ULK-101 is a potent and selective ULK1 inhibitor with in vitro IC50 of 8.3 nM. ULK-101 suppresses autophagy and sensitizes cancer cells to nutrient stress.
| Molecular Weight | 460.45 |
| Formula | C22H16F4N4OS |
| CAS Number | 2443816-45-1 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related ULK Products |
|---|
| DCC-3116
DCC-3116 is a first-in-class, potent and selective inhibitor of ULK1/2 kinases and autophagy. ULK1/2 are kinases that receive and process input from nutrient and stress sensors to initiate autophagy. |
| 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 treatment. |
| 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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