activity assay		48 to 72 h	Antiproliferative activity against human DLD1 cells after 48 to 72 hrs by MTT assay, IC50 = 0.009 μM.	22182929
B16F10 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 2.82 μM.	22503364
MCF7 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 3.07 μM.	22503364
A431 cells	Cytotoxicity assay		24 h	Cytotoxicity against human A431 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.07 μM.	22541051
MCF7 cells	Cytotoxicity assay		24 h	Cytotoxicity against human MCF7 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.18 μM.	22541051
BJ cells	Cytotoxicity assay		72 h	Cytotoxicity against human BJ cells after 72 hrs by Calcein AM assay, IC50 = 0.002 μM.	22921081
CEM cells	Cytotoxicity assay		72 h	Cytotoxicity against human CEM cells after 72 hrs by Calcein AM assay, IC50 = 0.023 μM.	22921081
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells after 72 hrs by Calcein AM assay, IC50 = 0.064 μM.	22921081
HeLa cells	Cytotoxicity assay		72 h	Cytotoxicity against human HeLa cells after 72 hrs by Calcein AM assay, IC50 = 0.175 μM.	22921081
HepG2 cells	Function assay		24 h	Inhibition of telomerase in human HepG2 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.14 μM.	23018096
SW1116 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human SW1116 cells after 48 hrs by MTT method, IC50 = 4.95 μM.	23018096
HepG2 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT method, IC50 = 6.73 μM.	23018096
BGC823 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human BGC823 cells after 48 hrs by MTT method, IC50 = 6.83 μM.	23018096
HeLa cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human HeLa cells after 48 hrs by MTT method, IC50 = 9.12 μM.	23018096
HCT116 cells	Function assay			Inhibition of TNIK-mediated TCF4/beta-casein transcription in human HCT116 cells by beta-lactamase reporter gene assay, IC50 = 0.039 μM.	23232060
HepG2 cells	Function assay		48 h	Inhibition of telomerase in human HepG2 cells after 48 hrs by TRAP-PCR-ELISA, IC50 = 8.3 μM.	23279864
SW1116 cells	Function assay		24 h	Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.18 μM.	24286761
KE-97 cells	Cytotoxicity assay		72 h	Cytotoxicity against human KE-97 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.13 μM.	24328283
Jurkat cells	Cytotoxicity assay		72 h	Cytotoxicity against human Jurkat cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.14 μM.	24328283
HuH7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HuH7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.23 μM.	24328283
BGC823 cells	Cytotoxicity assay		72 h	Cytotoxicity against human BGC823 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.38 μM.	24328283
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.52 μM.	24328283
NIH/3T3 cells	Cytotoxicity assay		96 h	Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
A2780 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
HT-29 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
8505C cells	Cytotoxicity assay		96 h	Cytotoxicity against human 8505C cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
518A2 cells	Cytotoxicity assay		96 h	Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
MCF7 cells	Cytotoxicity assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 0.4 μM.	24361521
A549 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A549 cells after 96 hrs by SRB assay, IC50 = 0.6 μM.	24361521
V79 MZ cells	Function assay			Inhibition of human aldosterone synthase expressed in V79 MZ cells assessed as inhibition of aldosterone synthesis, IC50 = 0.011 μM.	24422519
HEK293 cells	Cytotoxicity assay		72 h	Cytotoxicity against HEK293 cells after 72 hrs by CellTiterGlo assay, IC50 = 0.056 μM.	24763262
HeLa cells	Antiproliferative activity assay		24 to 48 h	Antiproliferative activity against human HeLa cells after 24 to 48 hrs by CCK-8 assay, IC50 = 2.72 μM.	24792811
A549 cells	Antiproliferative activity assay		24 to 48 h	Antiproliferative activity against human A549 cells after 24 to 48 hrs by CCK-8 assay, IC50 = 3.05 μM.	24792811
HepG2 cells	Cytotoxicity assay			Cytotoxicity against human HepG2 cells, EC50 = 2 μM.	25316317
Raji cells	Cytotoxicity assay			Cytotoxicity against human Raji cells, EC50 = 2 μM.	25316317
BJ cells	Cytotoxicity assay			Cytotoxicity against human BJ cells, EC50 = 2 μM.	25316317
HEK293 cells	Cytotoxicity assay			Cytotoxicity against HEK293 cells, EC50 = 2 μM.	25316317
A549 cells	Cytotoxicity assay		48 h	Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.02 μM.	25825934
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.025 μM.	25825934
PC3 cells	Cytotoxicity assay		48 h	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 0.031 μM.	25825934
MGC-803 cells	Function assay		24 h	Inhibition of telomerase in human MGC-803 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.97 μM.	26900656
Sf9 insect cells	Function assay		10 mins	Inhibition of N-terminal GST tagged recombinant full-length human CHK1 expressed in baculovirus Sf9 insect cells after 10 mins by luminescent ADP-Glo assay, IC50 = 0.0012 μM.	27089211
Sf21 cells	Function assay		60 mins	Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method, IC50 = 0.002 μM.	27137359
Neuro2a cells	Cytotoxicity assay		72 h	Cytotoxicity against mouse Neuro2a cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0113 μM.	28152427
MDA-MB-231 cells	Function assay		16 h	Inhibition of retinoblastoma protein phosphorylation in human MDA-MB-231 cells after 16 hrs by Hoechst 33342 staining based fluorescence assay, IC50 = 0.066 μM.	28431342
Sf9 insect cells	Function assay		20 mins	Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method, IC50 = 0.00029 μM.	28482151
HEK293 cells	Cytotoxicity assay		72 h	Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 72 hrs by CellTiter Glo luminescent assay, CC50 = 0.00354 μM.	28624701
BT549 cells	Cytotoxicity assay		24 h	Cytotoxic activity against human BT549 cells incubated for 24 hrs by MTT assay, IC50 = 0.08 μM.	28705432
MDA-MB-468 cells	Cytotoxicity assay		24 h	Cytotoxic activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay, IC50 = 0.15 μM.	28705432
MDA-MB-231 cells	Cytotoxicity assay		24 h	Cytotoxic activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay, IC50 = 0.24 μM.	28705432
Vero cells	Cytotoxicity assay		2 days	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 2 days by cell-titer-glo luminescent assay, TC50 = 0.0024 μM.	28763645
L929 cells	Antiproliferative activity assay		5 days	Antiproliferative activity against mouse L929 cells after 5 days by WST-1 assay, IC50 = 0.2 μM.	28956915
KB-3-1 cells	Antiproliferative activity assay		5 days	Antiproliferative activity against human KB-3-1 cells after 5 days by WST-1 assay, IC50 = 0.2 μM.	28956915
MCF7 cells	Antiproliferative activity assay		5 days	Antiproliferative activity against human MCF7 cells after 5 days by WST-1 assay, IC50 = 1.8 μM.	28956915
FS4-LTM cells	Antiproliferative activity assay		24 h	Antiproliferative activity against human FS4-LTM cells after 24 hrs by WST-1 assay, IC50 = 2.8 μM.	28956915
Vero cells	Cytotoxicity assay		2 days	Cytotoxicity against African green monkey Vero cells after 2 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.0024 μM.	28993106
HepG2 cells	Cytotoxicity assay	100 uM	3 days	Cytotoxicity against human HepG2 cells at 100 uM after 3 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.018 μM.	28993106
NIH/3T3 cells	Cytotoxicity assay		96 h	Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, EC50 = 0.008 μM.	29197730
518A2 cells	Cytotoxicity assay		96 h	Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, EC50 = 0.03 μM.	29197730
A549 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A549 cells after 96 hrs by SRB assay, EC50 = 0.04 μM.	29197730
MCF7 cells	Cytotoxicity assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, EC50 = 0.1 μM.	29197730
A2780 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, EC50 = 0.12 μM.	29197730
HT-29 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, EC50 = 0.15 μM.	29197730
PC3 cells	Cytotoxicity assay			Cytotoxicity against human PC3 cells by sulforhodamine B assay, IC50 = 0.017 μM.	29389122
HCT116 cells	Cytotoxicity assay			Cytotoxicity against human HCT116 cells by sulforhodamine B assay, IC50 = 0.055 μM.	29389122
insect cells	Function assay		30 mins	Inhibition of recombinant human PDGFRbeta expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 30 mins by LANCE method, IC50 = 0.00076 μM.	29549836
Sf9 insect cells	Function assay		60 mins	Inhibition of recombinant human KDR expressed in Sf9 insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.0021 μM.	29549836
insect cells	Function assay		10 mins	Inhibition of recombinant human Src expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 10 mins by LANCE method, IC50 = 0.005 μM.	29549836
insect cells	Function assay		15 mins	Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM.	29549836
insect cells	Function assay		15 mins	Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM.	29549836
Sf9 insect cells	Function assay		15 mins	Inhibition of recombinant human Flt1 expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 15 mins by LANCE method, IC50 = 0.035 μM.	29549836
Sf21 insect cells	Function assay		15 mins	Inhibition of recombinant human Aurora-A expressed in Sf21 insect cells using Ulight-RRRSLLE as substrate after 15 mins by LANCE method, IC50 = 0.039 μM.	29549836
insect cells	Function assay		60 mins	Inhibition of recombinant human AKT1 expressed in insect cells using CREBtide as substrate after 60 mins by LANCE method, IC50 = 0.056 μM.	29549836
Sf9 insect cells	Function assay		60 mins	Inhibition of recombinant human FAK expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.062 μM.	29549836
insect cells	Function assay		60 mins	Inhibition of recombinant human ABL expressed in insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.29 μM.	29549836
insect cells	Function assay		60 mins	Inhibition of recombinant human c-MET expressed in insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.31 μM.	29549836
PC3 cells	Cytotoxicity assay		72 h	Cytotoxicity against human PC3 cells after 72 hrs by SRB assay, IC50 = 0.039 μM.	29558119
Sf9 cells	Function assay		45 mins	Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.047 μM.	29902719
Sf9 cells	Function assay		45 mins	Inhibition of recombinant human N-terminal GST-tagged HER2 (679 to 1255 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.0608 μM.	29902719
HT-29 cells	Function assay		3 h	Inhibition of mitochondrial membrane potential in human HT-29 cells after 3 hrs by JC-1 staining based fluorescence assay, IC50 = 0.02 μM.	30057155
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM.	30067358
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM.	30067358
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM.	30067358
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM.	30067358
HCT116 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.03 μM.	30106291
Huh7.5 cells	Cytotoxicity assay		48 h	Cytotoxicity against human Huh7.5 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.6 μM.	30106291
K562 cells	Cytotoxicity assay		48 h	Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 1.7 μM.	30106291
LO2 cells	Cytotoxicity assay		48 h	Cytotoxicity against human LO2 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 9.5 μM.	30106291
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	466.53	화학식	C₂₈H₂₆N₄O₃	보관 (수령일로부터)	3년-20°C분말
CAS 번호	62996-74-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	AM-2282，Antibiotic AM-2282			Smiles	CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC

용해도

In vitro
배치:

DMSO : 46 mg/mL (98.6 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (199.34 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (199.34 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (199.34 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (199.34 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	5.000mg/ml (10.72mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC₅₀/Ki	PKCα (Cell-free assay) 2 nM c-Fgr (Cell-free assay) 2 nM phosphorylase kinase (Cell-free assay) 3 nM PKCη (Cell-free assay) 4 nM PKCγ (Cell-free assay) 5 nM S6 kinase (Cell-free assay) 5 nM v-Src (Cell-free assay) 6 nM Cdc2 (Cell-free assay) 9 nM Cdc2 (Cell-free assay) 9 nM PKA (Cell-free assay) 15 nM Syk (Cell-free assay) 16 nM PKG (Cell-free assay) 18 nM PKCδ (Cell-free assay) 20 nM CaMKII (Cell-free assay) 20 nM Lyn (Cell-free assay) 20 nM MLCK (Cell-free assay) 21 nM PKCε (Cell-free assay) 73 nM
시험관 내(In vitro)	미생물 알칼로이드인 Staurosporine (STS)은 2.7 nM의 IC50으로 쥐 뇌의 단백질 키나아제 C를 유의하게 억제합니다. 또한 4 nM의 IC50으로 HeLa S3 세포에 대해 강력한 억제 효과를 나타냅니다. 이 화합물은 PKA, PKG, 포스포릴라제 키나아제, S6 Kinase, Myosin light chain kinase (MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr 및 Syk를 포함한 다양한 다른 단백질 키나아제를 각각 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM 및 16 nM의 IC50으로 억제합니다. 1 μM에서 PC12 세포에서 >90%의 세포자멸사를 유도합니다. 일관되게, 이 치료는 세포 내 유리 칼슘 수준 [Ca²⁺]_i의 빠르고 지속적인 상승, 미토콘드리아 활성 산소 종 (ROS)의 축적, 그리고 이어서 미토콘드리아 기능 장애를 유도합니다. STS에 의해 유도된 MCF7 세포의 세포자멸사는 카스파아제-8 활성화 및 Bid 절단을 통한 기능성 카스파아제-3의 발현에 의해 향상될 수 있습니다. 1 μM에서의 치료는 IL-3-자극 Bcl2 인산화를 부분적으로만 억제하지만 PKC-매개 Bcl2 인산화는 완전히 차단합니다. 이는 리소좀 카텝신 D 매개 사이토크롬 c 방출 및 카스파아제 활성화에 따라 인간 포피 섬유아세포 AG-1518의 세포자멸사를 유도합니다. 고전적인 미토콘드리아 세포자멸사 경로를 활성화하는 것 외에도, STS는 Apaf-1이 없는 상태에서 카스파아제-9의 활성화에 의존하는 새로운 내인성 세포자멸사 경로를 유발합니다.
키나아제 분석	효소 분석 및 결합 분석
키나아제 분석	단백질 키나아제 C는 5 μmol의 Tris/HCl, pH 7.5, 2.5 μmol의 마그네슘 아세테이트, 50 μg의 히스톤 II S, 20 μg의 포스파티딜세린, 0.88 μg의 디올레인, 125 nmol의 CaCl₂, 1.25 nmol의 [γ-³²]ATP (5-10 × 10⁴ cpm/nmol) 및 5 μg의 부분 정제된 효소를 포함하는 반응 혼합물 (0.25 mL)에서 분석됩니다. [³H]PDBu의 단백질 키나아제 C에 대한 결합이 결정됩니다: 반응 혼합물 (200 μL)에는 4 μmol의 Tris/말레이트, pH 6.8, 20 μmol의 KCl, 30 nmol의 CaCl₂, 20 μg의 포스파티딜세린, 5 μg의 부분 정제된 단백질 키나아제 C, 0.5% (최종 농도)의 DMSO, 10 pmol의 [³H]PDBu (1-3 × 10⁴ cpm/pmol) 및 다양한 양의 Staurosporine (STS) 10 μL가 포함되었습니다.
생체 내(In vivo)	저빌 및 쥐 허혈 모델에서, 허혈 전 Staurosporine (STS) (0.1–10 ng) 전처리는 용량 의존적으로 신경 손상을 예방하며, 이는 허혈 후 CA1 피라미드 세포 사멸에 PKC가 관여함을 시사합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/3457562/ [2] https://pubmed.ncbi.nlm.nih.gov/8529658/ [3] https://pubmed.ncbi.nlm.nih.gov/9486765/ [4] https://pubmed.ncbi.nlm.nih.gov/10734071/ [5] https://pubmed.ncbi.nlm.nih.gov/10677502/ [6] https://pubmed.ncbi.nlm.nih.gov/14576777/ [7] https://pubmed.ncbi.nlm.nih.gov/21659556/ [8] https://pubmed.ncbi.nlm.nih.gov/2384538/

적용 분야

방법	바이오마커	PMID
Western blot	p-Akt / Akt / PARP /Cleaved PARP FAK / RIP Ambra1	24174874
Growth inhibition assay	Cell viability	25215174
Immunofluorescence	Tubulin / Actin Phalloidin / Type II collagen Pyk2 Annexin cleaved-caspase 3 FAK 4.47	25215174

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT05209347	Withdrawn	Ankle Fractures\|Post-traumatic Osteoarthritis\|Osteoarthritis Ankle	University of Iowa	December 2024	Not Applicable
NCT05956990	Not yet recruiting	Colorectal Cancer Survivor\|Rehabilitation\|Quality of Life	Qu Shen\|The First Affiliated Hospital of Xiamen University\|Xiamen University	July 1 2024	Not Applicable
NCT05957289	Not yet recruiting	Rehabilitation\|Colorectal Cancer Survivor\|Quality of Life\|Pilot Study	Qu Shen\|The First Affiliated Hospital of Xiamen University\|Xiamen University	June 1 2024	Not Applicable
NCT06245135	Not yet recruiting	Mobility Limitation	University of Toronto\|University Health Network Toronto\|March of Dimes Canada\|Heart and Stroke Foundation of Canada\|University of Alberta\|University of Manitoba\|Bruyere Research Institute	June 2024	Not Applicable
NCT06374108	Not yet recruiting	Multiple Sclerosis	University of Aarhus\|Aarhus University Hospital\|University of Copenhagen	May 1 2024	Not Applicable

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C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):