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BMS-986158 is a highly effective BET inhibitor, demonstrating IC50 values of 6.6 nM in NCI-H211 small cell lung cancer (SCLC) cells and 5 nM in MDA-MB231 triple negative breast cancer (TNBC) cells.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $79 | In Stock | |
5 mg | $272 | In Stock | |
10 mg | $490 | In Stock | |
25 mg | $785 | In Stock | |
50 mg | $1,080 | In Stock | |
100 mg | $1,460 | In Stock | |
1 mL x 10 mM (in DMSO) | $297 | In Stock |
Description | BMS-986158 is a highly effective BET inhibitor, demonstrating IC50 values of 6.6 nM in NCI-H211 small cell lung cancer (SCLC) cells and 5 nM in MDA-MB231 triple negative breast cancer (TNBC) cells. |
Targets&IC50 | BET:6.6 nM(in NCI-H211 SCLC cells), BET:5 nM (in MDA-MB231 TNBC) cells) |
In vitro | BMS-986158 acts as an inhibitor targeting the bromodomain (BRD) and extra-terminal domain (BET) protein family, offering potential for cancer treatment. When administered, BMS-986158 attaches to the BRD's acetyl-lysine binding site on BET proteins, blocking their interaction with acetylated histones. This interruption hampers chromatin remodeling and curbs the expression of genes that promote growth, thereby inhibiting tumor cell proliferation[2]. |
Molecular Weight | 495.62 |
Formula | C30H33N5O2 |
Cas No. | 1800340-40-2 |
Smiles | Cc1nnn(C)c1-c1cnc2c(c1)n([C@@H](C1CCOCC1)c1ccccc1)c1cc(ccc21)C(C)(C)O |
Relative Density. | 1.28 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/ml (121.06 mM), Sonication is recommended. ![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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