CP-380736: MK2 Inhibitor FAQs, Properties & Research Use
CP-380736: MK2 Inhibitor FAQs, Properties & Research Use
CP-380736 is a potent and selective small-molecule inhibitor of MAPK-activated protein kinase 2 (MK2/MAPKAPK2), widely used in research to dissect the p38 MAPK signaling pathway and its downstream inflammatory and stress-response functions.
- Target
- MAPK-activated protein kinase 2 (MK2 / MAPKAPK2)
- Compound Class
- ATP-competitive small-molecule kinase inhibitor
- Primary Research Application
- Dissection of p38 MAPK / MK2 signaling in inflammation and stress responses
- SKU
- C124695
- Supplier
- Aladdin Scientific
- Recommended Storage
- Store at –20 °C, protected from light and moisture; verify CoA for lot-specific guidance
What Is CP-380736 and How Does It Work?
CP-380736 is a selective, ATP-competitive inhibitor of MAPK-activated protein kinase 2 (MK2, also known as MAPKAPK2). MK2 is a serine/threonine kinase that functions as a critical downstream effector of the p38 MAPK signaling cascade. Upon cellular stress or pro-inflammatory stimulation, p38 MAPK phosphorylates and activates MK2, which in turn phosphorylates substrates including HSP27 and regulates the production of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-8 at the post-transcriptional level.
By occupying the ATP-binding pocket of MK2, CP-380736 blocks kinase catalytic activity, thereby attenuating downstream phosphorylation events and cytokine output without directly inhibiting p38 MAPK itself. This selectivity makes CP-380736 a valuable pharmacological tool for researchers wishing to isolate MK2-specific biology within the broader p38 signaling network.
Solubility, Formulation, and Handling Guidelines
CP-380736 is a small organic molecule. As with many kinase inhibitors of similar chemical class, it is generally soluble in dimethyl sulfoxide (DMSO) to prepare concentrated stock solutions. Researchers should consult the Certificate of Analysis (CoA) supplied with each lot for confirmed solubility data, as values can vary slightly between batches.
Recommended practice: Prepare stock solutions in DMSO at a concentration appropriate for subsequent dilution into aqueous assay buffers or cell culture media. Keep the final DMSO concentration in biological assays at or below 0.1% (v/v) to minimise solvent cytotoxicity. Avoid repeated freeze-thaw cycles; aliquot stock solutions upon first use. Water solubility may be limited; use of solubilising vehicles or co-solvents should be validated experimentally for each assay format.
Note: Specific solubility values (mg/mL or mM) are lot-dependent. Always refer to the product CoA provided by Aladdin Scientific (SKU C124695) for authoritative figures.
Storage Conditions and Stability
For long-term stability, CP-380736 should be stored at –20 °C in a tightly sealed container, protected from light and moisture. Under these conditions, the compound is expected to remain stable for an extended period when stored as a dry solid. Once dissolved in DMSO, aliquots should be stored at –20 °C and used promptly after thawing.
Researchers should always check the expiry date and storage instructions printed on the product label and CoA. If unusual color changes, precipitation, or loss of biological activity are observed, the compound should not be used and Aladdin Scientific customer service should be contacted for guidance.
Research Applications and Experimental Considerations
CP-380736 is used as a research tool compound in a range of in vitro and cell-based assay systems. Key application areas include:
- Inflammatory disease research: Studying the role of MK2 in regulating cytokine biosynthesis (TNF-α, IL-6, IL-8) in macrophages, monocytes, and other immune cells stimulated with LPS or other pro-inflammatory agents.
- Stress-response biology: Investigating MK2-dependent phosphorylation of heat shock protein 27 (HSP27) and its impact on actin cytoskeleton dynamics and cell survival.
- Pathway dissection: Used alongside p38 inhibitors (e.g., SB203580) to discriminate p38-dependent, MK2-independent effects from those specifically mediated through MK2.
- Cancer biology: Exploring MK2's role in DNA damage response, cell cycle checkpoint regulation, and tumor cell survival under genotoxic stress.
Researchers should validate CP-380736 concentrations in their specific cell or assay system, as effective concentrations may differ between cell types and experimental conditions. Appropriate vehicle controls (DMSO at matched concentration) are essential.
Ordering, Quality, and Technical Support
CP-380736 is available from Aladdin Scientific under SKU C124695. Each lot is supplied with a Certificate of Analysis (CoA) documenting purity (typically assessed by HPLC), identity (confirmed by NMR and/or MS), and lot-specific storage recommendations.
For technical questions regarding experimental design, solubility optimisation, or assay troubleshooting, contact Aladdin Scientific's technical support team. For order-related enquiries including pricing, shipping, returns, and payment options, visit the Aladdin Scientific website or contact customer service directly.
Researchers requiring Safety Data Sheet (SDS) information for risk assessment and safe handling in compliance with local regulations should download the SDS from the product page or request it from customer service.
Frequently asked questions
What is CP-380736 used for in research?
CP-380736 is used as a selective pharmacological tool to inhibit MK2 (MAPKAPK2), a key downstream kinase in the p38 MAPK signaling pathway. It is primarily applied in studies of inflammatory cytokine regulation, cellular stress responses, DNA damage checkpoint biology, and cancer cell survival, enabling researchers to define the specific contribution of MK2 activity independently of upstream p38 MAPK inhibition.
What is the recommended solvent for dissolving CP-380736?
CP-380736 is generally prepared as a stock solution in DMSO. The final DMSO concentration in biological assays should be kept at or below 0.1% (v/v) to avoid solvent-related cytotoxicity. Lot-specific solubility data are provided in the Certificate of Analysis (CoA) supplied with SKU C124695; always consult the CoA before preparing solutions.
How should CP-380736 (SKU C124695) be stored to maintain stability?
CP-380736 should be stored as a dry solid at –20 °C in a tightly sealed, light-protected container away from moisture. DMSO stock solutions should also be stored at –20 °C in single-use aliquots to avoid repeated freeze-thaw cycles. Always verify the expiry date and storage conditions stated on the product label and CoA supplied by Aladdin Scientific.
Is CP-380736 selective for MK2 over other kinases?
CP-380736 is described as a selective MK2 inhibitor; however, as with all kinase inhibitors, off-target activity against other kinases may occur, particularly at higher concentrations. Researchers should include appropriate controls, use the lowest effective concentration, and consult published selectivity profiling data when interpreting experimental results. Specific selectivity panel data should be verified in peer-reviewed literature or the product CoA.
Can CP-380736 be used in animal studies?
While CP-380736 has been developed as a research tool compound with potential in vivo utility, in vivo pharmacokinetic properties such as bioavailability, metabolic stability, and plasma protein binding must be experimentally determined for each animal species and route of administration. Researchers intending to use CP-380736 in vivo should consult the scientific literature for any published in vivo data and conduct appropriate formulation and PK/PD studies. Aladdin Scientific supplies CP-380736 for research use only.
References
- Mourey RJ et al. A bench-to-bedside perspective on the MK2 signaling pathway. Drug Discovery Today. Review article on MK2 as a therapeutic target downstream of p38 MAPK.
- Kotlyarov A et al. MAPKAP kinase 2 is essential for LPS-induced TNF-alpha biosynthesis. Nature Cell Biology, 1999.
- Gaestel M. MAPKAP kinases – MKs – two's company, three's a crowd. Nature Reviews Molecular Cell Biology, 2006.
Products are supplied for research and development use only. Not for use in humans, animals, diagnosis, or therapy.
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