ATX968

ATX968 is an inhibitor of DEAD-box helicase 9 (DDX9. IC50 = 8 nM for helicase activity). It is selective for DDX9 over DDX36, Brahma homolog (BRM), also known as SMARCA2, and Werner syndrome protein (WRN. IC50s = >10, >10, and >100 µM, respectively), as well as a panel of 96 kinases at 10 µM but does inhibit dual-specificity tyrosine phosphorylation-regulated kinase 1B (DYRK1B). ATX968 (1 µM) selectively induces unresolved nuclear R-loop accumulation in microsatellite instable-high with deficient mismatch repair (MSI-H/dMMR) LS411N colorectal carcinoma cells over microsatellite-stable with proficient mismatch repair (MSS/pMMR) NCI H747 colorectal carcinoma cells. It induces tumor regression in an LS411N mouse xenograft model when administered at a dose of 300 mg/kg. Formal Name: N-[3-chloro-5-[(methylsulfonyl)amino]phenyl]-4-(3-methyl-2-pyridinyl)-2-thiophenecarboxamide. CAS Number: 2973395-71-8. Synonyms: DHX9-IN-2 DHX9 Inhibitor 2. Molecular Formula: C18H16ClN3O3S2. Formula Weight: 421.9. Purity: >98%. Formulation (Request formulation change): A solid. Solubility: DMSO: Soluble: > 10 mg/ml. SMILES: CC1=C(C2=CSC(C(NC3=CC(Cl)=CC(NS(C)(=O)=O)=C3)=O)=C2)N=CC=C1. InChi Code: InChI=1S/C18H16ClN3O3S2/c1-11-4-3-5-20-17(11)12-6-16(26-10-12)18(23)21-14-7-13(19)8-15(9-14)22-27(2,24)25/h3-10,22H,1-2H3,(H,21,23). InChi Key: VDGNPEFFHQRGOP-UHFFFAOYSA-N. Storage: -20°C. Stability: > 4 years.