| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 200 mg/mL (213.21 mM) | [form ]
Solid | [pka]
15.29±0.46(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
MS645 is a cell penetrant bivalent bromodomain (BRD) inhibitor th at inhibits the tandem BD1/BD2 of BRD4. It potently represses BRD4 transcriptional activity in solid-tumor cells including TNBC. MS645 potently inhibits IL-6 expression MDA-MB-231 cells. MS645 exhibits sustained blockade of BRD4 by inhibition of BRD4 interactions with transcription enhancer/mediator proteins MED1 and YY1. | [IC 50]
BRD4(BD1BD2): 18.4 nM (Ki) | [storage]
Store at -20°C | [References]
[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. DOI:10.1073/pnas.1720000115 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
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