OTS964

OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM[1]. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM[2].

Product Specifications

CAS Number

[1338542-14-5]

UNSPSC

12352005

Target

Apoptosis; CDK; TOPK

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ots964.html

Solubility

10 mM in DMSO

Smiles

O=C(N1)C2=C(C=CS2)C3=C1C(C)=CC(O)=C3C4=CC=C([C@@H](C)CN(C)C)C=C4

Molecular Formula

C23H24N2O2S

Molecular Weight

392.51

References & Citations

[1]Matsuo Y , et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancerthrough inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6 (259) :259ra145.|[2]Lin A, et al. Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials. Sci Transl Med. 2019 Sep 11;11 (509) .|[3]Lu H, et al. TOPK inhibits autophagy by phosphorylating ULK1 and promotes glioma resistance to TMZ. Cell Death Dis. 2019 Aug 5;10 (8) :583.