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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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

CDK11

Citation 01

BioRxiv. 2025 Nov 20.|bioRxiv. 2025 Sep 28.|Cell Death Dis. 2019 Aug 5;10 (8) :583. |Cell. 2021 Jun 10;184 (12) :3143-3162.e32.|Mol Cell Proteomics. 2025 May 12:100991.|Mol Cell. 2025 Sep 4;85 (17) :3256-3274.e14.|Nature. 2022 Sep;609 (7928) :829-834.|SSRN. 2022 Nov 21.|Adv Sci (Weinh) . 2024 Apr;11 (14) :e2308496.|iScience. 2023 Jun 20;26 (7) :107185.|J Eur Acad Dermatol Venereol. 2024 May;38 (5) :851-863.

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