OTS964 hydrochloride

• CAT Number: I001293
• CAS Number: 1338545-07-5
• Molecular Formula: C23H25ClN2O2S
• Molecular Weight: 392.51
• Purity: 98%
• Synonyms: (R)-9-[4-[1-(Dimethylamino)propan-2-yl]phenyl]-8-hydroxy-6-methylthieno[2,3-c]quinolin-4(5H)-one Hydrochloride; OTS964 hydrochloride; OTS-964 hydrochloride; OTS964 HCl
• Target: TOPK
• Solubility: 10 mM in DMSO
• Appearance: Powder
• Storage: Store at -20°C
• IC50: 28 nM
• IUPAC Name: 9-[4-[(2R)-1-(dimethylamino)propan-2-yl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one;hydrochloride
• InChI: InChI=1S/C23H24N2O2S.ClH/c1-13-11-18(26)19(16-7-5-15(6-8-16)14(2)12-25(3)4)20-17-9-10-28-22(17)23(27)24-21(13)20;/h5-11,14,26H,12H2,1-4H3,(H,24,27);1H/t14-;/m0./s1
• InChIKey: YHPWOYBWUWSJDW-UQKRIMTDSA-N
• SMILES: CC1=CC(=C(C2=C1NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)[C@@H](C)CN(C)C)O.Cl

OTS964 hydrochloride（Cat No.:I001293）is a selective inhibitor of the cyclin-dependent kinase 1 (CDK1), an enzyme critical for cell cycle regulation and mitosis. By inhibiting CDK1, OTS964 induces cell cycle arrest and promotes apoptosis in cancer cells, particularly in those with high proliferative rates. This compound has demonstrated efficacy in preclinical studies against various cancers, including solid tumors and hematological malignancies. OTS964 is of interest in cancer research as it helps to elucidate the role of CDK1 in tumor growth and offers potential therapeutic benefits in targeted cancer therapies.

Reference

1. Oncotarget. 2017 Dec 9;9(3):3043-3059. doi: 10.18632/oncotarget.23077. eCollection 2018 Jan 9.
Targeting the T-Lak cell originated protein kinase by OTS964 shrinks the size of power-law coded heterogeneous glioma stem cell populations.
Sugimori M(1), Hayakawa Y(2), Koh M(2), Hayashi T(2), Tamura R(1), Kuroda S(2).
Author information:
(1)Department of Integrative Neuroscience, University of Toyama, 2630 Sugitani, Toyama, Toyama 930-0194, Japan. (2)Department of Neurosurgery, University of Toyama, 2630 Sugitani, Toyama, Toyama 930-0194, Japan.
Glioblastoma resists chemoradiotherapy, then, recurs to be a fatal space-occupying lesion. The recurrence is caused by re-growing cell populations such as glioma stem cells (GSCs), suggesting that GSC populations should be targeted. This study addressed whether a novel anti-cancer drug, OTS964, an inhibitor for T-LAK cell originated protein kinase (TOPK), is effective in reducing the size of the heterogeneous GSC populations, a power-law coded heterogeneous GSC populations consisting of glioma sphere (GS) clones, by detailing quantitative growth properties. We found that OTS964 killed GS clones while suppressing the growth of surviving GS clones, thus identifying clone-eliminating and growth-disturbing efficacies of OTS964. The efficacies led to a significant size reduction in GS populations in a dose-dependent manner. The surviving GS clones reconstructed GS populations in the following generations; the recovery of GS populations fits a recurrence after the chemotherapy. The recovering GS clones resisted the clone-eliminating effect of OTS964 in sequential exposure during the growth recovery. However, surprisingly, the resistant properties of the recovered-GS clones had been plastically canceled during self-renewal, and then the GS clones had become re-sensitive to OTS964. Thus, OTS964 targets GSCs to eliminate them or suppress their growth, resulting in shrinkage of the power-law coded GSC populations. We propose a therapy focusing on long-term control in recurrence of glioblastoma via reducing the size of the GSC populations by OTS964.