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HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $296 | In Stock | |
| 5 mg | $728 | In Stock | |
| 10 mg | $987 | In Stock | |
| 25 mg | $1,530 | In Stock | |
| 50 mg | $1,980 | In Stock | |
| 100 mg | $2,500 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $816 | In Stock |
| Description | HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer. |
| Targets&IC50 | DYRK4:41.8 nM, mTOR:632 nM, Pim1:60.6 nM, CDK7:1230 nM |
| In vitro | HTH-01-091 (0-10 μM, 1 h) 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 causes MELK degradation.[1] HTH-01-091 (1 μM) selectively inhibits 4% of the kinases over 90%[1]. HTH-01-091 (0-10 μM, 3 days) exhibits minor antiproliferative effects in breast cancer cells[1]. |
| Synonyms | HTH01-091, HTH-01091, HTH 01-091, HTH 01091 |
| Molecular Weight | 499.43 |
| Formula | C26H28Cl2N4O2 |
| Cas No. | 2000209-42-5 |
| Smiles | O=C1N(C2=C3C(=NC=C2CN1)C=CC(=C3)C4=CC(Cl)=C(O)C(Cl)=C4)[C@@H]5CC[C@@H](CN(C)C)CC5 |
| Relative Density. | 1.327 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 5 mg/mL (10.01 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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