蛋白激酶A (PKA)通過蛋白磷酸化調(diào)節(jié)多種信號轉(zhuǎn)導(dǎo)事件，是所有涉及環(huán)磷酸腺苷第二信使系統(tǒng)的細(xì)胞反應(yīng)的組成部分。KT 5720是由真菌Nocardiopsis sp .合成的化合物家族之一。它通過競爭性抑制ATP來阻斷PKA信號，Ki值為60 nM。[1]根據(jù)測試的ATP濃度，報告的IC50值變化很大，范圍從56 nM(低ATP)到3 M(生理ATP)。[2]，[3]KT 5720的非特異性作用包括在與抑制PKA同樣有效或更有效的濃度下抑制磷酸化酶激酶、PDK1、MEK、MSK1、PKBα和GSK3β。[2],[3]

產(chǎn)品性質(zhì)：

Cas No.:108068-98-0

別名:蛋白激酶仰制劑KT5720

化學(xué)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

儲存條件:Store at -20°C

注意事項(xiàng)：

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References:

[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).