ATX968

ATX968 (example 31) is an orally active, potent and selective inhibitor of ATP-dependent RNA helicase A (DHX9), with the EC50 of 0.054 μM in circBRIP1. ATX968 results in robust and durable tumor growth inhibition or regression in mouse xenograft studies with MSI-H/dMMR colorectal cancer cell lines[1][2][3].

Product Specifications

CAS Number

[2973395-71-8]

Product Name Alternative

DHX9-IN-2

UNSPSC

12352005

Target

DNA/RNA Synthesis

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/dhx9-in-2.html

Concentration

10mM

Purity

99.61

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

ClC1=CC(NC(C2=CC(C3=NC=CC=C3C)=CS2)=O)=CC(NS(C)(=O)=O)=C1

Molecular Formula

C18H16ClN3O3S2

Molecular Weight

421.92

References & Citations

[1]DANIELS Matthew H., et al. Preparation of imidazopyridines, thienopyrimidines, pyrrolopyrimidines and related heterocycles as inhibitors of RNA helicase DHX9 useful in treatment of cancers. World Intellectual Property Organization, WO2023154519 A1 2023-08-17|[2]Castro J, et al. A Potent, Selective, Small-Molecule Inhibitor of DHX9 Abrogates Proliferation of Microsatellite Instable Cancers with Deficient Mismatch Repair. Cancer Res. 2025 Feb 17;85 (4) :758-776.|[3]Castro J B, et al. DHX9 inhibition as a novel therapeutic for cancer with loss-of-function mutations in DNA damage repair genes BRCA1 and BRCA2[J]. Cancer Research, 2024, 84 (6_Supplement) : 3908-3908.