HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research.
HTH-01-091 (1 μM) TFA selectively inhibits 4% of the kinases over 90%[1]. HTH-01-091 (0-10 μM, 1 h) TFA is cell permeable and causes MELK degradation[1].HTH-01-091 (0-10 μM, 3 day) TFA exhibits minor antiproliferative effects in breast cancer cells[1].
References:
[1]. Huang HT, et al. MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife. 2017 Sep 19;6:e26693.