蛋白激酶仰制剂KT5823

蛋白激酶仰制剂KT5823用途

KT5823 是一种选择性 cGMP 依赖性蛋白激酶 (PKG) 抑制剂,Ki值为 0.23 μM,KT5823 也可以抑制 PKA 和 PKC,Ki值分别为 10 μM 和 4 μM。KT5823 是一种 staurosporine 星形孢菌素相关的蛋白激酶抑制剂,在甲状腺细胞中增加甲状腺刺激激素诱导的 (Na+/I- symporter) NIS 表达和碘离子摄取。KT5823 引起细胞凋亡 (apoptotic) DNA 片段化水平的增加。

蛋白激酶仰制剂KT5823名称

[ CAS 号 ]:
126643-37-6

[ 中文名 ]:
蛋白激酶仰制剂KT5823

[ 英文名 ]:
KT5823

[英文别名 ]:

MFCD00132119

蛋白激酶仰制剂KT5823生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

信号通路 >> 表观遗传学 >> PKC

信号通路 >> 蛋白酪氨酸激酶 >> PKA

研究领域 >> 其他

信号通路 >> 干细胞及 Wnt 通路 >> PKA

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[ 靶点 ]

PKA:10 μM (Ki)

PKC:4 μM (Ki)

[参考文献]

[1]. 1.Gadbois DM, et al. Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells. Proc Natl Acad Sci U S A. 1992 Sep 15;89(18):8626-30.

[2]. Wyatt TA, et al. KT5823 activates human neutrophils and fails to inhibit cGMP-dependent protein kinase phosphorylation of vimentin. Res Commun Chem Pathol Pharmacol. 1991 Oct;74(1):3-14.

[3]. Chan SL, et al. Guanylyl cyclase inhibitors NS2028 and ODQ and protein kinase G (PKG) inhibitor KT5823 trigger apoptotic DNA fragmentation in immortalized uterine epithelial cells: anti-apoptotic effects of basal cGMP/PKG. Mol Hum Reprod. 2003 Dec;9(12):775-83.

蛋白激酶仰制剂KT5823物理化学性质

[ 密度 ]:
1.52g/cm3

[ 沸点 ]:
629.2ºC at 760mmHg

[ 分子式 ]:
C₂₉H₂₅N₃O₅

[ 分子量 ]:
495.52600

[ 闪点 ]:
334.3ºC

[ 精确质量 ]:
495.17900

[ PSA ]:
74.93000

[ LogP ]:
4.58930

[ 蒸汽压 ]:
9.67E-16mmHg at 25°C

[ 折射率 ]:
1.763

[ 储存条件 ]:
-20°C，密封，干燥

蛋白激酶仰制剂KT5823MSDS

详细MSDS(安全技术说明书)

蛋白激酶仰制剂KT5823安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

蛋白激酶仰制剂KT5823合成路线

详细合成路线

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蛋白激酶仰制剂KT5823文献

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Biochem. Pharmacol. 91(2) , 191-201, (2014)

The nitroderivative 1-nitro-2-phenylethane (NPE) was recently described as a compound possessing heme-dependent soluble guanylyl cyclase (sGC) stimulating properties in vascular smooth muscle cells. I...

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