K252a是從擬諾卡氏菌屬分離的星形孢菌素類(lèi)似物。抑制蛋白激酶(PK) C、PKA、Ca2+/鈣調蛋白依賴(lài)性激酶ⅱ型和磷酸化酶激酶的土壤真菌，其IC50值分別為470、140、270和1.7 nM。[1]，[2]因為K252a抑制神經(jīng)營(yíng)養蛋白受體酪氨酸激酶，所以在100-500 nM波長(cháng)下，K252a被用于抑制滋養層細胞增殖，并增加與培養的絨毛膜癌細胞中線(xiàn)粒體功能破壞相關(guān)的凋亡。[3]最近，K252a被證明抑制PRK1(體外IC50 = 3.2 nM)，pr k1是一種PKC相關(guān)激酶，在蘇氨酸11位磷酸化組蛋白H3，并參與雄激素依賴(lài)性基因表達。[4]

產(chǎn)品性質(zhì)：

Cas No.;99533-80-9

別名:SF 2370

化學(xué)名:(5R,6S,8S)-methyl 6-hydroxy-5-methyl-13-oxo-6,7,8,13,14,15-hexahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate

Canonical SMILES: O[C@](C1)(C(OC)=O)[C@@]2(C)O[C@@H]1N3C4=C5N2C6=CC=CC=C6C5=C(CNC7=O)C7=C4C8=CC=CC=C38

分子式:C27H21N3O5

分子量:467.48

溶解度:Dichloromethane: 5 mg/ml,DMSO: 50 mg/ml,Methanol: 2 mg/ml

儲存條件:Desiccate at -20°C

注意事項：

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References:

[1]. Yasuzawa, T., Iida, T., Yoshida, M., et al. The structures of the novel protein kinase C inhibitors K-252a, b, c AND d. Journal of Antibiotics 39(8), 1072-1078 (1986).

[2]. Davis, P.D., Hill, C.H., Lawton, G., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides. Journal of Medicinal Chemistry 35, 177-184 (1992).

[3]. Kawamura, N., Kawamura, K., Manabe, M., et al. Inhibition of brain-derived neurotrophic factor/tyrosine kinase B signaling suppresses choriocarcinoma cell growth. Endocrinology 151(7), 3006-3014 (2010).

[4]. K?hler, J., Erlenkamp, G., Eberlin, A., et al. Lestaurtinib inhibits histone phosphorylation and androgen-dependent gene expression in prostate cancer cells. PLoS One 7(4), (2012).