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Merck

559389

SB 203580

≥98% (HPLC), film (Thin), p38 MAP kinase inhibitor, Calbiochem®

同義詞:

SB 203580, 4-(4-氟苯基)-2-(4-甲基亚磺酰基苯基)-5-(4-吡啶基)1H-咪唑，p38 MAP激酶抑制剂XVI

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經驗公式（希爾表示法）:
C21H16FN3OS
CAS 編號:
152121-47-6
分子量：:
377.43
MDL號碼:
MFCD00922198
分類程式碼代碼:
12352200
NACRES:
NA.77

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產品名稱

SB 203580, SB 203580, CAS 152121-47-6, is a highly specific, potent, cell-permeable, selective, reversible, and ATP-competitive inhibitor of p38 MAP kinase (IC50 = 34 nM in vitro, 600 nM in cells).

品質等級

100

化驗

≥98% (HPLC)

形狀

film (Thin)

製造商／商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

溶解度

DMSO: 30 mg/mL

運輸包裝

ambient

儲存溫度

−20°C

SMILES 字串

Fc1ccc(cc1)c2nc([nH]c2c4ccncc4)c3ccc(cc3)[S+]([O-])C

InChI

1S/C21H16FN3OS/c1-27(26)18-8-4-16(5-9-18)21-24-19(14-2-6-17(22)7-3-14)20(25-21)15-10-12-23-13-11-15/h2-13H,1H3,(H,24,25)

InChI 密鑰

CDMGBJANTYXAIV-UHFFFAOYSA-N

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本產品
S8307559388559398
SB 203580 SB 203580, CAS 152121-47-6, is a highly specific, potent, cell-permeable, selective, reversible, and ATP-competitive inhibitor of p38 MAP kinase (IC50 = 34 nM in vitro, 600 nM in cells).

Sigma-Aldrich

559389

SB 203580

SB 203580 solid, ≥98% (HPLC)

Sigma-Aldrich

S8307

SB 203580

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).

Millipore

559388

SB 202190

SB 203580 InSolution, ≥98%, 1 mg/ml, reversible inhibitor of p38 MAP kinase

Sigma-Aldrich

559398

SB 203580

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

film (Thin)

form

solid

form

solid

form

liquid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

solubility

DMSO: 30 mg/mL

solubility

DMSO: ≥20 mg/mL

solubility

DMSO: 50 mg/mL

solubility

-

一般說明

降低表阿霉素诱导的细胞损伤和caspase-3/7活性。p38 MAP激酶的一种高度特异性、有效性、细胞渗透性、选择性、可逆性和ATP竞争性抑制剂（体外IC50=34 nM，细胞内为600 nM）。在100 µM时不会显著抑制JNK和p42 MAP激酶。抑制LPS刺激的人单核细胞和人单核细胞系THP-1产生IL-1和TNFα（IC50=50-100 nM）。抑制骨形态发生蛋白-2诱导的PC12细胞突起生长。还可抑制由胶原蛋白（IC50 = 0.2-1.0 µM）或血栓素类似物U-46619（目录号538944）引起的血小板聚集。也可提供SB 203580（目录号559398）在无水DMSO中的1 mg/ml溶液。

生化／生理作用

产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：在体外对p38 MAP激酶为34 nM，在细胞中为600 nM；对LPS刺激的人单核细胞和人单核细胞系TNF-α产生的IL-1和TNF-为50-100 nM；对胶原蛋白引起的血小板聚集为0.2-1.0 µM

其他說明

Yamada.T., et al. 2012.Free Radic.Biol. Med. (In press)
Powell, D.J., et al. 2003.Mol.Cell Biol.23, 7794.
Davies, S.P., et al. 2000.Biochem.J.351, 95.
Iwasaki, S., et al. 1999.J. Biol. Chem.274, 26503.
Gallagher, T.F., et al. 1997.Bioorg.Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997.Biochem.36, 10422.
Hazzalin, C.A., et al. 1996.Curr.Biol.6, 1028.
Kramer, R.M., et al. 1996.J. Biol. Chem.271, 27723.
Saklatvala, J., et al. 1996.J. Biol. Chem. 271, 6586.
Cuenda, A., et al. 1995.FEBS Lett.364, 229.
Gallagher, T.F., et al. 1995.Bioorg.Med. Chem. Lett.5, 1171.
Lee, J.C., et al. 1994.Nature 372, 739.

法律資訊

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

免責聲明

毒性：刺激性（B）

象形圖

Exclamation mark
GHS07

訊號詞

Warning

危險聲明

H302

危險分類

Acute Tox. 4 Oral

儲存類別代碼

13 - Non Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析證明 (COA)

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相關內容

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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