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。

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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

Brain natriuretic peptide constitutively downregulates P2X3 receptors by controlling their phosphorylation state and membrane localization.

Mol. Pain 11 , 71, (2015)

ATP-gated P2X3 receptors are important transducers of nociceptive stimuli and are almost exclusively expressed by sensory ganglion neurons. In mouse trigeminal ganglion (TG), P2X3 receptor function is...

Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells.

Am. J. Physiol. Cell Physiol. 303(12) , C1260-8, (2012)

In this study, the interaction of natriuretic peptides (NP) and bradykinin (BK) signaling pathways was identified by measuring membrane potential (V(m)) and intracellular Ca(2+) using the patch-clamp ...

Cytoprotective effect of 1-nitro-2-phenylethane in mice pancreatic acinar cells subjected to taurocholate: putative role of guanylyl cyclase-derived 8-nitro-cyclic-GMP.

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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