Description
SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki 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.
Product information
CAS Number: 1072443-89-0
Molecular Weight: 313.86
Formula: C17H28ClNO2
Chemical Name: 2-(methylamino)-5-(4-pentylphenyl)pent-4-ene-1,3-diol hydrochloride
Smiles: Cl.CCCCCC1=CC=C(C=C1)C=CC(O)C(CO)NC
InChiKey: SGCJOKUPGVFNKS-CALJPSDSSA-N
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+;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
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.
Products are for research use only. Not for human use.
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