KAI-1678
KAI-1678 is a selective protein kinase Cε (PKCε) inhibitor that competitively blocks the binding of PKCε to its anchoring protein RACK. KAI-1678 attenuates the responses of nociceptive neurons in rodent neuropathic pain models. KAI-1678 can be used in research related to moderate to severe postoperative pain, neuropathic pain, and postherpetic neuralgia.
For research use only. We do not sell to patients.
- CAS No.: 1041004-14-1
- Formula: C107H190N44O28
- Molecular Weight:2540.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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PKCε |
KAI-1678 competitively and selectively blocks the binding of PKC epsilon to its anchoring protein RACK2, and inhibits PKC epsilon membrane translocation as well as phosphorylation of downstream pain-related substrates[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1041004-14-1
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Molecular Weight 2540.93
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Formula C107H190N44O28
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Sequence
Ac-Glu-Ala-Val-Ser-Leu-Lys-Pro-Thr-Gly-Gly-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2
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Sequence Shortening
Ac-EAVSLKPTGGYGRKKRRQRRR-NH2
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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.
Purity & Documentation
References
[1]. Cousins MJ, et al. The safety and efficacy of KAI-1678- an inhibitor of epsilon protein kinase C (εPKC)-versus lidocaine and placebo for the treatment of postherpetic neuralgia: a crossover study design. Pain medicine (Malden, Mass.). 2013 Apr;14(4):533-40. [Content Brief]
[2]. Yonezawa T, et al. PKC delta and epsilon in drug targeting and therapeutics. Recent patents on DNA & gene sequences. 2009;3(2):96-101. [Content Brief]
[3]. Leppänen T, et al. Protein kinase C and its inhibitors in the regulation of inflammation: inducible nitric oxide synthase as an example. Basic & clinical pharmacology & toxicology. 2014 Jan;114(1):37-43. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)