cGMP依賴性蛋白激酶(PKG)的活性受升高細(xì)胞cGMP的因子(如一氧化氮)和降低cGMP水平的因子(如某些磷酸二酯酶)的控制。KT 5823是一種有效的選擇性cGMP依賴性蛋白激酶(PKG)抑制劑(體外IC50 = 234nM)。1 KT 5823具有細(xì)胞滲透性，經(jīng)常在完整細(xì)胞中用于評(píng)估PKG在信號(hào)傳導(dǎo)中的作用，盡管也有其抑制細(xì)胞中PKG效果不佳的情況。[2] KT 5823是PKC (Ki = 4 M)和PKA (Ki >10 M)的弱抑制劑。[1]

產(chǎn)品性質(zhì)：

Cas No.:126643-37-6

別名:蛋白激酶仰制劑KT5823

化學(xué)名:(5S,6S,8S)-methyl 6-methoxy-5,14-dimethyl-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([C@@]([C@]1(C)O[C@@H]2N3C4=C5N1C6=CC=CC=C6C5=C(CN(C)C7=O)C7=C4C8=CC=CC=C38)(C2)OC)OC

分子式:C29H25N3O5

分子量:495.53

溶解度:1mg/mL in ethyl acetate or 20mg/mL in DMSO

儲(chǔ)存條件:Desiccate at -20°C

注意事項(xiàng)：

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References:

[1]. Hidaka, H., and Kobayashi, R. Pharmacology of protein kinase inhibitors. Annu. Rev. Pharmacol. Toxicol. 32, 377-397 (1992).

[2]. Burkhardt, M., Glazova, M., Gambaryan, S., et al. KT5823 inhibits cGMP-dependent protein kinase activity in vitro but not in intact human platelets and rat mesangial cells. J. Biol. Chem. 275(43), 33536-33541 (2000).