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LYN-1604 is a novel activator of ULK1, inducing cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. LYN-1604 has an IC50 of 1.66 μM against MDA-MB-231 cells, and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-231 cells |
| Preparation method | Cells are dispensed in 96-well plates at a density of 5 × 104 cells per mL. After 24 h of incubation, cells are treated with different concentrations of compounds for the indicated time periods. Cell viability is measured by the MTT assay. |
| Concentrations | 0.5, 1.0 and 2.0 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | MDA-MB-231 xenograft model (BALB/c nude mice) |
| Formulation | - |
| Dosages | 25 mg/kg, 50 mg/kg, 100 mg/kg |
| Administration | intragastric administration |
| Molecular Weight | 657.54 |
| Formula | C33H45Cl4N3O2 |
| CAS Number | 2088939-99-3 |
| Solubility (25°C) | Water 90 mg/mL DMSO 45 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. |
| DCC-3116
DCC-3116 is an orally active ULK1/2 inhibitor. |
| 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. |
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