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SBI-0206965 has very high selectivity, only inhibits 10 out of 456 kinases >95% when tested at 10 μM. SBI-0206965 suppressed ULK1-mediated phosphorylation events in cells, regulating autophagy and cell survival It can suppress autophagy induced by mTOR inhibition, prevent ULK1-dependent cell survival following nutrient deprivation. It greatly synergized with mechanistic target of rapamycin (mTOR) inhibitors to kill tumor cells, providing a strong rationale for their combined use in the clinic.
BMC Cancer. 2020 Aug.
Blockage of AMPK-ULK1 pathway mediated autophagy promotes cell apoptosis to increase doxorubicin sensitivity in breast cancer (BC) cells: an in vitro study
SBI-0206965 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | HEK-293T |
| Preparation method | Human embryonic kidney cells (HEK-293T) were transfected with wild-type (WT) or kinase inactive (KI) Myc-tagged ULK1 and wild-type Flag-tagged Vps34 (WT Vps34). 24 hours post-transfection, cells were treated with a panel of putative ULK1 competitive inhibitors in a dose response manner (1, 10, 50 μM). Cellular lysates were isolated after 1 hour of treatment and immunoblotted with the indicated antibodies. |
| Concentrations | 1, 10, 50 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 489.32 |
| Formula | C21H21BrN4O5 |
| CAS Number | 1884220-36-3 |
| Solubility (25°C) | DMSO ≥ 30 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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