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BMS-986158

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Catalog No. T14685Cas No. 1800340-40-2

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.

BMS-986158

BMS-986158

🥰Excellent
Purity: 98.77%
Catalog No. T14685Cas No. 1800340-40-2
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 SizePriceAvailabilityQuantity
1 mg$79In Stock
5 mg$272In Stock
10 mg$490In Stock
25 mg$785In Stock
50 mg$1,080In Stock
100 mg$1,460In Stock
1 mL x 10 mM (in DMSO)$297In Stock
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Purity:98.77%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight495.62
FormulaC30H33N5O2
Cas No.1800340-40-2
SmilesCc1nnn(C)c1-c1cnc2c(c1)n([C@@H](C1CCOCC1)c1ccccc1)c1cc(ccc21)C(C)(C)O
Relative Density.1.28 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.0177 mL10.0884 mL20.1767 mL100.8837 mL
5 mM0.4035 mL2.0177 mL4.0353 mL20.1767 mL
10 mM0.2018 mL1.0088 mL2.0177 mL10.0884 mL
20 mM0.1009 mL0.5044 mL1.0088 mL5.0442 mL
50 mM0.0404 mL0.2018 mL0.4035 mL2.0177 mL
100 mM0.0202 mL0.1009 mL0.2018 mL1.0088 mL

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