694433-59-5 | SB-505124

Packsize	Purity	Availability	Price	Discounted Price
1mg	≥98%	in stock	$48.00	$34.00
5mg	98%	in stock	$97.00	$68.00
10mg	98%	in stock	$151.00	$106.00
25mg	98%	in stock	$229.00	$161.00
50mg	98%	in stock	$395.00	$277.00
100mg	98%	in stock	$555.00	$389.00

Description

• Catalog Number: AH15228
• Chemical Name: SB-505124
• CAS Number: 694433-59-5
• Molecular Formula: C20H21N3O2
• Molecular Weight: 335.3996
• MDL Number: MFCD20926329
• SMILES: Cc1cccc(n1)c1[nH]c(nc1c1ccc2c(c1)OCO2)C(C)(C)C

Computed Properties

• Complexity: 466
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 25
• Hydrogen Bond Acceptor Count: 4
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 3
• XLogP3: 4.3

Literature

• Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.

  Journal of medicinal chemistry 20140522

• A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.

  The Biochemical journal 20130415

• NODAL and SHH dose-dependent double inhibition promotes an HPE-like phenotype in chick embryos.

  Disease models & mechanisms 20130301

• Endothelial cell transforming growth factor-β receptor activation causes tacrolimus-induced renal arteriolar hyalinosis.

  Kidney international 20121001

• Cdk4/6 inhibition induces epithelial-mesenchymal transition and enhances invasiveness in pancreatic cancer cells.

  Molecular cancer therapeutics 20121001

• Yin-Yang1 is required for epithelial-to-mesenchymal transition and regulation of Nodal signaling during mammalian gastrulation.

  Developmental biology 20120815

• Transforming growth factor-β2 induces synthesis and secretion of endothelin-1 in human trabecular meshwork cells.

  Investigative ophthalmology & visual science 20120807

• Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.

  Nature biotechnology 20111101

• Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

  European journal of medicinal chemistry 20110901

• Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

  Bioorganic & medicinal chemistry 20110415

• Smad signaling determines chondrogenic differentiation of bone-marrow-derived mesenchymal stem cells: inhibition of Smad1/5/8P prevents terminal differentiation and calcification.

  Tissue engineering. Part A 20110401

• Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

  Bioorganic & medicinal chemistry letters 20100715

• Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

  Bioorganic & medicinal chemistry 20100615

• Hydrogen sulfide attenuates epithelial-mesenchymal transition of human alveolar epithelial cells.

  Pharmacological research 20100401

• Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor.

  Molecular vision 20100101

• Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).

  Bioorganic & medicinal chemistry letters 20090815

• TGF-beta1 induced MMP-9 expression in HNSCC cell lines via Smad/MLCK pathway.

  Biochemical and biophysical research communications 20080711

• The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis.

  Gastroenterology 20080601

• TGF-beta signaling promotes survival and repair in rat alveolar epithelial type 2 cells during recovery after hyperoxic injury.

  American journal of physiology. Lung cellular and molecular physiology 20080401

• Synthesis and biological evaluation of 5-(pyridin-2-yl)thiazoles as transforming growth factor-beta type1 receptor kinase inhibitors.

  Bioorganic & medicinal chemistry letters 20080315

• The role of maternal Activin-like signals in zebrafish embryos.

  Developmental biology 20070915

• Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

  Journal of medicinal chemistry 20070628

• Time-dependent patterning of the mesoderm and endoderm by Nodal signals in zebrafish.

  BMC developmental biology 20070101

• SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7.

  Molecular pharmacology 20040301