HTH-01-091 TFA
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 613.46 |
| Molecular Formula | C28H29Cl2F3N4O4 |
| SMILES | O=C1N([C@H]2CC[C@H](CN(C)C)CC2)C3=C(CN1)C=NC4=CC=C(C5=CC(Cl)=C(O)C(Cl)=C5)C=C34.OC(C(F)(F)F)=O |
Summary
IC50 & 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) [1]
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| Cell Line: | MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells |
| Concentration: | 0, 0.001, 0.01, 0.1, 1.0, and 10 μM |
| Incubation Time: | 3 day |
| Result: | Showed antiproliferative activities in a panel of breast cancer cell lines, including MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells, with IC 50 values of 4.00 μM, 6.16 μM, 8.80 μM, >10 μM, 8.75 μM, and 3.87 μM, respectively. |
Western Blot Analysis [1]
| Cell Line: | MDA-MB-468 cells |
| Concentration: | 0, 0.1, 1.0, and 10 μM |
| Incubation Time: | 1 h |
| Result: | Reduced MELK protein levels in MDA-MB-468 cells; 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. Had no effect on ERK1/2 pull-down, showing no binding affinity of HTH-01-091 to ERK1/2. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
