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.
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- CAS No.: 1041004-14-1
- 화학식: C107H190N44O28
- 분자량:2540.93
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
[1]|
PKCε |
In Vitro
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. .
In Vivo
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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분자량 2540.93
-
화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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)