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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.
XST-14 (5 μM; for 24 h) induces apoptosis in HepG2 and human primary HCC cells. XST-14 (5 μM; for 12 h) inhibits the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1.
XST-14 (15, 30 mg/kg/day; IP; for 4 consecutive weeks) displays anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice.
| Molecular Weight | 291.34 |
| Formula | C16H21NO4 |
| CAS Number | 2607143-50-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 150 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 |
|---|
| 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. |
| 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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