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Merck
CN

05288

Sigma-Aldrich

K-252a

from Nocardiopsis sp.

别名:

Protein kinase inhibitor

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关于此项目

经验公式（希尔记法）:
C27H21N3O5
化学文摘社编号:
99533-80-9
分子量:
467.47
MDL编号:
MFCD00161522
UNSPSC代码:
12352200
PubChem化学物质编号:
329747678
NACRES:
NA.85

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生物来源

Nocardiopsis sp.

表单

powder

抗生素抗菌谱

viruses

作用机制

enzyme | inhibits

储存温度

−20°C

SMILES字符串

[H][C@]12C[C@](O)(C(=O)OC)[C@](C)(O1)n3c4ccccc4c5c6CNC(=O)c6c7c8ccccc8n2c7c35

InChI

1S/C27H21N3O5/c1-26-27(33,25(32)34-2)11-18(35-26)29-16-9-5-3-7-13(16)20-21-15(12-28-24(21)31)19-14-8-4-6-10-17(14)30(26)23(19)22(20)29/h3-10,18,33H,11-12H2,1-2H3,(H,28,31)/t18-,26+,27+/m1/s1

InChI key

KOZFSFOOLUUIGY-SOLYNIJKSA-N

基因信息

human ... NTRK1(4914)
rat ... Prkca(24680)

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应用

K-252a用于抑制参与细胞信号传导过程的蛋白激酶，包括CaM激酶；磷酸化酶激酶，丝氨酸/苏氨酸激酶，Trk。 它用于抑制神经生长因子（NGF）对PC1 2细胞的作用，并抑制平滑肌肌球蛋白轻链激酶。

生化/生理作用

多种蛋白激酶（包括蛋白激酶A，C和G）的有效抑制剂。据报道，它选择性地抑制神经生长因子（NGF）对PC1 2细胞的作用，并已显示出抑制平滑肌肌球蛋白轻链激酶的作用。

象形图

Health hazard
GHS08

警示用语：

Danger

危险声明

H360D,H371

危险分类

Repr. 1B - STOT SE 2

靶器官

Eyes,Central nervous system

储存分类代码

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Faceshields, Gloves, type P3 (EN 143) respirator cartridges

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
BCCD6165
BCBV8342

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S Nakanishi et al.
The Journal of biological chemistry, 263(13), 6215-6219 (1988-05-05)
Effects of K-252a, (8R*, 9S*, 11S*)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8, 11-epoxy-1H,8H,11H-2,7b,11a-triazadibenzo[a,g]cycloocta [cde]trinden-1-one, purified from the culture broth of Nocardiopsis sp., on the activity of myosin light chain kinase were investigated. 1) K-252a (1 x 10(-5) M) affected three characteristic properties of chicken gizzard myosin-B
S Koizumi et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 8(2), 715-721 (1988-02-01)
K-252a, a kinase inhibitor isolated from the culture broth of Nocardiopsis sp., selectively inhibits the actions of nerve growth factor (NGF) on PC 12 cells. At a concentration of 200 nM, K-252a prevents neurite generation initiated by NGF, but not
A new antibiotic SF-2370 produced by Actinomadura.
M Sezaki et al.
The Journal of antibiotics, 38(10), 1437-1439 (1985-10-01)
Inhibition of actin-myosin-ATP interaction of smooth muscle native actomyosin is not closely associated with inhibition of its myosin light chain phosphorylation: studies with derivatives of antibiotic SF-2370.
K Kohama et al.
Progress in clinical and biological research, 315, 460-462 (1989-01-01)
Monique Rascher et al.
Biomolecules, 10(10) (2020-10-18)
Medicinal mushrooms of the genus Hericium are known to produce secondary metabolites with homeostatic properties for the central nervous system. We and others have recently demonstrated that among these metabolites cyathane diterpenoids and in particular erinacine C possess potent neurotrophin
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