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HTH-01-091

Chemical Structure : HTH-01-091

CAS No.: 2000209-42-5

HTH-01-091 (MELK inhibitor)

Catalog No.: PC-61763Not For Human Use, Lab Use Only.

HTH-01-091 is a potent and selective, cell-permeable, ATP-competitive MELK inhibitor with biochemical IC50 of 10.5 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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

Physicochemical Properties

M.Wt 499.436
Formula C26H28Cl2N4O2
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

9-(3,5-dichloro-4-hydroxyphenyl)-1-((1r,4r)-4-((dimethylamino)methyl)cyclohexyl)-3,4-dihydropyrimido[5,4-c]quinolin-2(1H)-one

References

1. Huang HT, et al. Elife. 2017 Sep 19;6. pii: e26693.

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