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经验公式(希尔记法):
C27H21N3O5
化学文摘社编号:
分子量:
467.47
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
200-664-3
MDL number:
产品名称
K-252a, Ready Made Solution, from Nonomuraea longicatena, >98%
InChI key
KOZFSFOOLUUIGY-SOLYNIJKSA-N
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
SMILES string
[H][C@]12C[C@](O)(C(=O)OC)[C@](C)(O1)n3c4ccccc4c5c6CNC(=O)c6c7c8ccccc8n2c7c35
biological source
Nonomuraea longicatena
assay
>98%
form
solution
shipped in
dry ice
storage temp.
−20°C
Quality Level
Gene Information
human ... NTRK1(4914)
rat ... Prkca(24680)
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Biochem/physiol Actions
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。
Physical form
以 0.2μm 过滤的 1 mM 二甲亚砜 (DMSO) 溶液形式提供。
存储类别
10 - Combustible liquids
wgk
WGK 1
flash_point_f
188.6 °F - closed cup
flash_point_c
87 °C - closed cup
ppe
Eyeshields, Gloves, multi-purpose combination respirator cartridge (US)
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)
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
Siba P Raychaudhuri et al.
The Journal of investigative dermatology, 122(3), 812-819 (2004-04-17)
The peripheral nervous system, in addition to its sensory and motor functions, can induce a local inflammatory response known as neurogenic inflammation. This phenomenon plays a critical role in several inflammatory diseases, e.g., asthma, atopy, rheumatoid arthritis, psoriasis, and ulcerative
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