Home Proteases Proteasome 억제제 Celastrol

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Celastrol Proteasome 억제제

제품 번호S1290

Celastrol은 정제된 20S proteasome의 키모트립신 유사 활성에 대한 강력한 proteasome 억제제로, IC50은 2.5 μM입니다. 이 화합물은 ROS/JNK 신호 경로를 통해 apoptosis 및 autophagy를 유도합니다. mitophagy 활성화를 통해 파킨슨병의 도파민성 신경 세포 사멸을 억제합니다.
Celastrol Proteasome 억제제 Chemical Structure

화학 구조

분자량: 450.61

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품질 관리

배치: 순도: 99.64%
99.64

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production treated 3 hrs before LPS challenge assessed after 24 hrs by Griess reagent assay, IC50 = 0.23 μM. 11809076
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NF-kappaB activation treated 3 hrs before LPS challenge assessed after 24 hrs by SEAP reporter gene assay, IC50 = 0.27 μM. 11809076
RPMI8226 Growth inhibition assay Growth inhibition of human RPMI8226 cells, IC50 = 3 μM. 18164197
HeLa Function assay Inhibition of TNF-alpha-induced NF-kappaB activation in human HeLa cells by SEAP reporter gene assay, IC50 = 0.15 μM. 18841906
RAW264.7 Function assay Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells by SEAP reporter gene assay, IC50 = 0.3 μM. 18841906
SH-SY5Y Function assay Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50 = 0.03764 μM. 19138859
HeLa Function assay 2 hrs Amplification of HSF1 transcriptional activity in human heat shock-induced HeLa cells assessed as granule formation treated 1 hr before heat shock challenge measured after 2 hrs without recovery time by immunocytochemical staining, EC50 = 1.1 μM. 19502057
SK-N-SH Cytotoxicity assay 72 hrs Cytotoxicity against human SK-N-SH cells after 72 hrs by MTS assay, CC50 = 1.6 μM. 19502057
HeLa Function assay 3 hrs Amplification of HSF1 transcriptional activity in human HeLa cells assessed as granule formation pretreated for 3 hrs by immunocytochemical staining, EC50 = 2.6 μM. 19502057
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by MTS assay, CC50 = 3 μM. 19502057
HeLa Function assay Inhibition of NF-kappaB activity in human HeLa cells by SEAP reporter assay, IC50 = 0.15 μM. 20469887
LNCAP Antitumor assay Antitumor activity against human LNCAP cells, IC50 = 2.5 μM. 20627556
PC12 Cytoprotective assay Cytoprotective activity against t-BPH-induced cell damage in rat PC12 cells assessed as cell viability, IC50 = 3.15 μM. 20627556
PC12 Cytoprotective assay 1.6 uM Cytoprotective activity against t-BPH-induced cell damage in rat PC12 cells assessed as cell viability at 1.6 uM 20627556
THP1 Apoptosis assay 24 hrs Induction of apoptosis in TRAIL-resistant human THP1 cells after 24 hrs by annexin-V staining, EC50 = 15 μM. 20864342
293T Function assay 30 mins Inhibition of LPS-induced NF-kappaB activation in human 293T cells incubated for 30 mins followed by treated with LPS for 6 hrs by dual-luciferase reporter assay, IC50 = 0.17 μM. 21393004
293T Cytotoxicity assay Cytotoxicity against human 293T cells assessed as cell viability by dual-luciferase reporter assay, IC50 = 0.67 μM. 21393004
RAW264 Function assay 24 hrs Inhibition of LPS-induced NO production in mouse RAW264 cells after 24 hrs 21393004
NCI-H460 Cytotoxicity assay Cytotoxicity against human NCI-H460 cells after overnight incubation by MTT assay, IC50 = 12.3 μM. 21942765
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess reagent method, IC50 = 1 μM. 21978676
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by griess assay, IC50 = 1 μM. 22024033
RAW264.7 Function assay 18 hrs Inhibition of LPS-stimulated NFkappaB activation transfected in mouse RAW264.7 cells after 18 hrs by luciferase reporter gene assay, IC50 = 0.2 μM. 22705020
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CCR2 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in GRO/KC production at 200 ug, ip starting from arthritis onset and continued uninterrupted unti 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in MCP1 production at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in RANTES production at 200 ug, ip starting from arthritis onset and continued uninterrupted unti 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in TNFalpha production at 200 ug, ip starting from arthritis onset and continued uninterrupted un 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CCR3 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CCR6 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CXCR1 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CXCR2 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CXCR4 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Function assay 200 ug Increase in CCR1 expression in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation at 200 ug, ip starting from arthritis onset and continued uninterrupted until study end by qPCR relative baselin 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in IL-1beta production at 200 ug, ip starting from arthritis onset and continued uninterrupted un 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CCR5 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Function assay 24 hrs Increase in CCR1 protein surface expression in sonicated Mtb-stimulated spleen adherent cells isolated from Lewis rat adjuvant-induced arthritis model pre-incubated with 0.1 to 0.3 uM compound before stimulation with sonicated Mtb for 24 hrs by flow cytom 22854193
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method, IC50 = 1 μM. 23127886
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 24 hrs by ELISA, IC50 = 0.8 μM. 23234407
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide generation incubated for 24 hrs, IC50 = 1 μM. 23234407
RAW264.7 Antiinflammatory assay Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by Griess reaction based method, IC50 = 1 μM. 25637363
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay, IC50 = 0.153 μM. 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as pAkt degradation at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as Her2 degradation at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as Cdk6 degradation at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as Raf degradation at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Change in Cdc37 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Change in p23 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as disruption of interaction with Cdc37 at 5 times IC50 after 24 hrs by co-immunoprecipitation assay 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as disruption of interaction with p23 at 5 times IC50 after 24 hrs by co-immunoprecipitation assay 25756299
SGC7901 Anticancer assay 48 hrs Anticancer activity against human SGC7901 cells assessed as cell survival after 48 hrs by MTT assay, IC50 = 0.15 μM. 25812966
SMMC7721 Anticancer assay 48 hrs Anticancer activity against human SMMC7721 cells assessed as cell survival after 48 hrs by MTT assay, IC50 = 0.58 μM. 25812966
MGC803 Anticancer assay 48 hrs Anticancer activity against human MGC803 cells assessed as cell survival after 48 hrs by MTT assay, IC50 = 1.55 μM. 25812966
HepG2 Anticancer assay 48 hrs Anticancer activity against human HepG2 cells assessed as cell survival after 48 hrs by MTT assay, IC50 = 4.01 μM. 25812966
A549 Antiproliferative assay 48 hrs Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 2.01 μM. 27647369
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 2.02 μM. 27647369
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 2.13 μM. 27647369
PANC1 Antiproliferative assay 48 hrs Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 2.48 μM. 27647369
LNCAP Function assay 5 uM 24 hrs Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 5 uM after 24 hrs by dual luciferase reporter gene assay 27994731
A549 Growth inhibition assay 6 days Growth inhibition of human A549 cells measured every 2 hrs over 6 days by live cell imaging based method, IC50 = 0.69 μM. 28621943
HEK293 Function assay 10 uM 20 mins Inhibition of Galphao interaction with GFP-fused RGS17 (unknown origin) deltaN mutant expressed in HEK293 cells assessed as increase in RGS17 deltaN mutant localization at cytoplasm at 10 uM up to 20 mins by confocal microscopic analysis 28621943
HEK293 Function assay 100 uM 5 mins Inhibition of Galpha0 interaction with GFP-fused RGS17 (unknown origin) deltaN mutant expressed in HEK293 cells assessed as increase in RGS17 deltaN mutant localization at cytoplasm at 100 uM up to 5 mins by confocal microscopic analysis 28621943
HEK293 Function assay 10 uM 5 mins Inhibition of Galphao interaction with GFP-fused RGS17 (unknown origin) deltaN mutant expressed in HEK293 cells assessed as increase in RGS17 deltaN mutant localization at cytoplasm at 10 uM up to 5 mins by confocal microscopic analysis 28621943
MIAPaCa2 Antiproliferative assay 72 hrs Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay, IC50 = 0.46 μM. 28688281
SKBR3 Antiproliferative assay 72 hrs Antiproliferative activity against human SKBR3 cells after 72 hrs by MTT assay, IC50 = 0.72 μM. 28688281
SKOV3 Antiproliferative assay 72 hrs Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay, IC50 = 1.16 μM. 28688281
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 1.32 μM. 28688281
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 1.56 μM. 28688281
BJ Cytotoxicity assay 72 hrs Cytotoxicity against human BJ cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.74 μM. 28688281
NCI-H460 Function assay 1 uM 12 hrs Activation of HSF1 in human NCI-H460 cells assessed as upregulation of HSP25 protein levels at 1 uM after 12 hrs by Western blot analysis 28737916
NCI-H460 Function assay 1 uM 12 hrs Activation of HSF1 in human NCI-H460 cells assessed as upregulation of HSP70 protein levels at 1 uM after 12 hrs by Western blot analysis 28737916
NCI-H1299 Cytotoxicity assay Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
BCP-ALL Cytotoxicity assay Cytotoxicity in human BCP-ALL cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
T-ALL Cytotoxicity assay Cytotoxicity in human T-ALL cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
Daudi Cytotoxicity assay Cytotoxicity in human Daudi cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
HL60 Cytotoxicity assay Cytotoxicity in human HL60 cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 5.26 μM. 29486954
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 6.17 μM. 29486954
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 6.59 μM. 29486954
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 6.84 μM. 29486954
HEK293 Cytotoxicity assay Cytotoxicity against HEK293 cells (CO-ADD:MA_007); CC50 by cell viability assay in DMEM (10% FBS) media using TC plates, by Resazurin F(560/590), CC50 = 0.837 μM. ChEMBL
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 450.61 화학식

C29H38O4

 보관 (수령일로부터)
CAS 번호 34157-83-0 SDF 다운로드 원액 보관

동의어 NSC 70931, Tripterine Smiles CC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)O)C)C)C)C)O

용해도

In vitro
배치:

DMSO : 90 mg/mL (199.72 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:

생체 내 제형 계산기 (투명한 용액)

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

mg/kg g μL

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 potent antioxidant and anti-inflammatory drug.
Targets/IC50/Ki
20S proteasome
(Cell-free assay)
2.5 μM
시험관 내(In vitro)
5 μM의 Celastrol은 정제된 20S proteasome의 키모트립신 유사, PGPH 유사 및 트립신 유사 활성을 각각 80%, 5%, <1% 억제하는 반면, 10 μM에서는 이 세 가지 proteasome 활성을 각각 ~90%, 15%, <1% 억제합니다. 이 화합물은 PC-3 세포에서 농도 의존적으로 proteasome 키모트립신 활성을 유의하게 억제합니다. 2.5 μM ~ 5 μM에서 PC-3 세포의 caspase-3 활성을 4.7배 ~ 5.5배 유도합니다. 이 화학 물질(5 μM)로 처리된 세포에서 proteasome 표적 단백질인 IκB-α 및 Bax의 수준은 1시간 후 증가하고 4시간 ~ 12시간 동안 최고치로 더 증가합니다. 이 화합물(2.5 μM) 처리는 LNCaP 세포에서 키모트립신 유사 활성 감소 및 유비퀴틴화된 단백질 축적 증가로 나타나는 40%의 proteasome 억제를 유도합니다. Celastrol 처리된 LNCaP 세포에서 caspase-3 활성(최대 3.5배), PARP 분열 및 세포자멸 형태 증가로 나타나는 세포자멸사를 유도합니다(2.5 μM). 이 화합물(300 nM)은 인간 단핵구 및 대식세포에서 LPS 유도 TNF-알파 및 IL-1베타 생성을 억제하는 것으로 밝혀졌습니다. 또한 (100 nM) 미세아교세포에서 LPS 유도 클래스 II MHC 분자 발현을 감소시킵니다. 이 화학 물질은 대식세포 계열 세포에서 IC50이 200 nM인 LPS 및 IFN-γ 유도 NO 생성을 강력하게 억제합니다. 내피 세포에서 IC50이 200 nM인 TNF-α 및 IFN-γ 유도 NO 생성을 강력하게 억제합니다. 이 화합물(2.5 μM)은 KBM-5 세포에서 NF-kappaB 활성화에 의해 조절되는 TNF 및 화학 치료제 유도 세포자멸사를 강화하고 침윤을 억제합니다. 그것은 (2.5 μM) KBM-5 세포에서 항세포자멸사 (IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP 및 survivin), 증식 (cyclin D1 및 COX-2), 침윤 (MMP-9) 및 혈관 신생 (VEGF)에 관여하는 유전자 산물의 TNF 유도 발현을 억제합니다. 이 화학 물질 (5 μM)은 TNF 유도 IkappaBalpha 키나제 활성화, IkappaBalpha 인산화, IkappaBalpha 분해, p65 핵 전위 및 인산화, NF-kappaB 매개 리포터 유전자 발현을 억제하는 것으로 밝혀졌습니다. 그것은 RPMI 8226, KATOIII, UM-SCC1, U251MG 및 MDA-MB-231 세포의 증식을 각각 0.52 μM, 0.54 μM, 0.76 μM, 0.69 μM 및 0.67 μM의 IC50으로 억제합니다. 이 화합물 (1 μM)은 cyclin D1 및 cyclin E 수준 감소와 p21 및 p27 수준의 동시 증가와 함께 RPMI 8226의 성장을 억제합니다. 그것은 caspase-8 활성화, bid 분열, caspase-9 활성화, caspase-3 활성화, PARP 분열 및 항세포자멸사 단백질의 하향 조절을 통해 RPMI-8226 세포에서 세포자멸사를 유도합니다. 이 화학 물질 (1 μM)은 RPMI-8226 세포에서 Akt 경로를 억제하고 JNK 키나제를 활성화합니다.
키나아제 분석
정제된 20S proteasome 활성 억제
정제된 토끼 20S proteasome (0.1 μg)을 100 μL 분석 완충액 (20 mM Tris-HCl (pH 7.5))에서 40 μM의 다양한 형광 펩타이드 기질과 함께 Celastrol을 다양한 농도로 또는 용매 DMSO에 넣어 37℃에서 2시간 동안 배양한 후 각 proteasome 활성 억제를 측정합니다.
생체 내(In vivo)
Celastrol (3 mg/kg)은 PC-3 종양을 가진 수컷 누드 마우스에서 종양 성장을 유의하게 억제하고 (최대 70%) p27 수준 및 Bax 수준 증가와 관련이 있습니다. 이 화합물은 PC-3 종양을 가진 수컷 누드 마우스의 종양에서 다양한 PARP 분열 단편의 출현과 함께 더 많은 세포자멸사성 종양 세포를 유도합니다. C4-2B 종양을 가진 누드 마우스에서 proteasome 활성 감소 및 AR 단백질 발현 감소와 관련된 35%의 종양 억제를 유발합니다. 이 화학 물질은 마우스에서 관절 부종 및 기타 보조제 관절염의 증상을 강력하게 억제하는 것으로 밝혀졌습니다. 그것은 (0.2 mg/kg) 쥐의 기억, 학습 및 정신 운동 활동 테스트에서 성능을 유의하게 향상시킵니다.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/21786165/

적용 분야

방법 바이오마커 이미지 PMID
Western blot HIF-1α Akt / p-Akt / p-p70S6K PARP / p53 / p21 / cIAP1 / Bcl-xl / Bcl-2 IκBα / p-IKKα/β iNOS / COX-2 / Arg-1 Chk2 / p-Chk2 / Cyclin B1 / Cdc25c / p-Cdc25c
S1290-WB1
25383959
Immunofluorescence p21 / Nur77
S1290-IF1
28388439
Growth inhibition assay Cell viability
S1290-viability1
29040966

임상시험 정보

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

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT05494112 Recruiting
Safety
Legend Labz Inc.
 May 25 2022 Not Applicable
NCT05413226 Recruiting
Safety Issues
Legend Labz Inc.
 September 28 2021 Not Applicable

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