SB 431542 Inhibitor CAS No. 301836-41-9

Cat. No.	Name	Size	Price
KI0136	SB 431542	10 mg	$270
	SB 431542	50 mg	$752
	SB 431542	200 mg	$2032

Chemical Characteristic

Product Name	SB 431542
CAS No.	301836-41-9
Molecular Weight	384.39
Formula	C₂₂H₁₆N₄O₃
Chemical Name	4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide
Smiles	C(=O)(c1ccc(cc1)c1nc(c([nH]1)c1ccccn1)c1cc2OCOc2cc1)N
Chemical Structure

Biological activities

SB-431542 is a novel, small molecule ATP-mimetic inhibitor of the kinase activity associated with members of the activin receptor-like kinase (ALK) family-specifically ALK5 (TGF- β type I receptor, TGF- β RI), ALK4 (activin type I receptor), and ALK7 (nodal type I receptor). SB-431542 inhibits ALK5 and ALK4 with IC50s of 94 and 140 nM, respectively. SB-431542 as a potent inhibitor of ALK5 shows greater than 100-fold selectivity against p38 mitogen-activated protein kinase (MAPK) and 25 other kinases, and has no effect on the kinase activity of ALK2. SB-431542 is an excellent tool to evaluate the role of TGF-b and ALK5 in cellular mechanisms. SB-431542 at a concentration of 1 µM significantly reduces the TGF- β1??nduced nuclear accumulation of smad proteins, and the IC50 for inhibiting TGF- β1??nduced nuclear fluorescence is approximately 50 nM. SB-431542 also inhibits TGF- β1??nduced collagen Ia1 and PAI-1 mRNA with IC50s of 60 and 50 nM, respectively. In addition, SB-431542 inhibits TGF- β1-induced fibronectin mRNA and protein with IC50s of 62 and 22 nM, respectively.^[1] SB-431542 inhibits TGF- β - and activin-induced phosphorylation of Smad2, which is mediated by ALK5 and ALK4, respectively, but not BMP-induced phosphorylation of Smad1, which is mediated by ALKs 2, 3, and 6.^[2] Moreover, SB-431542 blocks the phosphorylation and nuclear translocation of the SMADs, intracellular mediators of TGF-b signaling, with decreased TGF- β -mediated transcription. SB-431542 treatment of glioma cultures inhibits proliferation, TGF- β -mediated morphologic changes, and cellular motility. Treatment of glioma cultures with SB-431542 blocks activation of the TGF- β pathway and expression of important effectors of the TGF- β -mediated phenotype. ^[3]

Protocols

SB-431542 is dissolved at a concentration of 10 mM in DMSO. ^[1]

References

[1] Laping NJ, et al. Inhibition of transforming growth factor (TGF)-b1-induced extracellular matrix with a novel inhibitor of the TGF-b type I receptor kinase activity: SB-431542. Mol Pharmacol. 2002, 62(1): 58-64. [2] Inman GJ, et al. SB-431542 is a potent and specificinhibitor of transforming growth factor-b superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmcol. 2002, 62(1): 65-74. [3] Hjelmeland MD, et al. SB-431542, a small molecule transforming growth factor-b-receptor antagonist,inhibits human gliomacell line proliferation and motility. Mol Cancer Ther. 2004, 3(6): 737-745. [4] Mahmood A, et al. Enhanced differentiation of human embryonic stem cells to mesenchymal progenitors by inhibition of TGF-beta/activin/nodal signaling using SB-431542. J Bone Miner Res. 2010, 25(6): 1216-1233.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com