SK1-I
|
|
- CAS号:
- 1072443-89-0
- 英文名:
- SK1-I
- 英文别名:
- SK1-I;BML258;BML-258;BML 258;BML-258 HCl;D-erythro-Pent-1-enitol, 1,2,4-trideoxy-4-(methylamino)-1-(4-pentylphenyl)-, (1E)-
- 中文名:
- SK1-I
- 中文别名:
- 化合物 T30485;BML 258|||BML-258|||BML258|||BML-258 HCL
- CBNumber:
- CB12535697
- 分子式:
- C17H27NO2
- 分子量:
- 277.41
- MOL File:
- 1072443-89-0.mol
|
|
|
SK1-I化学性质
-
沸点:
-
452.9±45.0 °C(Predicted)
-
|
-
密度:
-
1.039±0.06 g/cm3(Predicted)
-
|
-
形态:
-
White solid.
-
|
-
酸度系数(pKa):
-
13.57±0.20(Predicted)
-
|
SK1-I性质、用途与生产工艺
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。
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).
|
SK1-I
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
1072443-89-0, SK1-I 相关搜索:
- BML 258|||BML-258|||BML258|||BML-258 HCL
- 化合物 T30485
- 1072443-89-0
- D-erythro-Pent-1-enitol, 1,2,4-trideoxy-4-(methylamino)-1-(4-pentylphenyl)-, (1E)-
- BML-258
- BML258
- BML 258
- BML-258 HCl
- SK1-I