HTH-01-091

CAS No. 2000209-42-5

HTH-01-091( HTH-01-091 | HTH 01-091 | HTH01-091 )

Catalog No. M13123 CAS No. 2000209-42-5

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

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    HTH-01-091
  • Note
    Research use only, not for human use.
  • Brief Description
    HTH-01-091 is a potent and selective, cell-permeable, ATP-competitive MELK inhibitor with biochemical IC50 of 10.5 nM.
  • Description
    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.
  • In Vitro
    HTH-01-091 (1 μM) selectively inhibits 4% of the kinases over 90%. HTH-01-091 (0-10 μM, 1 h) is cell permeable and causes MELK degradation.HTH-01-091 (0-10 μM, 3 day) exhibits minor antiproliferative effects in breast cancer cells. Western Blot Analysis Cell Line:MDA-MB-468 cells Concentration:0, 0.1, 1.0, and 10 μM Incubation Time:1 h Result:Reduced MELK protein levels in MDA-MB-468 cells; Dose-dependently decreased MELK pull-down by streptavidin beads, demonstrating that the compound is cell permeable and binds to MELK in an ATP-competitive fashion. Had no effect on ERK1/2 pull-down, showing no binding affinity of HTH-01-091 to ERK1/2. Cell Proliferation Assay Cell Line:MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells Concentration:0, 0.001, 0.01, 0.1, 1.0, and 10 μM Incubation Time:3 day Result:Showed antiproliferative activities in a panel of breast cancer cell lines, including MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells, with IC50 values of 4.00 μM, 6.16 μM, 8.80 μM, >10 μM, 8.75 μM, and 3.87 μM, respectively.
  • In Vivo
    ——
  • Synonyms
    HTH-01-091 | HTH 01-091 | HTH01-091
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    MELK
  • Recptor
    MELK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2000209-42-5
  • Formula Weight
    499.436
  • Molecular Formula
    C26H28Cl2N4O2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C1N([C@H]2CC[C@H](CN(C)C)CC2)C3=C(CN1)C=NC4=CC=C(C5=CC(Cl)=C(O)C(Cl)=C5)C=C34
  • Chemical Name
    9-(3,5-dichloro-4-hydroxyphenyl)-1-((1r,4r)-4-((dimethylamino)methyl)cyclohexyl)-3,4-dihydropyrimido[5,4-c]quinolin-2(1H)-one

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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