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Cat. No. Product Name CAS No. Information
PC-42114

NVP-MELK8a hydrochloride

2096992-20-8

NVP-MELK8a hydrochloride (MELK8a hydrochloride) is a novel potent, and selective MELK inhibitor with IC50 of 2 nM; exhibits high selectivity with only 7 off-target kinases inhibited >85% against 456 kinases at 1 uM, Flt3 (IC50=0.18 uM), Haspin (IC50=0.19 uM), PDGFRα (IC50=0.42 uM); exhibits growth inhibition of MDA-MD-468 cells with IC50 of 0.11 uM, and increases cells harboring 4N DNA content.

PC-44480

OTS-167

1431697-89-0

OTS-167 (OTSSP-167) is a highly potent and selective MELK inhibitor with IC50 of 0.41 nM; shows anti-proliferative activity for A549, T47D, DU4475, and 22Rv1 cancer cells with IC50 of 6.7, 4.3, 2.3, and 6.0 nM, respectively; inhibits the phosphorylation of PSMA1 and DBNL, two novel MELK substrates and are important for stem-cell characteristics and invasiveness; shows robust tumor growth inhibition (TGI) in xenograft models; orally active.

Blood Cancer

Phase 2 Clinical

PC-35237

MELK inhibitor 17

2095596-44-2 MELK inhibitor 17 is a potent, selective MELK inhibitor with Ki/IC50 of 0.39/3 nM, >100-fold selectivity over CHK1, CAMKK2, NUAK1 and ERK2; inhibits the expression of the anti-apoptotic protein Mcl-1 and proliferation of TNBC cells exhibiting selectivity for cells expressing high levels of MELK.
PC-61764

JW-7-25-1

1222998-57-3 JW-7-25-1 is a potent MELK inhibitor with biochemical IC50 of 5.0 nM, also inhibits PIK3CA, mTOR, GSK3A and CDK7 with CI50 of 5-60 nM; exhibits a broad kinase selectivity profile with an S(35) score of 0.54 at 10 uM.
PC-61763

HTH-01-091

2000209-42-5 HTH-01-091 is a potent and selective, cell-permeable, ATP-competitive MELK inhibitor with biochemical IC50 of 10.5 nM; displays no significant activity for PIK3CA, mTOR, GSK3A and CDK7 (IC50>600 nM); exhibits substantially improved kinome selectivity in comparison with OTSSP167; induces MELK degradation, but demonstrates poor antiproliferative effects in basal-like breast cancer cell lines.
PC-61630

KIN-281

74151-26-1 KIN-281 is a small molecule that inhibits multiple kinases including MELK and the non-receptor tyrosine kinase BMX with IC50 of 1.4 and 1.9 uM, respectively; also inhibits BLK, CAMK Iiγ/δ, CAMK Iα, Tie2, BTK with IC50 of 1-10 uM; inhibit STAT3 activation, autophagy and cancer cell anchorage-independent growth in MDA-MB-231 and MDA-MB-468 breast cancer cells.
PC-70141

Kinase inhibitor C1

133712-17-1 A potent small molecule inhibitor of MELK kinase activity with IC50 of 42 nM; causes mitotic arrest and subsequent cellular apoptosis in vitro; strongly induces tumor cell apoptosis in slice cultures of GBM surgical specimens and attenuates growth of mouse intracranial tumors derived from GSCs; also inhibits Aurora A/B/C (IC50=61/31/124 nM), and Chk1 (IC50=262 nM); a multi-kinase inhibitor.

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