SMARCA2-IN-6

SMARCA2-IN-6 is a SMARCA2 (also known as BRM) inhibitor, with IC50s less than 5 nM for SMARCA2 and SMARCA4. SMARCA2-IN-6 inhibits KRT80 gene expression in H1299 cells (IC50: 26 nM) . SMARCA2-IN-6 inhibits proliferation in BRG1-mutant SKMEL5 cells (IC50: 13 nM) [1].

Product Specifications

CAS Number

[2270875-79-9]

UNSPSC

12352005

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/smarca2-in-6.html

Smiles

O=C(NC1=CC(C(F)F)=NS1)NC2=CC(Cl)=NC=C2N

Molecular Formula

C10H8ClF2N5OS

Molecular Weight

319.72

References & Citations

[1]Papillon JPN, et al. Discovery of Orally Active Inhibitors of Brahma Homolog (BRM) /SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1) /SMARCA4-Mutant Cancers. J Med Chem. 2018 Nov 21;61 (22) :10155-10172.