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SB431542

Cat. No. M1794
SB431542 Structure
Synonym:

SB-431542

Size Price Availability Quantity
10mg USD 85 In stock
50mg USD 335 In stock
100mg USD 610 In stock
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Quality Control
Biological Activity

SB 431542 is a potent and selective inhibitor of the TGF-β1 receptor ALK5 with an IC50 of 94 nM, and its relatives ALK4 and ALK7. It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested. SB 431542 specifically blocks Smad signaling, reducing gene expression relevant to fibrosis and cancer. Suppresses TGF-β-induced proliferation of human osteosarcoma cells.

Protocol
Cell Experiment
Cell lines human DCs
Preparation method Effects of SB-431542 on murine BM-DCs and human DCs. DCs were incubated in 96-well plates (5x104 cells/200 μl/well) with SB-431542 or vehicle alone and LPS in the presence of LPS at different concentrations in triplicates, and then examined for expression of co-stimulatory molecules using FACSCalibur. After 24 h of incubation, the cells were examined for surface expression of CD86 or CD83 within the CD11c+ populations, and the supernatants were tested for cytokine production by enzyme-linked immunosorbent assay (ELISA). Following 24 h of incubation with a test drug, BM-DCs were incubated for 10 min with 5 mg/ml of fluorescein isothiocyanate (FITC)-conjugated dextran (DX) (70,000 Dalton molecular weight, Sigma) at 4˚C or 37˚C, washed extensively, and then examined for FITC signals by CD11c+ cells. After drug pretreatment, BM-DC preparations (derived from BALB/c mice) were washed 3 times and then co-cultured in 96 round-bottom well plates at 4 different cell densities (0.3-10x103 cells/well) with splenic T cells purified from C57BL/6 mice (5x104 cells/well). The magnitude of T cell proliferation was assessed by 3H-thymidine uptake on day 4. Human DC cultures derived from PBMCs were examined for surface phenotype within the CD11c+ population and cytokine production by ELISA as well as for allogeneic mixed lymphocyte reaction.
Concentrations 0~10 μM
Incubation time 24 hr
Animal Experiment
Animal models BALB/c mice received intraperitoneal (i.p.) injections of colon-26 tumor cells
Formulation normal saline
Dosages 1 μM (100μL)
Administration directly injected into peritoneal cavity
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 384.39
Formula C22H16N4O3
CAS Number 301836-41-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

Differential signalling through ALK-1 and ALK-5 regulates leptin expression in mesenchymal stem cells.
Zeddou M, et al. Stem Cells Dev. 2012 Jul 20;21(11):1948-55. PMID: 22087763.

Activation of the activin A-ALK-Smad pathway in systemic sclerosis.
Takagi K, et al. J Autoimmun. 2011 May;36(3-4):181-8. PMID: 21377836.

Transforming growth factor β1 down-regulates Runx-2 and alkaline phosphatase activity of human dental pulp cells via ALK5/Smad2/3 signaling.
Lin PS, et al. Oral Surg Oral Med Oral Pathol Oral Radiol Endod. 2011 Mar;111(3):394-400. PMID: 21236710.

Transforming growth factor β signaling inhibitor, SB-431542, induces maturation of dendritic cells and enhances anti-tumor activity.
Tanaka H, et al. Oncol Rep. 2010 Dec;24(6):1637-43. PMID: 21042762.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB431542, SB-431542 supplier, ALK, inhibitors

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