616451-M

TGF-β RI Kinase Inhibitor

The TGF-β RI Kinase Inhibitor, also referenced under CAS 396129-53-6, controls the biological activity of TGF-β RI Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 別名: TGF-β RI Kinase Inhibitor, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor, ALK5 Inhibitor I, [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole, TβR-I Inhibitor, LY-364947, HTS-466284, [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole, TβR-I Inhibitor, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor, ALK5 Inhibitor I, LY-364947, HTS-466284
• 実験式（ヒル表記法）: C₁₇H₁₂N₄
• CAS番号: 396129-53-6
• 分子量: 272.30
• MDL番号: MFCD00800758
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 200
• アッセイ: ≥97% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: brown
• 溶解性: DMSO: 5 mg/mL
• 保管温度: 2-8°C
• InChI: 1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21)
• InChI Key: IBCXZJCWDGCXQT-UHFFFAOYSA-N

詳細

詳細

A cell-permeable diheteroaryl-substituted pyrazole compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of TGF-β Receptor I kinase (IC₅₀ = 51 nM). Displays ~15-fold greater selectivity over p38α MAP kinase (IC₅₀ = 740 nM). Shown to inhibit TGF-β-dependent cellular growth (IC₅₀ = 89 nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC₅₀ = 47 nM in mink lung cells).

A cell-permeable, a potent, selective, reversible, and ATP-competitive inhibitor of TGF-b RI serine/threonine kinase (IC₅₀ = 51 nM). Displays ~15-fold greater selectivity over p38α MAP kinase (IC₅₀ = 740 nM). Reported to inhibit TGF-b-dependent cellular growth (IC₅₀ = 89 nM in mouse NIH3T3 fibroblasts) and transcription activation (IC₅₀ = 47 nM in mink lung cells).

生物化学的／生理学的作用

Primary Target
TGF-β receptor I kinase

Target IC₅₀: 51 nM against TGF-β Receptor I kinase; 89 nM against TGF-β-dependent cellular growth in NIH 3T3 mouse fibroblasts; 47 nM against TGF-β-dependent transcription activation in mink lung cells

警告

Toxicity: Carcinogenic / Teratogenic (D)

再構成

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

その他情報

Sawyer, J.S., et al. 2003. J. Med. Chem.46, 3953.
Singh, J., et al. 2003. Bioorg. Med. Chem. Lett.13, 4355.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3