Home / Pharmacology / Enzyme-Linked Receptors / Receptor Serine/Threonine Kinases (RSTKs) / TGF-β Receptors / TGF-β Receptor Inhibitors / AZ 12799734

AZ 12799734

Cat. No. 6870 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent TGF-βRI inhibitor
Chemical Name: 4-[[4-[(2.6-Dimethyl-3-pyridinyl)oxy]-2-pyridinyl]amino]benzenesulfonamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Pathways (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for AZ 12799734

AZ 12799734 is a potent inhibitor of transforming growth factor-β type I receptor (TGF-βRI; ALK5) (IC50 = 17 nM in cellular inhibition assay and 47 nM in TGF-β-induced luciferase activity assay). Also inhibits ALK4, ALK6 and ALK7 at concentrations under 10 μM. Inhibits BMP signaling, phosphorylation of SMAD1 and SMAD2, and TGF-β-induced epithelial cell migration in vitro. Displays cardiotoxicity in vivo. Orally bioavailable.

Compound Libraries for AZ 12799734

AZ 12799734 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for AZ 12799734

M. Wt 370.43
Formula C18H18N4O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1117684-36-2
PubChem ID 25192277
InChI Key UEOZXMAOIHDDQE-UHFFFAOYSA-N
Smiles CC1=NC(C)=C(OC2=CC=NC(NC3=CC=C(C=C3)[S](N)(=O)=O)=C2)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AZ 12799734

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 37.04 100

Preparing Stock Solutions for AZ 12799734

The following data is based on the product molecular weight 370.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.7 mL 13.5 mL 27 mL
5 mM 0.54 mL 2.7 mL 5.4 mL
10 mM 0.27 mL 1.35 mL 2.7 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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References for AZ 12799734

References are publications that support the biological activity of the product.

Goldberg et al (2009) Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5). J.Med.Chem. 52 7901 PMID: 19736928

Anderton et al (2011) Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol.Pathol. 39 916 PMID: 21859884

Spender et al (2019) Preclinical evaluation of AZ12601011 and AZ12799734, inhibitors of transforming growth factor β superfamily type 1 receptors. Mol.Pharmacol. 95 222 PMID: 30459156

If you know of a relevant reference for AZ 12799734, please let us know.

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Keywords: AZ 12799734, AZ 12799734 supplier, AZ12799734, TGF-beta, RI, TGF-betaRI, ALK5, transforming, growth, factor, beta, receptor, type, 1, cell, migration, Receptors, 6870, Tocris Bioscience

Citations for AZ 12799734

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Literature in this Area

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Stem Cell Research Product Guide

Stem Cell Research Product Guide

This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:

  • Self-renewal and Maintenance
  • Differentiation
  • Reprogramming
  • Organoid Generation
  • GMP and Ancillary Material Grade Products
Stem Cells Scientific Review

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Stem Cells Poster

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Pathways for AZ 12799734

TGF-β Signaling Pathway

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.