OTS167 | MELK inhibitor | Probechem Biochemicals

Chemical Structure : OTS167

CAS No.: 1431697-89-0

OTS167 (OTSSP167, OTS-167)

Catalog No.: PC-44480Not For Human Use, Lab Use Only.

OTSSP167 (OTS167) is a highly potent, selective and orally active MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.

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5 mg	$88	In stock
10 mg	$128	In stock
25 mg	$218	In stock
50 mg	$358	In stock
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Biological Activity

OTSSP167 (OTS167) is a highly potent, selective and orally active MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.

OTSSP167 demonsrates in vitro anti-proliferative against MELK-highly expressed A549 (lung), T47D (breast), DU4475 (breast), and 22Rv1 (prostate) cancer cells with IC50 of 6.7, 4.3, 2.3, and 6.0 nM, respectively, with significant lower activity against HT1197 (bladder, low-MELK expression) cancer cells (IC50=97 nM).

OTSSP167 shows the effectiveness on the growth of various human cancer xenograft.

OTSSP167 inhibits the phosphorylation of novel MELK substrates, significantly suppresses the phosphorylation levels of DBNL and PSMA1 in breast cancer cell lines.

Physicochemical Properties

M.Wt	487.4214
Formula	C25H28Cl2N4O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(6-(3,5-dichloro-4-hydroxyphenyl)-4-(((1r,4r)-4-((dimethylamino)methyl)cyclohexyl)amino)-1,5-naphthyridin-3-yl)ethanone

References

1. Chung S, et al. Oncotarget. 2012 Dec;3(12):1629-40.

2. Alachkar H, et al. Oncotarget. 2014 Dec 15;5(23):12371-82.

3. Stefka AT, et al. Blood Cancer J. 2016 Aug 19;6(8):e460.

OTS167 (OTSSP167, OTS-167)

Biological Activity

Physicochemical Properties

References

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