MS645 |
| Catalog No.GC38474 |
MS645는 BRD4-BD1/BD2에 대해 Ki가 18.4nM인 2가 BET 브로모도메인(BrD) 억제제입니다. MS645는 BRD4 BrDs의 2가 억제를 공간적으로 제한하여 고형 종양 세포에서 BRD4 전사 활성을 지속적으로 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2250091-96-2
Sample solution is provided at 25 µL, 10mM.
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MS645 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells[1].
MS645 has cell growth inhibitory effects on noncancer cell lines of mouse macrophage RAW cells and nontumorigenic breast epithelial MCF10A with IC50s of 4.1 nM, 6.8 nM, 7.9 nM for triple-negative breast cancer (TNBC) cell lines HS5878T, BT549, and MCF 10A[1]. MS645 (15, 30, 60 nM) results in a dramatic reduction of c-Myc expression and an increase of p21, a tumor suppressor and cell-cycle inhibitor in HCC1806 cells[1].
[1]. Ren C, et al. Spatially constrained tandem bromodomain inhibition bolsters sustained repression of BRD4 transcriptional activity for TNBC cell growth.Proc Natl Acad Sci U S A. 2018 Jul 31;115(31):7949-7954.
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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