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| Product Name: | SK1-I | | Synonyms: | SK1-I;BML-258 HCl;BML 258;BML258;BML-258;D-erythro-Pent-1-enitol, 1,2,4-trideoxy-4-(methylamino)-1-(4-pentylphenyl)-, (1E)- | | CAS: | 1072443-89-0 | | MF: | C17H27NO2 | | MW: | 277.41 | | EINECS: | | | Product Categories: | | | Mol File: | 1072443-89-0.mol |  |
| | SK1-I Chemical Properties |
| Boiling point | 452.9±45.0 °C(Predicted) | | density | 1.039±0.06 g/cm3(Predicted) | | form | White solid. | | pka | 13.57±0.20(Predicted) | | color | Off-white to light yellow |
| | SK1-I Usage And Synthesis |
| Uses | 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]. | | 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±3.5g) [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). |
| | IC 50 | SphK1 | | References | [1] Melissa R Pitman, et al. Inhibitors of the sphingosine kinase pathway as potential therapeutics. Curr Cancer Drug Targets. 2010 Jun;10(4):354-67. DOI:10.2174/156800910791208599
[2] Santiago Lima, et al. TP53 is required for BECN1- and ATG5-dependent cell death induced by sphingosine kinase 1 inhibition. Autophagy. 2018;14(6):942-957. DOI:10.1080/15548627.2018.1429875
[3] Fiona H Greig, et al. Requirement for sphingosine kinase 1 in mediating phase 1 of the hypotensive response to anandamide in the anaesthetised mouse. Eur J Pharmacol. 2019 Jan 5;842:1-9. DOI:10.1016/j.ejphar.2018.10.027 |
| | SK1-I Preparation Products And Raw materials |
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