1072443-89-0
1072443-89-0 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點452.9±45.0 °C(Predicted)
密度1.039±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)13.57±0.20(Predicted)
形態(tài)白色固體。
顏色Off-white to light yellow
常見問題列表
生物活性
SK1-I (BML-258) 是鞘氨醇的類似物，是同功酶特異性 SPHK1 競爭抑制劑，Ki 值為 10 μM。SK1-I (BML-258) 具有良好的水溶性。SK1-I (BML-258) 對 SPHK2，PKCα，PKCδ，PKA，AKT1，ERK1，EGFR，CDK2，IKKβ 或 CamK2β 無活性。SK1-I (BML-258) 增強(qiáng)自噬并具有抗腫瘤活性。靶點
Ki: 10 μM (SPHK1)
體外研究
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. |
體內(nèi)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). |