Home NF-κB ADC Cytotoxin 화합물 Triptolide

연구용

Triptolide Hsp90 Middle Domain Inhibitor

제품 번호S3604

Triptolide는 중국 약초 Tripterygium wilfordii에서 추출한 디테르펜 트리에폭사이드 면역억제제입니다. 이는 p65/CBP 상호작용 방해 및 p65 단백질 감소를 통해 이중 작용으로 NF-κB 억제제 역할을 합니다. Triptolide (PG490)는 열충격 전사 인자 1 (HSF1)의 전사 활성 기능을 제거합니다. Triptolide는 MDM2를 억제하고 p53 비의존적 경로를 통해 세포자멸사를 유도합니다.
Triptolide ADC Cytotoxin 화합물 Chemical Structure

화학 구조

분자량: 360.4

바로가기

품질 관리

배치: 순도: 99.95%
99.95

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
HT-29 Cytotoxicity against Cytotoxicity against human HT-29 cells, IC50=0.0021μM 21470864
HCT116 Cytotoxicity against Cytotoxicity against human HCT116 cells assessed as decrease in cell viability, IC50=0.0047μM 31121546
SKOV3 Antiproliferative activity against 72 hrs Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay, IC50=0.006μM 20833543
SKOV3 Cytotoxicity against 72 hrs Cytotoxicity against human SKOV3 cells after 72 hrs by sulforhodamine B assay, IC50=0.006μM 24378709
SKOV3 Cytotoxic activity against 72 hrs Cytotoxic activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0072μM 28011223
KBM5 Cytotoxicity against 72 hrs Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.0083μM 20149665
SKOV3 Cytotoxicity against Cytotoxicity against human SKOV3 cells by SRB assay, IC50=0.009μM 19637874
MDA-MB-468 Cytotoxicity against Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=0.01μM 19637874
HCT116 Cytotoxicity against 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.01μM 19637874
SKOV3 Cytotoxicity against 72 hrs Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay, IC50=0.01μM 19637874
KBM5 Cytotoxicity against 72 hrs Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.0103μM 20149665
Rh30 Cytotoxicity against 72 hrs Cytotoxicity against human Rh30 cells after 72 hrs by MTT assay, IC50=0.014μM 19637874
A549 Antagonist activity at Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay, IC50=0.014μM 23895492
SGC7901 Cytotoxicity against 72 hrs Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay, IC50=0.015μM 19637874
MOLT4 Cytotoxicity against 72 hrs Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay, IC50=0.017μM 19637874
A549 Cytotoxic activity against 72 hrs Cytotoxic activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0175μM 28011223
SMMC7721 Cytotoxicity against 72 hrs Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50=0.018μM 19637874
PC3 Cytotoxic activity against 72 hrs Cytotoxic activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0183μM 28011223
MCF7 Cytotoxicity against 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50=0.019μM 19637874
A549 Cytotoxicity against Cytotoxicity against human A549 cells, IC50=0.019μM 21470864
PC3 Cytotoxicity against Cytotoxicity against human PC3 cells by SRB assay, IC50=0.02μM 19637874
Bel7402 Cytotoxicity against 72 hrs Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay, IC50=0.02μM 19637874
PC3 Antiproliferative activity against 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay, IC50=0.02μM 20833543
PC3 Cytotoxicity against 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by sulforhodamine B assay, IC50=0.02μM 24378709
PC3 Cytotoxicity against Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.02μM 25467158
786-O Cytotoxicity against 72 hrs Cytotoxicity against human 786-O cells after 72 hrs by MTT assay, IC50=0.022μM 19637874
A549 Antagonist activity at Antagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISA, IC50=0.023μM 23895492
MDA-MB-231 Cytotoxicity against 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.024μM 19637874
DU145 Cytotoxicity against 72 hrs Cytotoxicity against human DU145 cells after 72 hrs by MTT assay, IC50=0.024μM 19637874
HO8910 Cytotoxicity against 72 hrs Cytotoxicity against human HO8910 cells after 72 hrs by MTT assay, IC50=0.028μM 19637874
HCT15 Cytotoxicity against 72 hrs Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay, IC50=0.029μM 19637874
A549 Growth inhibition of human Growth inhibition of human A549 cells, IC50=0.03μM 28814374
32D Cytotoxicity against 72 hrs Cytotoxicity against mouse 32D cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.032μM 20149665
U251 Cytotoxicity against Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.033μM 25467158
32D Cytotoxicity against 72 hrs Cytotoxicity against imatinib-resistant mouse 32D cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.034μM 20149665
PC3 Cytotoxicity against 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=0.043μM 19637874
KB Cytotoxicity against 72 hrs Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=0.043μM 19637874
HepG2 Cytotoxicity against 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs by XTT assay, IC50=0.0433μM 30613335
HeLa Cytotoxicity against 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=0.047μM 19637874
U251 Cytotoxicity against 72 hrs Cytotoxicity against human U251 cells after 72 hrs by MTT assay, IC50=0.049μM 19637874
K562 Cytotoxicity against 72 hrs Cytotoxicity against human K562 cells after 72 hrs by MTT assay, IC50=0.05μM 19637874
NIH/3T3 Cytotoxicity against Cytotoxicity against mouse NIH/3T3 cells assessed as decrease in cell viability, IC50=0.05μM 31121546
SW1116 Cytotoxicity against 72 hrs Cytotoxicity against human SW1116 cells after 72 hrs by MTT assay, IC50=0.052μM 19637874
A549 Cytotoxicity against 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=0.059μM 19637874
HeLa Cytotoxicity against Cytotoxicity against human HeLa cells assessed as decrease in cell viability, IC50=0.087μM 31121546
Jurkat Cytotoxicity against Cytotoxicity against human Jurkat cells assessed as decrease in cell viability, IC50=0.14μM 31121546
MKN28 Cytotoxicity against 72 hrs Cytotoxicity against human MKN28 cells after 72 hrs by MTT assay, IC50=0.2μM 19637874
MDCK Cytotoxicity against Cytotoxicity against MDCK cells assessed as decrease in cell viability, IC50=1.2μM 31121546
Pkd1-/- Induction of Induction of cell growth arrest in mouse Pkd1-/- cells in presence of calcium 17360534
Pkd1-/- Increase in 100 nM 96 hrs Increase in p21CIP/WAF expression in mouse Pkd1-/- cells at 100 nM after 96 hrs by Western blot analysis 17360534
Pkd1+/- Increase in 100 nM Increase in PC2 dependent calcium release in mouse Pkd1+/- cells at 100 nM 17360534
Pkd1-/- Increase in 100 nM Increase in PC2 dependent calcium release in mouse Pkd1-/- cells at 100 nM 17360534
Pkd1-/- Increase in 50 uM Increase in calcium release in mouse Pkd1-/- cells at 50 uM in presence of RyR antagonist dantrolene 17360534
Pkd2+/- Growth inhibition of PC2 expressing mouse 100 nM 24 hrs Growth inhibition of PC2 expressing mouse Pkd2+/- cells as cell death at 100 nM after 24 hrs 17360534
KBM5 Cytotoxicity against 0.001 to 17 uM 72 hrs Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl at 0.001 to 17 uM after 72 hrs by MTS assay 20149665
KBM5 Cytotoxicity against 0.001 to 17 uM 72 hrs Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant at 0.001 to 17 uM after 72 hrs by MTS assay 20149665
LNCAP Antagonist activity at 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
LNCAP Antagonist activity at 500 nM 24 hrs Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 500 nM after 24 hrs by dual luciferase reporter gene assay 27994731
HepG2 Antitumor activity against 0.2 mg/kg 15 days Antitumor activity against human HepG2 cells xenografted in Balb/c nude mouse assessed as reduction in tumor growth at 0.2 mg/kg, ip administered once daily for 15 days 30613335
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 360.4 화학식

C20H24O6

 보관 (수령일로부터)
CAS 번호 38748-32-2 SDF 다운로드 원액 보관

용해도

In vitro
배치:

DMSO : 72 mg/mL (199.77 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

Targets/IC50/Ki
NF-κB
HSF1
MDM2
시험관 내(In vitro)
Triptolide는 강력한 면역억제 및 항염증 특성을 가진 디테르펜 트리에폭사이드입니다. 이 화합물은 활성화된 T 세포에서 IL-2의 발현을 퓨린 박스/핵 인자 및 NF-κB 매개 전사 활성 수준에서 억제하는 것으로 나타났습니다. 이 화합물은 극히 낮은 농도(2–10 ng/mL)에서 종양 세포의 증식 및 콜로니 형성을 억제합니다. 이 화학물질은 유방, 위암 및 백혈병 세포주 HL-60 세포에 대한 억제 활성을 가집니다. NF-κB 활성화를 차단하고 TNF-α 유도 세포 사멸에 종양 세포를 민감하게 만듦으로써 종양 세포에서 세포자멸사를 유도합니다.
생체 내(In vivo)
Triptolide는 동물 모델에서 이식편 생존 촉진 및 동종 골수 이식에서 이식편대숙주병 억제에 사이클로스포린 A와 시너지 효과를 나타냅니다. 또한, 종양 세포에서 세포자멸사를 유도하고 c-IAP2 및 c-IAP1 유도를 억제함으로써 종양 괴사 인자(TNF-α)의 세포자멸사 유도를 강화합니다. 이 화합물로 2-3주간 치료하면 네 가지 다른 종양 세포주(B16 흑색종, MDA-435 유방암, TSU 방광암, MGC80-3 위암)에 의해 형성된 이종이식편의 성장을 억제하며, 이는 TPL이 야생형 및 돌연변이형 p53을 모두 포함하는 종양에 대해 광범위한 활성 스펙트럼을 가지고 있음을 나타냅니다. 또한, 마우스의 폐 및 비장으로의 B16F10 세포의 실험적 전이를 억제합니다. 다낭성 신장 질환의 마우스 모델에 대한 생체 내 및 생체 외 활성을 가지고 있습니다. LD50: 마우스 0.83mg/kg (i.v.).
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/17360534/
  • [5] https://pubmed.ncbi.nlm.nih.gov/23583804/

적용 분야

방법 바이오마커 이미지 PMID
Western blot c-Jun MDM2 p-AKT / AKT / p-Foxo3a / Foxo3a / p53 p-PI3K / PI3K / p85 / p110
S3604-WB1
22666381
Growth inhibition assay Cell viability
S3604-viability1
22666381

기술 지원

취급 설명서

Tel: +1-832-582-8158 Ext:3

다른 문의사항이 있으시면 메시지를 남겨주세요.

이름을 입력해주세요.
이메일을 입력해주세요. 유효한 이메일 주소를 입력해주세요.
저희에게 무엇이든 작성해주세요.