616459

TGF-β RI Kinase Inhibitor VIII

The TGF-β RI Kinase Inhibitor VIII, also referenced under CAS 356559-20-1, controls the biological activity of TGF-β RI Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 别名: TGF-β RI Kinase Inhibitor VIII, ALK5 Inhibitor VIII, SB-525334, 6-(2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl)-quinoxaline, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor VIII
• 经验公式（希尔记法）: C₂₁H₂₁N₅
• CAS号: 356559-20-1
• 分子量: 343.42
• MDL號碼: MFCD11045307
• 分類程式碼代碼: 12352200

属性

• 品質等級: 100
• 化驗: ≥97% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: yellow
• 溶解度: DMSO: 10 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 2-8°C
• InChI: 1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)
• InChI 密鑰: DKPQHFZUICCZHF-UHFFFAOYSA-N

说明

一般說明

A cell-permeable quinoxaline compound that acts as a potent, highly selective, ATP-competitive inhibitor against type I TGF-β receptor TβR-I/ALK5 (IC₅₀ = 14.3 nM), while exhibiting 4-fold less potency toward ALK4 (IC₅₀ = 58.5 nM) and little or no activity against ALK2/3/6 and a panel of 26 other commonly studied kinases (≤29% inhibition at 10 µM). Effectively blocks (by >95%) TGF-β1-induced Smad2/3 activation (2 µM in ELT-3 cultures) and nuclear localization (1 µM in RPTE cultures), as well as TGF-β1-dependent p3TP- and ARE-luciferase transcription (0.1 µM in HaCat cultures). SB-525334 is orally available and is shown to attenuate Bleomycin- and Puromycin-induced tissue fibrosis in mice and rats in vivo.

包裝

Packaged under inert gas

警告

Toxicity: Harmful (C)

重構

Following reconstitution, aliquot and freeze (-20&deg:C). Stock solution is stable for up to 3 months at -20°C.

其他說明

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Higashiyama, H., et al. 2007. Exp. Mol. Pathol.83, 39.
Grygielko, E.T., et al. 2005. J. Pharmacol. Exp. Ther.313, 943.

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3