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Autocamtide-2-related inhibitory peptide
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Autocamtide-2-related inhibitory peptide图片
CAS NO:167114-91-2
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Autocamtide-2-related inhibitory peptide 是一种高度特异性和有效的 CaMKII 抑制剂，IC50 为 40 nM。
Cas No.167114-91-2
化学名(2S,3Z,5S,6Z,8S,9Z,11S,12Z,14S,15Z,17S)-17-((Z)-((2S,3Z,5S,6Z,8S,9Z,11S,12Z,14S,15Z,17S,18Z,20S,21Z)-17,20-bis(4-aminobutyl)-5,8-bis(3-guanidinopropyl)-1,4,7,10,13,16,19,22-octahydroxy-2-(3-hydroxy-3-iminopropyl)-11-isobutyl-14-methyl-3,6,9,12,15,18,21-he
Canonical SMILESCCCCCCCCCCCCC/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=O)([H])CC(C)C)([H])C)([H])CC(O)=O)([H])C(C)C)([H])C)([H
分子式C78H142N22O20. C2H F3O2
分子量1822.14
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,PBS (pH 7.2): 10 mg/ml
储存条件Desiccate at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 40 nM for CaM-kinase II [1].

Synthetic peptide AIP (autocamtide-2-related inhibitory peptide) is a nonphosphorylatable analog of autocamtide-2, which was identified to be a highly specific and potent inhibitor of calmodulin-dependent protein kinase II (CaM-kinase II, CaMKII). CaMKII is a serine/threonine-specific protein kinase, which is modulated by the Ca2+/calmodulin.

In vitro: AIP (1 mM) completely inhibited CaMKII activity, but did not affect cAMP-dependent protein kinase, calmodulin-dependent protein kinase IV and protein kinase C,. The inhibition was noncompetitive, and the action was caused by binding to the autophosphorylation site, which is distinc from that for the exogenous substrate. The IC50 for the autophosphorylation of CaM II is 100 nM [1].

In vivo: Mice treated with AIP by transgenic expression of AIP, were protected from fructose-rich diet-induced arrhythmogenesis, spontaneous contractions and spontaneous Ca2+ release events [2]. Intra-nucleus accumbens (NAc) injection of AIP could dose-dependently increase the HWL (hindpaw withdrawal latency) to noxious thermal and mechanical stimulation in rats with mononeuropathy [3].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Ishida A1, Kameshita I, Okuno S, Kitani T, Fujisawa H.  A novel highly specific and potent inhibitor of calmodulin-dependent protein kinase II. Biochem Biophys Res Commun. 1995 Jul 26;212(3):806-12.
[2] Sommese L, Valverde CA, Blanco P, Castro MC, Rueda OV, Kaetzel M, Dedman J, Anderson ME, Mattiazzi A, Palomeque J.  Ryanodine receptor phosphorylation by CaMKII promotes spontaneous Ca(2+) release events in a rodent model of early stage diabetes: The arrhythmogenic substrate. Int J Cardiol. 2016 Jan 1;202:394-406.
[3] Bian H, Yu LC.  Intra-nucleus accumbens administration of the calcium/calmodulin-dependent protein kinase II inhibitor AIP induced antinociception in rats with mononeuropathy. Neurosci Lett. 2015 Jul 10;599:129-32.