RB-042
RB-042 is a SK1 and SK2 inhibitor with IC50 values of 5.3 μM and 5.0 μM, respectively. RB-042 is applicable to the research of inflammatory diseases.
For research use only. We do not sell to patients.
- CAS No.: 1491909-40-0
- Formula: C25H43NO
- Molecular Weight:373.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
SphK1 5.3 μM (IC50) |
SphK2 5.0 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
5.3 μM
Compound: RB-042
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Inhibition of recombinant sphingosine kinase 1 (unknown origin) expressed in HEK293 cells using sphingosine as substrate after 30 mins in presence of [gamma32P]-ATP
Inhibition of recombinant sphingosine kinase 1 (unknown origin) expressed in HEK293 cells using sphingosine as substrate after 30 mins in presence of [gamma32P]-ATP
|
[PMID: 24164513] |
In Vitro
RB-042 is an equipotent inhibitor of sphingosine kinase 1 and sphingosine kinase 2, with an IC50 value of 5.3 μM against SK1 and 5.0 μM against SK2[1].
RB-042 binds to the catalytic site of sphingosine kinase 1 via polar interactions with residues D178, D81, and L268[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1491909-40-0
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Molecular Weight 373.63
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Formula C25H43NO
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SMILES
C(CC1=CC=C(CCCCCCCCCCCC)C=C1)N2[C@@H](CO)CCC2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[1]. Baek DJ, et al. Structure-activity relationships and molecular modeling of sphingosine kinase inhibitors. J Med Chem. 2013;56(22):9310-9327. [Content Brief]
[2]. Shrestha J, et al. Synthesis of Novel FTY720 Analogs with Anticancer Activity through PP2A Activation. Molecules. 2018;23(11):2750. Published 2018 Oct 24. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)