Name | SK1-I |
Synonyms | SK1-I BML258 BML 258 BML-258 BML-258 HCl |
CAS | 1072443-89-0 |
Molecular Formula | C17H27NO2 |
Molar Mass | 277.41 |
Appearance | White solid. |
Storage Condition | -20°C,干燥,密封 |
biological activity | SK1-I (BML-258) is an analog of sphingosine, which is a competitive inhibitor of SPHK1, ki value was 10 µm. SK1-I (BML-258) has good water solubility. SK1-I (BML-258) was inactive against SPHK2, pkcα, pkcδ, PKA,AKT1,ERK1,EGFR,CDK2,IKKβ or CamK2β. SK1-I (BML-258) enhanced autophagy and had anti tumor activity. |
Target | Ki: 10 µm (SPHK1) |
Cell Line: | HCT116 cells and HCT116 cells bearing TP53 null cancer HCT116 cells and HCT116 cells bearing TP53 null cancer |
Concentration: | 0 µM, 2.5 µM, 5 µM, 7.5 µM, 10 µM 0 µM, 5 µM, 10 µM, 20 µM |
Incubation Time: | 24 hours 12 hours |
Result: | Decreased cancer cell growth and survival. Induced more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53. Significantly lowered baseline mean arterial blood pressure (MAP). |
Animal Model: | Male C57BL/6 mice (24 ± 3.5 g) |
Dosage: | 75 mg/kg |
Administration: | Intraperitoneal (i.p.) injection; once; 24 hours prior to baseline MAP measurement |