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SB431542

SB431542

Manufacturer	Selleckchem
Category	Oncology Neuroscience Neural Lineage Markers Molecular Targets for Neuroscience Cardiovascular Research Thrombosis & Hemostasis Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Colorectal Cancer Breast Cancer Neurodegeneration Markers;Research Area Targets for Rodent Neurosciences
Type	Inhibitors
Specific against	other
Amount	10 mg
Item no.	S1067-10
Targets	ALK
CASRN	301836-41-9
eClass 6.1	30220300
eClass 9.0	32160605
Available
Administration	Directly injected into peritoneal cavity
Animal Models	BALB/c mice receive intraperitoneal (i.p.) injections of colon-26 tumor cells.
Cell lines	MG63 and NIH3T3
Chemical Name	4-(4-(benzo[d][1, 3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide
Concentrations	0.3 uM
Description	SB 431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM.
Dosages	1 uM solution, 100 uL/mouse
Formulation	DMSO
IC50	94 nM [1], 94 nM [1], 94 nM [1], 94 nM [1], 94 nM [1], 94 nM [1]
In vitro	SB 431542 inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are responsible for the phosphorylation of Smad2. SB 431542 has little effect on ALK1, ALK2, ALK3, and ALK6, which show phosphorylation of Smad1. SB 431542 is a selective inhibitor of endogenous activin but has no apparent effect on BMP signaling. SB 431542 could induce both Smad2/Smad4- and Smad3/Smad4-dependent transcription. [2] In A498 cells, SB 431542 inhibits both TGF-beta1–induced collagen Ialpha1 and PAI-1 mRNA with IC50 of 60 nM and 50 nM, respectively. In addition, SB 431542 inhibits production of TGF-beta1–induced fibronectin mRNA and protein with IC50 of 62 nM and 22 nM, respectively. [3] SB 431542 blocks the TGF-beta–mediated growth factors, including PDGF-A, FGF-2 and HB-EGF, leading to an increase in proliferation of MG63 cells. SB 431542 also inhibits TGF-beta–induced c-Myc and p21 WAF1/CIP1. [4] SB 431542 significantly suppresses TGF-beta–induced G1 arrest, leading to accumulation of cellsphase of the cell cycle in FET, RIE, and Mv1Lu cells. SB 431542 also inhibits TGF-beta-induced epithelial to mesenchymal transition (EMT) in NMuMG and PANC-1 cells. [5] SB 431542 significantly elevates the expression of CD86 in BM-DCs and that of CD83 within CD11c+ cells suppressed by TGF-beta. SB 431542 is able to induce NK activity through functional maturation and IL-12 production of human DCs. [6]
In vivo	SB 431542 triggers cytotoxic T lymphocyte (CTL) activities in the colon-26 carcinoma models and is most likely to produce antitumor immunological outcomes through alteration of DC function suppressed by TGF-beta. [6]
Incubation Time	30 minutes
Kinase Assay	Flashplate assay for ALK5, SB 431542 is dissolved in DMSO at a concentration of 10 mM. The kinase domain of TGFbetaRI, from amino acid 200 to the C-terminus, and the full-length Smad3 protein are expressed as N-terminal glutathion S-transferase (GST) fusion proteins in the baculovirus expression system. Proteins are purified with glutathion Sepharose beads 4B. Basic FlashPlates are coated with 0.1 M sterile filtered sodium bicarbonate, pH 7.6, containing 700 ng of GST-Smad3 per 100 uL. Assay buffer contains 50 mM HEPES (pH 7.4), 5 mM MgCl2, 1 mM CaCl2, 1 mM DTT, 100 mM GTP, 3 uM ATP plus 0.5 uCi/well 33P-ATP, and 85 ng of GST-ALK5 with or without SB 431542. Plates are incubated at 30 C for 3 hours. The assay buffer is removed by aspiration, and the plate is counted on a Packard TopCount 96-well scintillation plate reader.
Method	To explore the effects of ligands, MG63 and NIH3T3 cells are seeded at a density of 8 x 104 cells/well in 6-well plates and starved (0.1% FCS for MG63 cells and 0.5% FCS for NIH3T3 cells) for 24 hours before ligand stimulation. Media containing various ligands are exchanged at 48-hours intervals. Cells are trypsinized and counted by a Coulter counter on days 2, 4, and 6 after ligand stimulation. To explore the effects of constitutively active receptors, cells are seeded at a density of 2 x 105 cells/well in 6-well plates. The next day, cells are infected with adenoviruses carrying various cDNAs at a multiplicity of infection of 100. Cells are trypsinized and counted on day 3. Cell proliferation assay is performed in the presence of 0.3 uM SB 431542.
Molecular Weight (MW)	384, 39
Picture ChemicalStructure Description	SB 431542 Chemical Structure
Picture Description 1	, , Dr Kah-Wai Lin of Karolinska Biomics Center, SB 431542purchased from Selleck, SB431542 inhibit expression of TGF-beta induced pS2 in MvILu cell
Solubility (25C)	DMSO 77 mg/mL, Water <1 mg/mL, Ethanol 45 mg/mL
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

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