2366222-05-9
2366222-05-9 structure
- Name: SK1-I hydrochloride
- Chemical Name: SK1-I hydrochloride
- CAS Number: 2366222-05-9
- Molecular Formula: C17H28ClNO2
- Molecular Weight: 313.86
- Catalog: Signaling Pathways Immunology/Inflammation SPHK
- Create Date: 2021-06-09 20:44:30
- Modify Date: 2024-01-08 17:37:28
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SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. 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[2].
| Name | SK1-I hydrochloride |
|---|
| Description | SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. 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[2]. |
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| Related Catalog | |
| Target |
Ki: 10 µM (SPHK1)[1] |
| 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 null cancer[2]. 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[2]. Cell Viability Assay[2] 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[2] 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. |
| 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[3]. Animal Model: Male C57BL/6 mice (24 ± 3.5 g) [3] 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). |
| References |
| Molecular Formula | C17H28ClNO2 |
|---|---|
| Molecular Weight | 313.86 |
| Hazard Codes | Xi |
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