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Merck
CN

559396

SB 220025

A cell-permeable, potent, reversible, ATP-competitive, and specific inhibitor of human p38 MAP Kinase (IC50 = 60 nM).

别名:

SB 220025, 5-(2-Amino-4-pyrimidinyl)-4-(4-fluorophenyl)-1-(4-piperidinlyl)imidazole, p38 MAP Kinase Inhibitor XIV

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关于此项目

经验公式(希尔记法):
C18H19FN6
化学文摘社编号:
分子量:
338.38
MDL number:
UNSPSC Code:
12352202
NACRES:
NA.77
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产品名称

SB 220025, A cell-permeable, potent, reversible, ATP-competitive, and specific inhibitor of human p38 MAP Kinase (IC50 = 60 nM).

SMILES string

Fc1ccc(cc1)c2nc[n](c2c4nc(ncc4)N)C3CCNCC3

InChI

1S/C18H19FN6/c19-13-3-1-12(2-4-13)16-17(15-7-10-22-18(20)24-15)25(11-23-16)14-5-8-21-9-6-14/h1-4,7,10-11,14,21H,5-6,8-9H2,(H2,20,22,24)

InChI key

VSPFURGQAYMVAN-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

potency

60 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

white to pale yellow

solubility

DMSO: 22 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

Biochem/physiol Actions

Primary Target
P38MAPK

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, potent, reversible, ATP-competitive, and specific inhibitor of human p38 MAP Kinase (IC50 = 60 nM). Binds to an extended pocket in the active site of the enzyme. Exhibits over 2000-fold greater selectivity for p38 MAPK over ERK (p42/p44 MAP kinase), 500-fold over PKA, 50-fold over PKC, and >1000-fold over EGFR. Also acts as a potent inhibitor of angiogenesis and as an inhibitor of LPS-induced TNF-α production.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
A potent and specific inhibitor of human p38 mitogen-activated protein (MAP) kinase (IC50 = 60 nM). Binds to an extended pocket in the active site of the enzyme. Exhibits >2500-fold greater selectivity for p38 MAPK over ERK (p42/p44 MAP kinase), 500-fold over PKA, 50-fold over PKC, and >1600-fold over EGFRK. Also acts as a potent inhibitor of angiogenesis and as an inhibitor of LPS-induced TNF-α production.

Other Notes

Jackson, J.R., et al. 1998. J. Pharmacol. Exp. Ther.284, 687.
Wang, Z., et al. 1998. Structure6, 1117.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 1


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