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^[1][2][3].

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.

KAI-1678 (subcutaneous infusion) exerts dose-dependent effects in rodent models including carrageenan-induced acute inflammatory pain in rats, chronic constriction injury (CCI), and L5 spinal nerve transection-induced peripheral neuropathy, and reverses inflammatory hyperalgesia and mechanical allodynia^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

2540.93

C₁₀₇H₁₉₀N₄₄O₂₈

1041004-14-1

Ac-Glu-Ala-Val-Ser-Leu-Lys-Pro-Thr-Gly-Gly-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2

Ac-EAVSLKPTGGYGRKKRRQRRR-NH2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]