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616451 TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem

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 & Dep

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Synonyme: [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

Primary Target: TGF-β receptor I kinase
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616451
Preis & Verfügbarkeit

Übersicht

Key Spec Table

CAS #Empirical Formula
396129-53-6C₁₇H₁₂N₄

Preis & Verfügbarkeit

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616451-5MG
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      		 Kst.-Ampulle 5 mg
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      Description
      OverviewA 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).
      Catalogue Number616451
      Brand Family Calbiochem®
      Synonyms[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
      References
      ReferencesSawyer, J.S., et al. 2003. J. Med. Chem. 46, 3953.
      Singh, J., et al. 2003. Bioorg. Med. Chem. Lett. 13, 4355.
      Product Information
      CAS number396129-53-6
      ATP CompetitiveY
      FormBrown solid
      Hill FormulaC₁₇H₁₂N₄
      Chemical formulaC₁₇H₁₂N₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ200
      Biological Information
      Primary TargetTGF-β receptor I kinase
      Primary Target IC<sub>50</sub>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
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Carcinogenic / Teratogenic
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Bestellnummer GTIN
      616451-5MG 04055977185805