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Merck
CN

K2015

Sigma-Aldrich

K-252a

From Nonomuraea longicatena, >98%, tyrosine kinase receptor inhibitor, solution

别名:

SF 2370

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关于此项目

经验公式(希尔记法):
C27H21N3O5
CAS Number:
分子量:
467.47
EC 号:
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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Product Name

K-252a, Ready Made Solution, from Nonomuraea longicatena, >98%

生物来源

Nonomuraea longicatena

质量水平

方案

>98%

表单

solution

运输

dry ice

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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生化/生理作用

K-252a 还是Trk(酪氨酸激酶)受体的特异性抑制剂,可选择性阻断神经生长因子的效应。较低浓度的 K-252a 可作为神经保护性化合物,促进原代神经元培养物存活。K-252a 通过抑制 Cdc2 和 Cdc25c,诱导细胞周期停滞和凋亡。K-252a 可改善 SCID 小鼠-人类皮肤模型中的牛皮癣状况,并可抑制与急性胰腺炎相关的机械超敏反应和神经肽上调。

特点和优势

《受体分类和信号转导》手册的 MetPKC 页面有该化合物的介绍。想要浏览手册的其他页面, 请单击此处

外形

以 0.2μm 过滤的 1 mM 二甲亚砜 (DMSO) 溶液形式提供。

储存分类代码

10 - Combustible liquids

WGK

WGK 1

闪点(°F)

188.6 °F - closed cup

闪点(°C)

87 °C - closed cup

个人防护装备

Eyeshields, Gloves, multi-purpose combination respirator cartridge (US)


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Z Pawlowska et al.
Journal of neurochemistry, 60(2), 678-686 (1993-02-01)
The phosphorylation of surface proteins by ecto-protein kinase has been proposed to play a role in mechanisms underlying neuronal differentiation and their responsiveness to nerve growth factor (NGF). PC12 clones represent an optimal model for investigating the mode of action
M A Glicksman et al.
Journal of neurochemistry, 64(4), 1502-1512 (1995-04-01)
The organic molecule K-252a promoted cell survival, neurite outgrowth, and increased choline acetyltransferase (ChAT) activity in rat embryonic striatal and basal forebrain cultures in a concentration-dependent manner. A two- to threefold increase in survival was observed at 75 nM K-252a
L S Chin et al.
Cancer investigation, 17(6), 391-395 (1999-08-06)
The indole carbazole K252a has been shown in previous studies to inhibit the platelet-derived growth factor signal transduction pathway in gliomas. Because K252a has nonspecific effects on protein kinase function, we studied its effect on cyclin-dependent kinases (CDK) and cell
Winston, J.H., et al.
Pain, 4, 329-337 (2003)
Haridas B Rode et al.
Bioorganic & medicinal chemistry, 19(1), 429-439 (2010-12-07)
Here we present the synthesis and biological activity of a series of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase (MLCK) and the epidermal growth factor receptor kinase (EGFR). The inhibitory effect of these molecules was found to be dependent

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