| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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?±?3.5?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). |
| [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 |
|
| Company Name: |
Enzo Biochem Inc
|
| Tel: |
Enzo Biochem Inc. 13797054060 |
| Website: |
www.enzo.com |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|