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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $296 | In Stock | In Stock | |
| 5 mg | $728 | In Stock | In Stock | |
| 10 mg | $987 | In Stock | In Stock | |
| 25 mg | $1,530 | In Stock | In Stock | |
| 50 mg | $1,980 | In Stock | In Stock | |
| 100 mg | $2,500 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $816 | In Stock | 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. | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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