| Bioactivity | MLKL-IN-4 (compound 56) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-4 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 82 nM[1]. |
| Invitro | MLKL-IN-4 (compound 56) (10 μM) slightly inhibits RIPK1, does not affect the phosphorylation status of RIPK1 and MLKL[1].MLKL-IN-4 (1 μM, 24 h) inhibits the translocation of MLKL to cell membranes in HT-29 cells[1]. |
| In Vivo | MLKL-IN-4 (compound 56) shows T1/2 over 48 h and more than 150-fold lower reaction rates with glutathione (GSH), which potentially decreased their off-target effects and cell toxicity[1]. |
| Name | MLKL-IN-4 |
| Formula | C30H27ClN4O5 |
| Molar Mass | 559.01 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Cui B, et al. Discovery of a New Class of Uracil Derivatives as Potential Mixed Lineage Kinase Domain-like Protein (MLKL) Inhibitors. J Med Chem. 2022 Oct 13;65(19):12747-12780. |