1. Epigenetics
  2. Epigenetic Reader Domain
  3. BMS-986158

BMS-986158 

Cat. No.: HY-101567 Purity: 98.22%
Handling Instructions

BMS-986158 est un inhibiteur puissant de BET avec des IC50s de 6,6 et 5 nM dans les cellules NCI-H211 à petites cellules du cancer du poumon à cellules (SCLC) et les cellules MDA-MB231 triple négatif du cancer du sein (TNBC), respectivement.

BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.

For research use only. We do not sell to patients.

BMS-986158 Chemical Structure

BMS-986158 Chemical Structure

CAS No. : 1800340-40-2

Size Price Stock Quantity
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 900 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3960 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively[1].

IC50 & Target

IC50: 6.6 nM (BET, in NCI-H211 SCLC cells), 5 nM (in MDA-MB231 TNBC) cells)[1]

In Vitro

BMS-986158 is an inhibitor of the bromodomain (BRD) and extra-terminal domain (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor BMS-986158 binds to the acetyl-lysine binding site in the BRD of BET proteins, thereby preventing the interaction between BET proteins and acetylated histones. This disrupts chromatin remodeling and prevents the expression of certain growth-promoting genes, resulting in an inhibition of tumor cell growth[2].

Clinical Trial
Molecular Weight

495.62

Formula

C₃₀H₃₃N₅O₂

CAS No.

1800340-40-2

SMILES

OC(C)(C)C1=CC=C2C(N([[email protected]](C3=CC=CC=C3)C4CCOCC4)C5=C2N=CC(C6=C(C)N=NN6C)=C5)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 1 mg/mL (2.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0177 mL 10.0884 mL 20.1767 mL
5 mM --- --- ---
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

BMS-986158BMS986158BMS 986158Epigenetic Reader DomainInhibitorinhibitorinhibit

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BMS-986158
Cat. No.:
HY-101567
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