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Cat. No. Product Name CAS No. Information
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.
PC-70140

MELK-T1

1610586-62-3 A novel, cell-permeable, potent and selective inhibitor of MELK kinase domain with IC50 of 37 nM; shows >50% inhibition at 1 uM against 6 kianses in a panel of 235 kinases (Flt3 IC50=18 nM); triggers a rapid and proteasome-dependent degradation of the MELK protein, induces the accumulation of stalled replication forks and DSBs in MCF-7 cells; induces a strong phosphorylation of p53, a prolonged up-regulation of p21 and a down-regulation of FOXM1 target genes.
PC-70139

MELK-T1 hydrochloride

1610536-69-0 A novel, cell-permeable, potent and selective inhibitor of MELK kinase domain with IC50 of 37 nM; shows >50% inhibition at 1 uM against 6 kianses in a panel of 235 kinases (Flt3 IC50=18 nM); triggers a rapid and proteasome-dependent degradation of the MELK protein, induces the accumulation of stalled replication forks and DSBs in MCF-7 cells; induces a strong phosphorylation of p53, a prolonged up-regulation of p21 and a down-regulation of FOXM1 target genes.

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