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KT 5720

(Synonyms: 蛋白激酶仰制剂KT5720) 目录号 : GC14648

A potent inhibitor of PKA

KT 5720 Chemical Structure

Cas No.:108068-98-0

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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).

Chemical Properties

Cas No. 108068-98-0 SDF
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 SMILES CCCCCCOC([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°C
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1 mM 1.8601 mL 9.3004 mL 18.6008 mL
5 mM 0.372 mL 1.8601 mL 3.7202 mL
10 mM 0.186 mL 0.93 mL 1.8601 mL
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