MELK|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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MELK (Maternal embryonic leucine zipper kinase) belongs to the CAMK serine/threonine protein kinase superfamily. Melk is a protein serine/threonine kinase that is maximally active during mitosis. It is involved in diverse functions such as cell cycle, cytokinesis, mRNA splicing and apoptosis. Expression MELK is expressed in cells of various tissue origins. MELK expression is strongly dependant on cell-cycle: MELK is undetectable in cells which have exited cell cycle. The exact function of MELK is currently unknown, however MELK was shown to be involved in cell cycle progression via the protein phosphatase CDC25B phosphorylation, in cytokinesis, in apoptosis via its interaction with the Bcl-2 family of proapoptotic genes and apoptosis signal-regulating kinase (ASK1) and in inhibition of mRNA splicing during mitosis via its association with NIPP1. MELK function is required for mammary tumorigenesis in vivo.

Cat. No.	Product Name	CAS No.	Information
H6951	JNJ-47117096 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.
H6950	JNJ-47117096	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.
H6949	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.
H6948	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.
H6947	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.
H6946	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.
H6945	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.
H6954	OTS-167 hydrochloride	1431698-10-0	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.
H6953	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.
H6952	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.

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