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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)
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
Ruslana Bryk et al.
Bioorganic & medicinal chemistry letters, 21(13), 4108-4114 (2011-06-03)
We report the identification of new, structurally diverse inhibitors of interferon-induced, double-stranded RNA-activated protein kinase (PKR) using a combined experimental and computational approach. A training set with which to build a predictive statistical model was generated by screening a set
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
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
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