559388
SB 202190
≥98% (HPLC), solid, p38 MAP kinase inhibitor, Calbiochem®
别名:
SB 202190
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关于此项目
经验公式（希尔记法）:
C20H14FN3O
化学文摘社编号:
分子量:
331.34
UNSPSC Code:
12352202
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
产品名称
SB 202190, SB 202190, CAS 152121-30-7, is a potent, reversible, competitive inhibitor of p38. Inhibits p38 phosphorylation of myelin basic protein. Blocks the activity of p38β (Ki = 16 nM; IC50 = 350 nM).
Quality Level
assay
≥98% (HPLC)
form
solid
potency
16 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
Fc1ccc(cc1)C2=C(NC(=C4C=CC(=O)C=C4)N2)c3ccncc3
InChI
1S/C20H14FN3O/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(25)8-4-15/h1-12,23-24H
InChI key
NJNKPVPFGLGHPA-UHFFFAOYSA-N
General description
一种有效的、可逆的、竞争性的、细胞渗透性p38 MAP激酶抑制剂。抑制髓鞘碱性蛋白（MBP）的p38磷酸化，而不影响ERK或JNK MAP激酶亚群的活性。还抑制p38β的激酶活性（Ki=16 nM；IC50=350 nM）和激活转录因子2的p38磷酸化（ATF-2；IC50=280 nM）。阻断LPS诱导的TNF-α和白细胞介素生物合成已报道在Hep52细胞中诱导LDL受体表达。也可提供SB 202190（目录号559397）在无水DMSO中的1 mg/ml溶液。
Biochem/physiol Actions
主要靶标
p38β
p38β
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：针对p38β的激酶活性，为350 nM；针对激活转录因子2(ATF-2)的p38磷酸化，为280 nM
Preparation Note
复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多6个月。
Other Notes
Davies, S.P., et al. 2000.Biochem.J.351, 95.
Ajizian, S.J., et al. 1999.J. Infect.Dis.179, 939.
Singh, R.P., et al. 1999.J. Biol. Chem.274, 19593.
Wang, S.W., et al. 1999.Inflamm.Res.48, 533.
Gallagher, T.F., et al. 1997.Bioorg.Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997.Biochem.36, 10422.
Jiang, Y., et al. 1996.J. Biol. Chem. 271, 17920.
Kramer, R.M., et al. 1996.J. Biol. Chem.271, 27723.
Li, Z., et al. 1996.Biochem.Biophys.Res.Commun.228, 334.
Lee, J.C., et al. 1994.Nature 372, 739.
Ajizian, S.J., et al. 1999.J. Infect.Dis.179, 939.
Singh, R.P., et al. 1999.J. Biol. Chem.274, 19593.
Wang, S.W., et al. 1999.Inflamm.Res.48, 533.
Gallagher, T.F., et al. 1997.Bioorg.Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997.Biochem.36, 10422.
Jiang, Y., et al. 1996.J. Biol. Chem. 271, 17920.
Kramer, R.M., et al. 1996.J. Biol. Chem.271, 27723.
Li, Z., et al. 1996.Biochem.Biophys.Res.Commun.228, 334.
Lee, J.C., et al. 1994.Nature 372, 739.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：标准处理（A）
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存储类别
11 - Combustible Solids
Christina L Sherry et al.
Journal of immunology (Baltimore, Md. : 1950), 178(2), 663-670 (2007-01-05)
Dysregulated inflammation is a complication of type 2 diabetes (T2D). In this study, we show that augmented LPS-induced TNF-alpha production by resident peritoneal macrophages (PerMphi) in type 2 diabetic (db/db) mice is dependent on elevated glucose and requires p38 MAPK.
Tomoaki Inazumi et al.
Cell reports, 33(2), 108265-108265 (2020-10-15)
Lipolysis, the breakdown of triglyceride storage in white adipose tissue, supplies fatty acids to other tissues as a fuel under fasting conditions. In morbid obesity, fibrosis limits adipocyte expandability, resulting in enforced lipolysis, ectopic fat distribution, and ultimately insulin resistance.
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| 559388-1MG | 04055977192476 |