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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.
Autophagy. 2025 Oct 14; .
Lnc-HZ14 promotes LLPS-mediated SPHK1 aggrephagy degradation to suppress trophoblast cell proliferation in unexplained recurrent miscarriage
SBI-0206965 purchased from AbMole
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 |
|---|
| LYN-1604 2HCl
LYN-1604 is a novel activator of ULK1, inducing cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. |
| 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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