SB-525334

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SB-525334

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Cat No: 16281

Biochemicals - Kinase Inhibitors

SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM).{27599} It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.{27599} SB-525334 blocks TGF-β1-induced phosphorylation and n...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

6-[2-(1,1-dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]-quinoxaline

Correlated keywords:

SB525334 SB-525334 TGF? RI kinase inhibitor VIII TGF ? potent ATP-competitive receptor TbR-I/ALK5 TbR-I ALK5 TbRI ALK-5 ALK 5 TbR I transforming growths factor-? TGF-?RI factors TGF?RI TGF ?RI cell-permeable quinoxalines compound cell permeable ATPs competitive TGF-b types Smad2/3 activation Smad2 Smad3 Smad-2 Smad-3 2 3 Smad nuclear localization TGF-b1-dependent p3TP-luciferase luciferase p3TP ARE-luciferase transcription ARE CTR-IB CTP IB CTPIB COL1A1 procollagen ?1 and PAI-1 PAI1 PAI 1 plasminogen activator inhibitor-1 T?R-I mRNA expression kidney cells bleomycin-induced pulmonary fibrosis bleomycin renal proximal tubule biochemistry intracellular signaling signal transduction biochemical cancer hypertension translocation gene

Product Overview:
SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM).{27599} It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.{27599} SB-525334 blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression.{27599} It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.{27599,27600,27601} SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.{27601,27602,27603}

Size	1 mg
Shipping	dry ice
CAS Number	356559-20-1
Molecular Formula	C₂₁H₂₁N₅
SMILES	CC(C)(C)C(N1)=NC(C2=CC=CC(C)=N2)=C1C(C=C3)=CC4=C3N=CC=N4
Molecular Weight	343,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.29
UNSPSC code	12352100

Technical File

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.