I-BET151 (GSK1210151A)
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I-BET151 (GSK1210151A) 속성
- 밀도
- 1.314
- 저장 조건
- 2-8°C
- 용해도
- DMSO: 용해성20mg/mL, 투명
- 물리적 상태
- 가루
- 산도 계수 (pKa)
- 11.14±0.20(Predicted)
- 색상
- 흰색에서 베이지색
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
I-BET151 (GSK1210151A) C화학적 특성, 용도, 생산
개요
The bromodomain and extra terminal domain (BET) family of proteins including BRD2, BRD3, and BRD4 play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. I-BET151 is an isoxazole class pan-BET family inhibitor, blocking BRD2, BRD3, and BRD4 with IC50 values of 0.5, 0.25, and 0.79 μM, respectively. Through this action, it blocks the growth of leukemic cell lines driven by mixed lineage leukemia (MLL) fusions at nanomolar concentrations, whereas tyrosine kinase activated cells were much less sensitive. Specifically, I-BET151 induces apoptosis via reduced expression of BCL2 or triggers G0/G1 cell cycle arrest in MLL-fusion cell lines. I-BET151 is effective in vivo, suppressing MLL leukemia progression in two different mouse models.화학적 성질
Off-White Solid용도
I-BET 151 is part of a novel series of quinoline isoxazole BET family bromodomain inhibitors, a family of four proteins that selectively bind to aceylated lysine residues in histone. I-BET 151 play ke y roles in many cellular processes, including anti-inflammatory gene expression, mitosis, and viral/host interaction by controlling the conformation of histone acetylation -dependent chromatin complex es. Studies have shown that I-BET 151 increased ApoA1 expression within the nanomolar range in human hepatic cell line HepG2. The upregulation by I-BET 151 suggested potential anti-inflammatory activi ties upon administration.I-BET151 (GSK1210151A) 준비 용품 및 원자재
원자재
GSK1210151A S isomer
7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-(1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one
[3-(3,5-diMethyl-4-isoxazolyl)-4-(Methyloxy)phenyl]aMine
3,5-Dimethylisoxazole-4-boronic acid
4-(2-methoxy-5-nitrophenyl)-3,5-dimethylisoxazole
diethyl 2-((3-(3,5-dimethylisoxazol-4-yl)-4-methoxyphenylamino)methylene)malonate
4-chloro-7-(3,5-dimethylisoxazol-4-yl)-6-methoxyquinoline-3-carboxamide
3-QuinolinecarboxaMide, 7-(3,5-diMethyl-4-isoxazolyl)-6-Methoxy-4-[[(1R)-1-(2-pyridinyl)ethyl]aMino]-
2-Iodo-4-nitroanisole
준비 용품
I-BET151 (GSK1210151A) 공급 업체
글로벌( 135)공급 업체
| 공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32686 | 60 |
| Biochempartner | 0086-13720134139 |
candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 |
linda@hubeijusheng.com | CHINA | 28180 | 58 |
| BOC Sciences | +1-631-485-4226 |
inquiry@bocsci.com | United States | 19553 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
sales@conier.com | China | 49391 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; |
factory@coreychem.com | China | 29826 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 |
marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 |
sales@hzclap.com | CHINA | 6313 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 |
1026@dideu.com | China | 28812 | 58 |
| Dayang Chem (Hangzhou) Co.,Ltd. | 571-88938639 +8617705817739 |
info@dycnchem.com | CHINA | 52867 | 58 |