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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 & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: TGF-β receptor I kinase
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
396129-53-6C₁₇H₁₂N₄

Products

Catalogue NumberPackaging Qty/Pack
616451-5MGCN 塑膠安瓿;塑膠針藥瓶 5 mg
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
Applications
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
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
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
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
616451-5MGCN 04055977185805

Documentation

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

Title

Safety Data Sheet (SDS) 

TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem Certificates of Analysis

TitleLot Number
616451

References

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

Citations

Title
  • Anush Oganesian, et al. (2006) The NH2-terminal propeptide of type I procollagen acts intracellularly to modulate cell function. Journal of Biological Chemistry 281, 38507-38518.
    		•
    Data Sheet

    Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

    Revision13-January-2010 RFH
    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
    DescriptionA 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).
    FormBrown solid
    Intert gas (Yes/No) Packaged under inert gas
    CAS number396129-53-6
    Chemical formulaC₁₇H₁₂N₄
    Structure formulaStructure formula
    Purity≥97% by HPLC
    SolubilityDMSO (5 mg/ml)
    Storage Protect from light
    +2°C to +8°C
    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.
    Toxicity Carcinogenic / Teratogenic
    ReferencesSawyer, J.S., et al. 2003. J. Med. Chem. 46, 3953.
    Singh, J., et al. 2003. Bioorg. Med. Chem. Lett. 13, 4355.
    Citation
  • Anush Oganesian, et al. (2006) The NH2-terminal propeptide of type I procollagen acts intracellularly to modulate cell function. Journal of Biological Chemistry 281, 38507-38518.
    		•