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Necrostatin-1 (Nec-1) RIPK1 억제제

Name: Necrostatin-1 (Nec-1)
Brand: Selleck Chemicals
SKU: S8037
Rating: 5 (317 reviews)

제품 번호S8037

Necrostatin-1 (Nec-1)은 특이적인 RIP1 (RIPK1) 억제제이며 293T 세포에서 490 nM의 EC50으로 TNF-α 유도 괴사 세포 사멸을 억제합니다. Necrostatin-1은 또한 IDO를 차단하고 Autophagy 및 Apoptosis를 억제합니다.

Necrostatin-1 (Nec-1) RIP kinase 억제제 Chemical Structure

화학 구조

분자량: 259.33

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품질 관리

배치: 순도: 99.97%

99.97

관련 타겟	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
기타 RIP kinase 억제제	Necrostatin 2 racemate (Nec-1s) GSK872 Mito-TEMPO GSK'963 RIPA-56 GSK2982772 Resibufogenin GSK583 HS-1371 GSK2983559 (compound 3)

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
HT-22	Cytotoxicity Assay	10 μM	12 h		protects against cell death induced by 5 mmol/L glutamate	17760869
Jurkat	Function Assay	200 μm	30 min		reduces Naegleria fowleri-induced reactive oxygen species (ROS) generation	21535020
Jurkat	Cytotoxicity Assay	50/ 100/200 μm	1/3 h		reduces Naegleria fowleri-induced cytotoxicity	21535020
SW13	Cell Viability Assay	100 μM	24 h	DMSO	increases cellular survival	22136818
8505c	Cell Viability Assay	100 μM	24 h	DMSO	increases cellular survival	22136818
TPC-1	Cell Viability Assay	100 μM	24 h	DMSO	increases cellular survival	22136818
L929sA	Apoptosis Assay	10 μM	1 h		abrogates the interaction of caspase-8 with FADD	22362767
L929sA	Apoptosis Assay	10 μM	1 h		rescues cells expressing RIPK1ΔID from TNF-induced apoptosis	22362767
L929sA	Apoptosis Assay	10 μM	1 h		inhibits the apoptotic response to TNF	22362767
K562/Adr	Function Assay	60 μM	12 h		increases the activity of caspases, caspase 8 and 9	22837689
K562	Function Assay	60 μM	12 h		increases the activity of caspases, caspase 8 and 9	22837689
HL60/Adr	Function Assay	60 μM	12 h		increases the activity of caspases, caspase 8 and 9	22837689
HL60	Function Assay	60 μM	12 h		increases the activity of caspases, caspase 8 and 9	22837689
K562/Adr	Function Assay	60 μM	12 h		augments the caspase-3 activity	22837689
K562	Function Assay	60 μM	12 h		augments the caspase-3 activity	22837689
HL60/Adr	Function Assay	60 μM	12 h		augments the caspase-3 activity	22837689
HL60	Function Assay	60 μM	12 h		augments the caspase-3 activity	22837689
K562/Adr	Apoptosis Assay	60 μM	12 h		enhances shikonin-induced apoptosis	22837689
K562	Apoptosis Assay	60 μM	12 h		enhances shikonin-induced apoptosis	22837689
HL60/Adr	Apoptosis Assay	60 μM	12 h		enhances shikonin-induced apoptosis	22837689
HL60	Apoptosis Assay	60 μM	12 h		enhances shikonin-induced apoptosis	22837689
SH-EP	Apoptosis Assay	10 μM	72 h		inhibits IAP inhibitor- and Lexatumumab-induced apoptosis	22890322
NIH3T3	Function Assay	10/50 μM	1/3 h		ameliorates TNFα-driven complex formation	23261677
HT-22	Function Assay	25 μM	0–30 min	DMSO	inhibits ERK Activation induced by glutamate	23307752
HT-22	Cell Viability Assay	10 μM	12 h	DMSO	protects against glutamate-induced cell death	23307752
KMS-12-BM	Cytotoxicity Assay	90 µM	1 h		blocks BAY 11-7082 induced rapid cell swelling	23527154
MM.1S	Cytotoxicity Assay	90 µM	1 h		blocks BAY 11-7082 induced rapid cell swelling	23527154
ΔN-Karpas 299	Cytotoxicity Assay	20 μM	16 h		inhibits CD30-induced cell death	23545938
MEFs	Function Assay	20 μM	1/2/4 h		suppresses TNFα-induced RIPK1 phosphorylation	23727581
MEFs	Cytotoxicity Assay	2/6/20 μM	18 h		inhibits TNFα-induced cell death in RelA KO MEFs	23727581
RMS13	Cell Viability Assay	40 μg/ml	24 h		rescues GX15-070-induced loss of cell viability	23744296
TE671	Cell Viability Assay	40 μg/ml	24 h		rescues GX15-070-induced loss of cell viability	23744296
U87	Function Assay	1 mmol/L	1.5-3 h		suppresses the expression of RIP-1 caused by shikonin	23840441
C6	Function Assay	1 mmol/L	1.5-3 h		suppresses the expression of RIP-1 caused by shikonin	23840441
U87	Cytotoxicity Assay	1 mmol/L	3 h		blocks shikonin induced necrosis	23840441
C6	Cytotoxicity Assay	1 mmol/L	3 h		blocks shikonin induced necrosis	23840441
U87	Cell Viability Assay	1 mmol/L	3 h		attenuates Shikonin induced glioma cell death	23840441
C6	Cell Viability Assay	1 mmol/L	3 h		attenuates Shikonin induced glioma cell death	23840441
L929	Function Assay	5 μg/ml	24 h		blocks zVAD induced necroptosis and autophagy	23941769
L929	Function Assay	2 μg/ml	24 h		promots caspase-6 (p20) activity and procaspase-6 cleavage	23941769
L929	Growth Inhibition Assay	2/5 μg/ml	24 h		reverses the cell growth inhibition and cell death induced by TNFα alone as well as TNFα + zVAD	23941769
L929	Function Assay	2/5 μg/ml	24 h		reversed the autophagy induced by TNFα alone as well as TNFα + zVAD	23941769
NRK-52E	Cell Viability Assay	20 μM	24 h		inhibits increased Drp1 protein expression after TNF-α Stimulation and ATP Depletion	24351845
NRK-52E	Cell Viability Assay	20 μM	24 h		increases cell viability after TNF-α Stimulation and ATP Depletion	24351845
NRK-52E	Cell Viability Assay	20 μM	24 h		protects cells from cell death caused by ischemia injury	24351845
AGS	Cell Viability Assay	60 μm	1 h		prevents shikonin-induced cell death	24463199
L-540	Cell Viability Assay	60 μm	1 h		reduces the Givinostat/Sorafenib-induced cell death	24561519
L-540	Function Assay	60 μm	1 h		prevents the mitochondrial membrane depolarization	24561519
L-540	Function Assay	60 μm	1 h		prevents the generation of ROS	24561519
SK-Hep1	Function Assay	60 μM	18 h		blocks β-lapachone-mediated PAR accumulation and AIF translocation to the cytosol	24832602
SK-Hep1	Function Assay	60 μM	18 h		inhibits β-Lapachone-induced leakage of HMGB-1	24832602
SK-Hep1	Function Assay	60 μM	18 h		blocks β-lapachone-induced morphological change, cell death and PI uptake	24832602
OHC	Function Assay	300 μM		DMSO	increases the number of apoptotic OHCs without altering the levels of CC8 after noise exposure	24874734
OHC	Function Assay	300 μM		DMSO	diminishes noise-induced AMPK activation	24874734
OHC	Function Assay	300 μM		DMSO	results in a reduction of noise-induced RIP1 and RIP3 immunofluorescence	24874734
OHC	Function Assay	300 μM		DMSO	decreases noise-induced swollen nuclei	24874734
OHC	Function Assay	300 μM		DMSO	increases noise-induced condensed nuclei	24874734
Huh7	Cell Viability Assay	50 µM	24/48 h	DMSO	prevents cell death of rAdHCV co-infected Huh7 cells	24973240
L929	Cell Viability Assay	30 μM	1 h		inhibits TNF-α-induced cleavage of Topo I	25095742
L929	Cell Viability Assay	30 μM	1 h		inhibits TNF-α-induced loss of cell viability	25095742
L929-A	Function Assay	50 μM	12 h		inhibits the TNFα-induced loss of mitochondrial membrane permeability	25398540
L929	Function Assay	50 μM	12 h		inhibits TNFα-induced Bid cleavage	25398540
L929-N	Function Assay	50 μM	12 h		blocks the cleavage of Caspase-3 and PARP	25398540
L929-A	Function Assay	50 μM	12 h		blocks the cleavage of Caspase-3 and PARP	25398540
L929-N	Cell Viability Assay	50 μM	24 h		blocks TNFα-induced cell death	25398540
L929-A	Cell Viability Assay	50 μM	24 h		blocks TNFα-induced cell death	25398540
KMS-12-PE	Cell Viability Assay	60 μM	5 h		inhibits SHK-induced cell death	25530098
SGC-7901	Cell Viability Assay	30 μM	1 h		suppresses oxaliplatin-mediated cell death	25767076
BxPC-3	Function Assay	20 μM	24 h		decreases the early necrotic cells	26000607
MiaPaCa-2	Function Assay	20 μM	24 h		decreases the early necrotic cells	26000607
NCI-H28	Cell Viability Assay	10 μM	24 h		prevents DAPE-induced reduction of NCI-H28 cell viability	26004138
BMDM	Function Assay	10 μM	30 min		protects cells from TAKI-induced LDH release	26381601
MEFs	Cell Viability Assay	10 μM	48 h	DMSO	inhibits zVAD-promoted death of CNOT3-depleted MEFs	26437789
A549	Cell Viability Assay	50 μM	24 h		inhibits MMS-induced cell death	26472723
Jurkat T	Necroptosis assay				Inhibition of TNF-alpha-induced necroptosis in FADD-deficient human Jurkat T cells, EC50 = 0.05 μM.	18467094
Jurkat	Function assay				Inhibition of endogenous RIP1 autophosphorylation in human Jurkat cells, EC50 = 0.182 μM.	18408713
Sf9	Function assay		30 mins		Inhibition of recombinant human GST-fused RIPK1 (1 to 497 residues) expressed in baculovirus infected insect Sf9 cells in presence of 32P-gamma-ATP after 30 mins by autoradiogram-based Western blot method, IC50 = 0.182 μM.	28280261
Jurkat T	Necroptosis assay				Effective concentration required for inhibition of necroptosis in FADD deficient Jurkat T cells treated with TNF-alpha, EC50 = 0.49 μM.	16153840
Jurkat	Necroptosis assay				Inhibition of cellular necroptosis in TNFalpha treated FADD deficient human Jurkat cells, EC50 = 0.49 μM.	18408713
Jurkat T	Necroptosis assay	30 uM	24 hrs		Inhibition of necroptosis in TNF-alpha-induced human Jurkat T cells assessed as cell viability at 30 uM after 24 hrs	18467094
L929	Necroptosis assay	30 uM	24 hrs		Inhibition of necroptosis in zVAD-induced mouse L929 cells assessed as cell viability at 30 uM after 24 hrs	18467094
L929	Necroptosis assay	30 uM	24 hrs		Inhibition of necroptosis in TNF-alpha-induced mouse L929 cells assessed as cell viability at 30 uM after 24 hrs	18467094
3T3	Cell death assay		24 hrs		Inhibition of death receptor signaling mediated necrotic cell death in mouse 3T3 cells assessed as cell viability after 24 hrs by ATP based viability assay in presence of TNFalpha and zVAD.fmk	16408008
3T3	Cell death assay		24 hrs		Inhibition of death receptor signaling mediated necrotic cell death in mouse 3T3 cells assessed as cell viability after 24 hrs by ATP based viability assay in presence of FasL and zVAD.fmk	16408008
MEF	Cell death assay		16 hrs		Inhibition of death receptor signaling mediated necrotic cell death in SV40 transformed mouse MEF cells assessed as cell viability after 16 hrs by ATP based viability assay in presence of TNFalpha, CHX and zVAD.fmk	16408008
IEC18	Cell death assay				Inhibition of death receptor signaling mediated necrotic cell death in rat IEC18 cells assessed as cell viability in presence of TNFalpha and zVAD.fmk	16408008
HL60	Cell death assay				Inhibition of death receptor signaling mediated necrotic cell death in human HL60 cells assessed as cell viability in presence of TNFalpha and zVAD.fmk	16408008
L929	Cell death assay		24 hrs		Inhibition of death receptor signaling mediated necrotic cell death in mouse L929 cells assessed as cell viability after 24 hrs by ATP based viability assay in presence of TNFalpha	16408008
Jurkat	Necrosis assay				Inhibition of necrosis in human Jurkat cells assessed as nuclear condensation by bright field microscopy in presence of FasL, CHX and zVAD-fmk	16408008
Jurkat	Necrosis assay				Inhibition of necrosis in human Jurkat cells assessed as organelle swelling by bright field microscopy in presence of FasL, CHX and zVAD-fmk	16408008
Jurkat	Necrosis assay				Inhibition of necrosis in human Jurkat cells assessed as early loss of plasma membrane integrity by bright field microscopy in presence of FasL, CHX and zVAD-fmk	16408008
Jurkat	Necrosis assay				Inhibition of necrosis in human Jurkat cells assessed as appearance of translucent cytosol in presence of FasL, CHX and zVAD-fmk	16408008
Jurkat	Necrosis assay				Inhibition of necrosis in human Jurkat cells deficient in FADD assessed as inhibition of nuclear condensation by bright field microscopy in presence of TNFalpha	16408008
Jurkat	Necrosis assay				Inhibition of necrosis in human Jurkat cells deficient in FADD assessed as inhibition of organelle swelling by bright field microscopy in presence of TNFalpha	16408008
Jurkat	Necrosis assay				Inhibition of necrosis in human Jurkat cells deficient in FADD assessed as inhibition of early loss of plasma membrane integrity by bright field microscopy in presence of TNFalpha	16408008
Jurkat	Necrosis assay				Inhibition of necrosis in human Jurkat cells deficient in FADD assessed as inhibition of appearance of translucent cytosol in presence of TNFalpha	16408008
U937	Cell death assay		48 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human U937 cells assessed as cell viability after 48 hrs by ATP based viability assay in presence of TNFalpha and zVAD-fmk	16408008
3T3	Cell death assay		24 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in mouse 3T3 cells assessed as cell viability after 24 hrs by ATP based viability assay in presence of TNFalpha and zVAD-fmk	16408008
Jurkat	Cell death assay		24 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD assessed as decreased levels of PE-conjugated LC3-II (autophagy marker) after 24 hrs by Western blot method in presence of TNFalpha	16408008
L929	Cell death assay		24 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in mouse L929 cells assessed as decreased levels of PE-conjugated autophagy marker LC3-II after 24 hrs by Western blot method in presence of TNFalpha	16408008
3T3	Cell death assay		24 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in mouse 3T3 cells assessed as decreased levels of PE-conjugated autophagy marker LC3-II after 24 hrs by Western blot method in presence of TNFalpha and zVAD-fmk	16408008
3T3	Cell death assay		24 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in mouse 3T3 cells assessed as decreased levels of PE-conjugated autophagy marker LC3-II after 24 hrs by Western blot method in presence of FasL and zVAD-fmk	16408008
3T3	Cell death assay		24 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in mouse 3T3 cells assessed as decreased levels of PE-conjugated autophagy marker LC3-II after 24 hrs by Western blot method in presence of rapamycin	16408008
Jurkat	Cell death assay		48 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing FKBP12-based dimerization domain assessed as cell viability after 48 hrs by FACS in presence of AP1510, zVAD-fmk	16408008
Jurkat	Cell death assay		48 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP kinase assessed as cell viability after 48 hrs by FACS in presence of AP1510, zVAD-fmk	16408008
Jurkat	Cell death assay		48 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP K45M mutant assessed as cell viability after 48 hrs by FACS in presence of AP1510, zVAD-fmk	16408008
Jurkat	Cell death assay		48 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP kinase domain assessed as cell viability after 48 hrs by FACS in presence of AP1510, zVAD-fmk	16408008
Jurkat	Cell death assay		48 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing FKBP12-based dimerization domain assessed as cell viability after 48 hrs by FACS in presence of AP1510	16408008
Jurkat	Cell death assay		48 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP kinase assessed as cell viability after 48 hrs by FACS in presence of AP1510	16408008
Jurkat	Cell death assay		48 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP K45M mutant assessed as cell viability after 48 hrs by FACS in presence of AP1510	16408008
Jurkat	Cell death assay		48 hrs		Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP kinase domain assessed as cell viability after 48 hrs by FACS in presence of AP1510	16408008
Sf9	Function assay				Inhibition of human RIP1 K45M mutant autophosphorylation expressed in Sf9 cells	18408713
Jurkat	Cytoprotective assay	30 uM	1 hr		Cytoprotective activity against FasL-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by FasL stimulation measured after 20 hrs by Alamar blue assay	29541357
Jurkat	Cytoprotective assay	30 uM	1 hr		Cytoprotective activity against CHX-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by CHX stimulation by Alamar blue assay	29541357
Jurkat	Cytoprotective assay	30 uM	1 hr		Cytoprotective activity against Z-VAD-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by Z-VAD stimulation by Alamar blue assay	29541357
Jurkat	Cytoprotective assay	30 uM	1 hr		Cytoprotective activity against FasL-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by FasL stimulation measured after 20 hrs by phase contrast microscopy	29541357
Jurkat	Cytoprotective assay	30 uM	1 hr		Cytoprotective activity against CHX-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by CHX stimulation by phase contrast microscopy	29541357
Jurkat	Cytoprotective assay	30 uM	1 hr		Cytoprotective activity against Z-VAD-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by Z-VAD stimulation by phase contrast microscopy	29541357
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	259.33	화학식	C₁₃H₁₃N₃OS	보관 (수령일로부터)	3년-20°C분말
CAS 번호	4311-88-0	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	Nec-1			Smiles	CN1C(=O)C(NC1=S)CC2=CNC3=CC=CC=C32

용해도

In vitro
배치:

DMSO : 57 mg/mL (219.79 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 52 mg/mL (200.51 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 51 mg/mL (196.66 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 52 mg/mL (200.51 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 51 mg/mL (196.66 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.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.850mg/ml (10.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 57 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 10%PEG 300 2 85 %ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	1.200mg/ml (4.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clarified DMSO stock solution to 100 μL of PEG300, mix evenly to clarify it; add 850 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.
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

특징	A powerful tool for characterizing the role of necroptosis with characterized primary target.
Targets/IC₅₀/Ki	IDO RIP1 (293T cells) 490 nM(EC50)
시험관 내(In vitro)	Necrostatin-1 (1-100 μM)은 과발현된 및 내인성 RIP1의 자가인산화를 억제합니다. RIP1은 이 화합물의 괴사 세포 사멸 억제 활성에 책임이 있는 주요 세포 표적임이 밝혀졌습니다. 이 화학 물질은 다양한 세포 유형에서 다양한 자극에 의해 유발되는 괴사 세포 사멸을 효율적으로 억제합니다. 이전에 괴사 세포 사멸의 저분자 억제제로 확인된 이 물질은 RIP kinase 유도 괴사 세포 사멸을 억제하고 Jurkat 세포에서 490 nM의 EC50으로 TNF-α 유도 괴사 세포 사멸을 억제합니다.
키나아제 분석	RIP1 키나아제 분석
키나아제 분석	RIP1의 인산화는 키나아제 활성을 필요로 한다. FLAG가 표지된 야생형(WT) 또는 키나아제 비활성 점 돌연변이 RIP1(K45M)의 발현 벡터는 293T 세포에 형질감염되고, RIP1 키나아제 분석은 [γ-³²P]ATP 존재 하에 30℃에서 30분 동안 Methods에 기술된 대로 수행된다. 샘플은 SDS-PAGE에 로딩되고 RIP1 밴드는 자가방사선 사진으로 시각화된다. 방사성 밴드의 상대적 강도는 정량화되어 이 및 다른 모든 자가방사선 사진에 (비율로) 표시된다. 키나아제 반응과 병행하여, 비드 샘플은 항-RIP1 항체를 사용하여 웨스턴 블롯 분석에 로딩되어 키나아제 반응에서 동등한 단백질 양을 보장한다.
생체 내(In vivo)	Necrostatin-1 (Nec-1)은 수용체 상호작용 단백질 키나아제 1 (RIPK1)의 특정 저분자 억제제이며, 이 화합물의 인산화를 특이적으로 억제합니다.
참조	[1] http://www.ncbi.nlm.nih.gov/pubmed/?term=18408713 [2] http://www.ncbi.nlm.nih.gov/pubmed/?term=16408008 [3] https://pubmed.ncbi.nlm.nih.gov/30542285/

적용 분야

방법	바이오마커	이미지	PMID
Immunofluorescence	RIP1 / RIP3		30462730

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