MS645 is a bivalent BET bromodomains (BrD) inhibitor with a K i 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.
Storage Temp
Store at -20°C,Argon charged
Shipped In
Ice chest + Ice pads
Product Description
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a K i 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
In Vitro
MS645 has cell growth inhibitory effects on noncancer cell lines of mouse macrophage RAW cells and nontumorigenic breast epithelial MCF10A with IC 50 s of 4.1 nM, 6.8 nM, 7.9 nM for triple-negative breast cancer (TNBC) cell lines HS5878T, BT549, and MCF 10A. ?\nMS645 (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
