BET bromodomain inhibitor 1

BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2 (2), BRD3 (2), BRD4 (1), BRD4 (2), and BRDT (2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively) . bromodomain inhibitor 1 has anti-cancer activity[1].

Product Specifications

CAS Number

[2411226-02-1]

UNSPSC

12352005

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bet-bromodomain-inhibitor-1.html

Purity

99.91

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1C2=C(C)C=C(C3=CC(CS(=O)(CC)=O)=CN=C3OC4=CC=C(F)C=C4F)N2C=CN1

Molecular Formula

C22H19F2N3O4S

Molecular Weight

459.47

References & Citations

[1]Zizhou Li, et al. Discovery of 8-Methyl-pyrrolo[1,2- a]pyrazin-1 (2 H) -one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors. J Med Chem. 2020 Apr 23;63 (8) :3956-3975.