BMS-986158

SKU: orb1308546

Description

BMS-986158 is a potent and selective BET bromodomain inhibitor, exhibiting low nanomolar IC50 values in cellular assays, including 6.6 nM in NCI-H211 SCLC and 5 nM in MDA-MB-231 TNBC cells. It is a valuable chemical probe for oncology research, utilized in both in vitro and in vivo studies to investigate epigenetic mechanisms in cancer.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1800340-40-2
• MW: 495.62
• Purity: 99.45% (May vary between batches)
• Formula: C₃₀H₃₃N₅O₂
• SMILES: Cc1nnn(C)c1-c1cnc2c(c1)n([C@@H](C1CCOCC1)c1ccccc1)c1cc(ccc21)C(C)(C)O
• Target: Epigenetic Reader Domain
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.04 mM);DMSO:60 mg/mL (121.06 mM)

Bioactivity

• Target IC50:
  BET:5 nM (in MDA-MB231 TNBC) cells)|BET:6.6 nM(in NCI-H211 SCLC 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BET, BMS 986158, BMS986158, BMS-986158, Inhibitor, EpigeneticReaderDomain, Epigenetic Reader Domain, inhibit

Compound Identifiers

PubChem CID

118196485