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HTH-01-091 

Cat. No. M29094
HTH-01-091  Structure
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Quality Control & Documentation
Biological Activity

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research.

Chemical Information
Molecular Weight 499.43
Formula C26H28Cl2N4O2
CAS Number 2000209-42-5
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ian M McDonald, et al. J Biol Chem. Mass spectrometry-based selectivity profiling identifies a highly selective inhibitor of the kinase MELK that delays mitotic entry in cancer cells

[2] Hai-Tsang Huang, et al. Elife. MELK is not necessary for the proliferation of basal-like breast cancer cells

Related MELK Products
HTH-01-091 TFA

HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM.

MELK-IN-1 

MELK-IN-1 is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK) with an IC50 and a Ki of 3 nM and 0.39 nM, respectively.

JNJ-47117096 hydrochloride

JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.

MELK-8a hydrochloride

MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM.

OTSSP167 hydrochloride

OTSSP167 hydrochloride is a highly potent, selective MELK inhibitor with IC50 of 0.41 nM.

  Catalog
Abmole Inhibitor Catalog




Keywords: HTH-01-091  supplier, MELK, inhibitors, activators


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