CS-1581 - Names and Identifiers
CS-1581 - Physico-chemical Properties
Molecular Formula | C21H21BrN4O5
|
Molar Mass | 489.32 |
Density | 1.434±0.06 g/cm3(Predicted) |
Melting Point | 170 - 172°C |
Solubility | 10 mM in DMSO |
Appearance | powder |
Color | white to beige |
pKa | 14.80±0.46(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
In vitro study | In HEK293T transfected with WT or KI Myc-labeled ULK1 and WT Vps34, SBI-0206965 inhibited Ser249 phosphorylation and Beclin1 Ser15 phosphorylation of overexpressing vps34. In A549 cells, SBI-0206965 inhibited mTOR inhibition-induced autophagy and prevented ulk1-dependent cell survival in WT MEFs. In addition, SBI-0206965 also enhances mTOR inhibition to induce cancer cell death. |
CS-1581 - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
---|
1 mM | 2.044 ml | 10.218 ml | 20.437 ml |
5 mM | 0.409 ml | 2.044 ml | 4.087 ml |
10 mM | 0.204 ml | 1.022 ml | 2.044 ml |
5 mM | 0.041 ml | 0.204 ml | 0.409 ml |
Last Update:2024-01-02 23:10:35
CS-1581 - Reference Information
biological activity | SBI-0206965 is a highly selective autophagocytic kinase ULK1 inhibitor with IC50 of 108 nM, which is 7 times more selective than ULK2. SBI-0206965 can inhibit autophagy in human glioblastoma and lung cancer cells and enhance apoptosis. |
target | TargetValue ULK1 (cell-free say) 108 nM ULK2 (cell-free say) 711 nM |
Target | Value |
ULK1
(Cell-free assay)
| 108 nM |
ULK2
(Cell-free assay)
| 711 nM |
in vitro study | In the HEK293T transfected with WT or KI Myc-labeled ULK1 and WT Vps34, Ser249 phosphorylation and Beclin1 Ser15 phosphorylation were SBI-0206965 inhibited. In A549 cells, SBI-0206965 inhibited autophagy induced by mTOR inhibition and prevented ULK1-dependent cell survival in WT MEFs. In addition, SBI-0206965 will also enhance mTOR inhibition to induce cancer cell death. |
Last Update:2024-04-09 21:50:46