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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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S647696-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $350.90 | |
S647696-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $580.90 | |
S647696-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,100.90 |
Specifications & Purity | ≥98% |
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Biochemical and Physiological Mechanisms | SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K i value of 10 µM. SK1-I shows no activity at SPHK1 PKCα, PKCδ , PKA , AKT1 , ERK1 , EGFR , CDK2 , IKKβ or CamK2β. SK1-I enhances autophagy and has |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K i value of 10 µM 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 . 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 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. 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 (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. 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:Solid IC50& Target:Ki: 10 µM (SPHK1) |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | (E,2R,3S)-2-(methylamino)-5-(4-pentylphenyl)pent-4-ene-1,3-diol;hydrochloride |
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INCHI | InChI=1S/C17H27NO2.ClH/c1-3-4-5-6-14-7-9-15(10-8-14)11-12-17(20)16(13-19)18-2;/h7-12,16-20H,3-6,13H2,1-2H3;1H/b12-11+;/t16-,17+;/m1./s1 |
InChi Key | SGCJOKUPGVFNKS-UUCPMUBFSA-N |
Canonical SMILES | CCCCCC1=CC=C(C=C1)C=CC(C(CO)NC)O.Cl |
Isomeric SMILES | CCCCCC1=CC=C(C=C1)/C=C/[C@@H]([C@@H](CO)NC)O.Cl |
PubChem CID | 49793059 |
MeSH Entry Terms | BML 258;BML-258;BML258;N-methyl-5-(4'-pentylphenyl)-2-aminopent-4-ene-1,3-diol;SK1-I cpd |
Molecular Weight | 277.40 |
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Solubility | DMSO : 100 mg/mL (360.49 mM; Need ultrasonic) |
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