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DCC-3116 is a first-in-class, potent and selective orally inhibitor of ULK1/2 kinases and autophagy. ULK1/2 are kinases that receive and process input from nutrient and stress sensors to initiate autophagy. Inhibition of the MAPK pathway releases tonic inhibition of ULK1/2 and triggers autophagy as a survival mechanism, suggesting that ULK1/2 may provide a promising therapeutic target. DCC-3116 showed preclinical antitumor activity in combination with the MAPK kinase inhibitor trametinib.
| Molecular Weight | 535.6 |
| Formula | C26H36F3N7O2 |
| CAS Number | 2543673-19-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ULK Products |
|---|
| XST-14
XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 has antitumor effects. |
| MRT68921
MRT68921 is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. |
| SBP-7455
SBP-7455 is a dual-Specific ULK1/2 autophagy inhibitor with IC50s of 13 nM and 476 nM for ULK1 and ULK2 in ADP-Glo assay, respectively. |
| BL-918
BL-918 is a potent, orally active activator of UNC-51-like kinase 1 (ULK1) with EC50 of 24.14 nM and Kd of 0.719 μM. BL-918 induces cytoprotective autophagy for Parkinson's disease. |
| MRT68921 dihydrochloride
MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. |
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