MK-0731

MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy[1][2].

Product Specifications

CAS Number

[845256-65-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Kinesin; Lipoxygenase

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mk-0731.html

Purity

99.85

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(N(C)[C@@H](CC1)[C@H](F)CN1C)N2[C@@](C3=CC=CC=C3)(CO)C=C(C4=CC(F)=CC=C4F)C2

Molecular Formula

C25H28F3N3O2

Molecular Weight

459.50

Precautions

H302, H315, H319, H335

References & Citations

[1]Christopher D Cox, et al. Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S) -4- (2,5-difluorophenyl) -n-[ (3R,4S) -3-fluoro-1-methylpiperidin-4-yl]-2- (hydroxymethyl) -N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer. J Med Chem. 2008 Jul 24;51 (14) :4239-52.|[2]Kyle Holen, et al. A phase I trial of MK-0731, a kinesin spindle protein (KSP) inhibitor, in patients with solid tumors. Invest New Drugs. 2012 Jun;30 (3) :1088-95.