Product Description: 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].
Applications: Cancer-Kinase/protease
Formula: C23H25ClN2O2S
Citations: Cell Death Dis. 2019 Aug 5;10(8):583. /Cell. 2021 Jun 10;184(12):3143-3162.e32./Nature. 2022 Sep;609(7928):829-834./SSRN. 2022 Nov 21./Adv Sci (Weinh). 2024 Feb 2:e2308496./iScience. 2023 Jun 16./J Eur Acad Dermatol Venereol. 2023 Dec 22.
References: [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.
CAS Number: 1338545-07-5
Molecular Weight: 428.97
Compound Purity: 99.74
Research Area: Cancer
Solubility: DMSO : ≥ 83.33 mg/mL/H2O : 2 mg/mL (ultrasonic;warming;heat to 60°C)
Target: Apoptosis;CDK;TOPK
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