SK1-I
| 中文名称 | SK1-I |
|---|---|
| 中文同义词 | 化合物 T30485;BML 258|||BML-258|||BML258|||BML-258 HCL |
| 英文名称 | SK1-I |
| 英文同义词 | SK1-I;BML-258 HCl;BML 258;BML258;BML-258;D-erythro-Pent-1-enitol, 1,2,4-trideoxy-4-(methylamino)-1-(4-pentylphenyl)-, (1E)- |
| CAS号 | 1072443-89-0 |
| 分子式 | C17H27NO2 |
| 分子量 | 277.41 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1072443-89-0.mol |
| 结构式 |  |
SK1-I 性质
| 沸点 | 452.9±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.039±0.06 g/cm3(Predicted) |
| 形态 | 白色固体。 |
| 酸度系数(pKa) | 13.57±0.20(Predicted) |
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。
Ki: 10 µM (SPHK1)
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. |
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). |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-119016 | SK1-I | 1 mg | 1590元 | |
| 2024/04/30 | HY-119016 | SK1-I SK1-I | 1072443-89-0 | 5mg | 3500元 |