OTSSP167 (hydrochloride)

OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC50 value of 0.41 nM.

Product Specifications

CAS Number

[1431698-10-0]

Product Name Alternative

OTS167 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

MELK

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/OTSSP167-hydrochloride.html

Purity

99.78

Solubility

DMSO : 33.33 mg/mL (ultrasonic) |H2O : 7.14 mg/mL (ultrasonic)

Smiles

ClC1=CC(C2=CC=C(N=CC(C(C)=O)=C3N[C@H]4CC[C@H](CN(C)C)CC4)C3=N2)=CC(Cl)=C1O.[H]Cl

Molecular Formula

C25H29Cl3N4O2

Molecular Weight

523.88

Precautions

H302, H315, H319

References & Citations

[1]Chung S, Suzuki H, Miyamoto T, et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget. 2012 Dec 21.|[2]Ji W, et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases. PLoS One. 2016 Apr 15;11 (4) :e0153518.|[3]Cho YS, et al. The crystal structure of MPK38 in complex with OTSSP167, an orally administrative MELK selective inhibitor. Biochem Biophys Res Commun. 2014 Apr 25;447 (1) :7-11.|[4]Jurmeister S, et al. Identification of potential therapeutic targets in prostate cancer through a cross-species approach. EMBO Mol Med. 2018 Feb 5. pii: e8274.|[5]Meel MH, et al. MELK inhibition in Diffuse Intrinsic Pontine Glioma. Clin Cancer Res. 2018 Jul 30. pii: clincanres.0924.2018.