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KT 5823
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 5823图片
CAS NO:126643-37-6
包装与价格:
包装价格(元)
25ug电议
50ug电议
100ug电议
500ug电议

产品介绍
KT 5823 是一种选择性 cGMP 依赖性蛋白激酶 (PKG) 抑制剂,Ki 值为 0.23 μM,它还抑制 PKA 和 PKC,Ki 值分别为 10 μM 和 4 μM。
Cas No.126643-37-6
别名蛋白激酶仰制剂KT5823
化学名(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 SMILESO=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
储存条件Desiccate at -20°C
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

The activity of cGMP-dependent protein kinase (PKG) is controlled by factors that elevate cellular cGMP, like nitric oxide (NO), and by those that reduce cGMP levels, like certain phosphodiesterases. KT 5823 is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC50 = 234 nM).1 KT 5823 is cell-permeable and is often used in intact cells to assess the role of PKG in signaling, although there are cases where it poorly inhibits PKG in cells.[2] KT 5823 is a weak inhibitor of PKC (Ki = 4 μM) and PKA (Ki >10 μM).[1]

Reference:
[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).