For research use only. Not for therapeutic Use.
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[1].
HTH-01-091 (1 μM) selectively inhibits 4% of the kinases over 90%[1].
HTH-01-091 (0-10 μM, 1 h) is cell permeable and causes MELK degradation[1].
HTH-01-091 (0-10 μM, 3 day) exhibits minor antiproliferative effects in breast cancer cells[1].
| Catalog Number | I028919 |
| CAS Number | 2000209-42-5 |
| Synonyms | 9-(3,5-dichloro-4-hydroxyphenyl)-1-[4-[(dimethylamino)methyl]cyclohexyl]-3,4-dihydropyrimido[5,4-c]quinolin-2-one |
| Molecular Formula | C26H28Cl2N4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H28Cl2N4O2/c1-31(2)14-15-3-6-19(7-4-15)32-24-18(13-30-26(32)34)12-29-23-8-5-16(9-20(23)24)17-10-21(27)25(33)22(28)11-17/h5,8-12,15,19,33H,3-4,6-7,13-14H2,1-2H3,(H,30,34) |
| InChIKey | FUVRHGKKWNNBJX-UHFFFAOYSA-N |
| SMILES | CN(C)CC1CCC(CC1)N2C3=C4C=C(C=CC4=NC=C3CNC2=O)C5=CC(=C(C(=C5)Cl)O)Cl |
| 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. |
