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Merck
CN

05288

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:
分子量:
467.47
NACRES:
NA.85
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Form:
powder
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biological source

Nocardiopsis sp.

form

powder

antibiotic activity spectrum

viruses

mode of action

enzyme | inhibits

storage temp.

−20°C

SMILES string

[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

Gene Information

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

Application

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

Biochem/physiol Actions

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


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pictograms

Health hazard

signalword

Danger

Hazard Classifications

Repr. 1B - STOT SE 2

target_organs

Eyes,Central nervous system

存储类别

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

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

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

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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
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
A new antibiotic SF-2370 produced by Actinomadura.
M Sezaki et al.
The Journal of antibiotics, 38(10), 1437-1439 (1985-10-01)



全球贸易项目编号

货号GTIN
05288-100UG-F04061838637277