OTS964 (hydrochloride)

OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM[1]. OTS964 hydrochloride 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

[1338545-07-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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/OTS-964.html

Purity

99.74

Solubility

DMSO : ≥ 83.33 mg/mL|H2O : 2 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

OC1=CC(C)=C2C(C3=C(SC=C3)C(N2)=O)=C1C4=CC=C([C@@H](C)CN(C)C)C=C4.Cl

Molecular Formula

C23H25ClN2O2S

Molecular Weight

428.97

Precautions

H302, H315, H319, H335

References & Citations

[1]Matsuo Y, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition ofcytokinesis. 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.