SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K i value of 10 µM SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ , PKA , AKT1 , ERK1 , EGFR , CDK2 , IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity . In Vitro SK1-I hydrochloride (0-10 μM; 24 hours) attenuates cancer cell growth and survival in a TP53-dependent manner in HCT116 cells and HCT116 cells bearing TP53 cancer. SK1-I hydrochloride (0-20 μM; 12 hours) induces more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53, leading to a hallmark of apoptosis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HCT116 cells and HCT116 cells bearing TP53 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 AnalysisCell Line: HCT116 cells and HCT116 cells bearing TP53 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. In Vivo Pre-treatment with SK1-I hydrochloride (BML-258 hydrochloride; 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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). Form:Liquid IC50& Target:SphK1
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SK1-I hydrochloride
CAS number：2366222-05-9 molecular formula：C17H28ClNO2
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| Chinese alias | SK1-I盐酸盐 | ||
| English alias | - | ||
| CAS number | 2366222-05-9 | molecular formula | C17H28ClNO2 |
| molecular weight | 313.86 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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