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KT 5720
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。
KT 5720图片
CAS NO:108068-98-0
包装与价格:
包装价格(元)
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产品介绍
KT 5720 是一种可渗透细胞的、有效的、特异性的、可逆的、ATP 竞争性的蛋白激酶 A (PKA) 抑制剂,Ki 为 60 nM。
Cas No.108068-98-0
别名蛋白激酶仰制剂KT5720
化学名(5S,6S,8R)-hexyl 6,13-dihydroxy-5-methyl-6,7,8,15-tetrahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate
Canonical SMILESCCCCCCOC([C@]([C@@]12C)(O)C[C@](O2)([H])N3C4=CC=CC=C4C5=C6C(CN=C6O)=C7C8=CC=CC=C8N1C7=C53)=O
分子式C32H31N3O5
分子量537.61
溶解度DMSO: 1 mg/ml; Methanol: 5 mg/ml
储存条件Store at -20℃
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

Protein kinase A (PKA) regulates multiple signal transduction events via protein phosphorylation and is integral to all cellular responses involving the cyclic AMP second messenger system. KT 5720 is one of a family of compounds synthesized by the fungus Nocardiopsis sp. It blocks PKA signaling through competitive inhibition of ATP with a Ki value of 60 nM.[1] Reported IC50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 μM (physiologic ATP).[2],[3] Non-specific effects of KT 5720 include inhibition of phosphorylase kinase, PDK1, MEK, MSK1, PKBα, and GSK3β at concentrations as effective as or more potent than that for inhibition of PKA.[2],[3]

Reference:
[1]. Kase, H., Iwahashi, K., Nakanishi, S., et al. K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases. Biochemical and Biophysical Research Communications 142(2), 436-440 (1987).
[2]. Davies, S.P., Reddy, H., Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem. J. 351(1), 95-105 (2000).
[3]. Murray, A.J. Pharmacological PKA inhibition: All may not be what it seems. Science Signaling 1(22), (2008).