product name SBI-0206965
Description: SBI-0206965 is a highly potent and selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, it is about 7-fold selectivity over ULK2. SBI-0206965 is a highly selective ULK1 kinase inhibitor in vitro and suppressed ULK1-mediated phosphorylation events in cells, regulating autophagy and cell survival. SBI-0206965 greatly synergized with mechanistic target of rapamycin (mTOR) inhibitors to kill tumor cells, providing a strong rationale for their combined use in the clinic.
References: Mol Cell. 2015 Jul 16;59(2):285-97.
489.32
Formula
C21H21BrN4O5
CAS No.
1884220-36-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 97 mg/mL (198.2 mM)
Water: < 1 mg/mL
Ethanol: 10 mg/mL (20.4 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19396823
| In Vitro |
In vitro activity: In HEK293T transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibits Ser249 phosphorylation of overexpressed Vps34 and Beclin1 Ser15 phosphorylation. SBI-0206965 suppresses autophagy induced by mTOR inhibition in A549 cells, and prevents ULK1-dependent cell survival in WT MEFs. In addition, SBI-0206965 also synergizes with mTOR inhibition to induce cancer cell death. Kinase Assay: Cell Assay: In HEK293T cells transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibited Ser249 phosphorylation of overexpressed Vps34 at the dose of ~ 5 μM. In HEK293T cells, it was found that SBI-0206965 also inhibited the phosphorylation of Beclin1 Ser15 to comparable extents. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Mol Cell. 2015 Jul 16;59(2):285-97. |
Related Posts
product name SBI-0206965
Description: SBI-0206965 is a highly potent and selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, it is about 7-fold selectivity over ULK2. SBI-0206965 is a highly selective ULK1 kinase inhibitor in vitro and suppressed ULK1-mediated phosphorylation events in cells, regulating autophagy and cell survival. SBI-0206965 greatly synergized with mechanistic target of rapamycin (mTOR) inhibitors to kill tumor cells, providing a strong rationale for their combined use in the clinic.
References: Mol Cell. 2015 Jul 16;59(2):285-97.
489.32
Formula
C21H21BrN4O5
CAS No.
1884220-36-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 97 mg/mL (198.2 mM)
Water: < 1 mg/mL
Ethanol: 10 mg/mL (20.4 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19396823
| In Vitro |
In vitro activity: In HEK293T transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibits Ser249 phosphorylation of overexpressed Vps34 and Beclin1 Ser15 phosphorylation. SBI-0206965 suppresses autophagy induced by mTOR inhibition in A549 cells, and prevents ULK1-dependent cell survival in WT MEFs. In addition, SBI-0206965 also synergizes with mTOR inhibition to induce cancer cell death. Kinase Assay: Cell Assay: In HEK293T cells transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibited Ser249 phosphorylation of overexpressed Vps34 at the dose of ~ 5 μM. In HEK293T cells, it was found that SBI-0206965 also inhibited the phosphorylation of Beclin1 Ser15 to comparable extents. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Mol Cell. 2015 Jul 16;59(2):285-97. |