1072443-89-0
1072443-89-0 结构式
物理化学性质
沸点452.9±45.0 °C(Predicted)
密度1.039±0.06 g/cm3(Predicted)
酸度系数(pKa)13.57±0.20(Predicted)
形态白色固体。
颜色Off-white to light yellow
常见问题列表
生物活性
SK1-I (BML-258) 是鞘氨醇的类似物，是同功酶特异性 SPHK1 竞争抑制剂，Ki 值为 10 µM。SK1-I (BML-258) 具有良好的水溶性。SK1-I (BML-258) 对 SPHK2，PKCα，PKCδ，PKA，AKT1，ERK1，EGFR，CDK2，IKKβ 或 CamK2β 无活性。SK1-I (BML-258) 增强自噬并具有抗肿瘤活性。靶点
Ki: 10 µM (SPHK1)
体外研究
SK1-I (0-10 μM; 24 hours) attenuates cancer cell growth and survival in a TP53-dependent manner in HCT116 cells and HCT116 cells bearing
TP53
null cancer.
SK1-I (0-20 μM; 12 hours) induces more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53, leading to a hallmark of apoptosis.
Cell Viability Assay
| Cell Line: | HCT116 cells and HCT116 cells bearing TP53 null cancer |
| Concentration: | 0 µM, 2.5 µM, 5 µM, 7.5 µM, 10 µM |
| Incubation Time: | 24 hours |
| Result: | Decreased cancer cell growth and survival. |
Western Blot Analysis
| Cell Line: | HCT116 cells and HCT116 cells bearing TP53 null cancer |
| Concentration: | 0 µM, 5 µM, 10 µM, 20 µM |
| Incubation Time: | 12 hours |
| Result: | Induced more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53. |
体内研究
Pre-treatment with SK1-I (BML-258; intraperitoneal (i.p.) injection; once; 24 hours prior to baseline mean arterial blood pressure (MAP) measurement; 75 mg/kg) before anandamide (i.v. injection; two doses; 1 and 10 mg/kg) significantly decreases the hypotensive response.
| 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 |
| Result: | Significantly lowered baseline mean arterial blood pressure (MAP). |