1072443-89-0
1072443-89-0 structure
- Name: SK1-I (BML-258)
- Chemical Name: (1E)-1,2,4-Trideoxy-4-(methylamino)-1-(4-pentylphenyl)-D-erythro- pent-1-enitol hydrochloride (1:1)
- CAS Number: 1072443-89-0
- Molecular Formula: C17H28ClNO2
- Molecular Weight: 313.86300
- Catalog: Signaling Pathways Immunology/Inflammation SPHK
- Create Date: 2017-10-09 06:38:56
- Modify Date: 2024-01-06 14:13:44
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SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity[2].
| Name | (1E)-1,2,4-Trideoxy-4-(methylamino)-1-(4-pentylphenyl)-D-erythro- pent-1-enitol hydrochloride (1:1) |
|---|---|
| Synonyms |
H-D-Thr-OBzl
D-Threonine Benzyl Ester SK1-I (BML-258) |
| Description | SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity[2]. |
|---|---|
| Related Catalog | |
| Target |
Ki: 10 µM (SPHK1)[1] |
| In Vitro | 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[2]. 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[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 (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[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 | 313.86300 |
| Exact Mass | 313.18100 |
| PSA | 52.49000 |
| LogP | 3.56660 |
| Hazard Codes | Xi |
|---|