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XMD16-5 is found to be potent in the inhibition of TNK2 phosphorylation. XMD8-87 and XMD16-5 potently inhibit phosphorylation of TNK2 truncation mutations found in solid tumor types.
| Cell Experiment | |
|---|---|
| Cell lines | 293T cells |
| Preparation method | 293T cells expressing TNK2 are plated in 6-well format at a density of 250,000 cells per well 48 hours prior to treatment. Cells are then treated with a 100 μL of XMD8-87 or XMD16-5 at 5 μmol/L and with 9 1:1 serial dilutions down to ≈10 nmol/L. Two additional samples are treated with DMSO only. Cells are then incubated for 6 hours at 37°C. Protein extraction is accomplished by adding 300 μL of lysis buffer to cells after removing media. Plates are gently shaken for 5 minutes at room temperature. Lysates are collected and cleared of incompletely solubilized material by spinning for 10 minutes at maximum speed in a microcentrifuge. Samples are prepared for SDS-PAGE using the EPage loading buffer. |
| Concentrations | 10 nM-5 μM |
| Incubation time | 6 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 416.48 |
| Formula | C23H24N6O2 |
| CAS Number | 1345098-78-3 |
| Form | Solid |
| Solubility (25°C) | 83 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Tyrosinase Products |
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Deoxyarbutin can effectively inhibit tyrosinase activity and melanin synthesis, and obtain significant and lasting whitening effect, with strong antioxidant effect. |
| α-Methyl-p-tyrosine
α-Methyl-p-tyrosine (AMPT) is a competitive inhibitor of tyrosine hydroxylase, which converts tyrosine into DOPA. α-Methyl-p-tyrosine is also an orally active inhibitor of catecholamine synthesis, inhibiting the hydroxylation of tyrosine into DOPA. |
| Trifolirhizin
Trifolirhizin is a pterocarpan flavonoid isolated from the root of Sophora flavescoreae. Trifolirhizin showed high tyrosinase inhibitory activity with IC50 of 506 μM. Trifolirhizin has potential anti-inflammatory and anticancer activities. |
| XMD8-87
XMD8-87 is a novel tyrosine kinase nonreceptor 2(TNK2) inhibitor with IC50s of 38 nmol/L and 113 nmol/L for the D163E and R806Q mutations. |
| Dihydromorin
trans-Dihydromorin is an effective hypopigmenting agent in normal skin cells, hypopigmenting agents effective in melanoma system may not be effective on normal melanocytes, indicating that a non-tumor melanocyte system is more suitable for the screening of hypopigmenting agents. |
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