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You are here:Home-Inhibitors & Agonists-PI3K/Akt/mTOR Pathway-MELK

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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
GY02561

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.

GY01977

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.

GY01436

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.

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