| Bioactivity | 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[1]. | ||||||||||||
| Target | IC50: 10.5 nM (MELK), 41.8 nM (DYRK3), 42.5 nM (RIPK2), 60.6 nM (PIM1), 108.6 nM (smMLCK), 632 nM (mTOR), 962 nM (PIK3CA), 1230 nM (CDK7), 1740 nM (GSK3A) | ||||||||||||
| Invitro | HTH-01-091 (1 μM) TFA 选择性抑制 4% 的激酶超过 90%[1]。 HTH-01-091 (0-10 μM, 1 h) TFA 具有细胞渗透性并导致 MELK 降解[1]。 HTH-01-091（0-10 μM，3 天）TFA 在乳腺癌细胞中表现出轻微的抗增殖作用[1]。 Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| Name | HTH-01-091 TFA | ||||||||||||
| Formula | C28H29Cl2F3N4O4 | ||||||||||||
| Molar Mass | 613.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Huang HT, et al. MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife. 2017 Sep 19;6:e26693. |