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Merck
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Key Documents

05288

Sigma-Aldrich

K-252a

from Nocardiopsis sp.

同義詞:

Protein kinase inhibitor

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About This Item

經驗公式(希爾表示法):
C27H21N3O5
CAS號碼:
分子量::
467.47
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.85

生物源

Nocardiopsis sp.

形狀

powder

抗生素活性譜

viruses

作用方式

enzyme | inhibits

儲存溫度

−20°C

SMILES 字串

[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 密鑰

KOZFSFOOLUUIGY-SOLYNIJKSA-N

基因資訊

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

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應用

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

象形圖

Health hazard

訊號詞

Danger

危險聲明

危險分類

Repr. 1B - STOT SE 2

標靶器官

Eyes,Central nervous system

儲存類別代碼

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

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

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


分析證明 (COA)

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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)
Qian Jian et al.
Experimental eye research, 132, 34-47 (2015-01-15)
Müller cells can completely repair retinal injury by acting as endogenous stem/progenitor cells in lower-order vertebrates. However, a safe and effective approach to activate progenitor potential of retinal Müller cells in higher-order vertebrates, which rarely re-enter the cell cycle, is

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