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 K_d of 40 nM^[2].

OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation^[1].
OTS964 (10 nM; 48 hours) increases cancer cell death^[1].
OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

OTS964 (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression^[1].
OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

392.51

C₂₃H₂₄N₂O₂S

1338542-14-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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).  [Content Brief]

  [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.  [Content Brief]