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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 |
|---|
| SBI-0206965
SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 . |
| ULK-101
ULK-101 is a potent and selective ULK1 inhibitor with in vitro IC50 of 8.3 nM. |
| LYN-1604 dihydrochloride
LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC). |
| MRT68921 dihydrochloride
MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, 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. |
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