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SB-505124

Cat. No. M2550
SB-505124 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 120 In stock
50mg USD 430 In stock
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Quality Control
Biological Activity

SB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively). SB-505124 also blocks more complex endpoints of TGF-beta action, as evidenced by its ability to abrogate cell death caused by TGF-beta1 treatment. SB-505124 is three to five times more potent than a related ALK5 inhibitor described previously, SB-431542.

Customer Product Validations & Biological Datas
Source Arthritis Res Ther (2017). Figure 1. SB-505124
Method Western Blot
Cell Lines Primary bovine chondrocytes
Concentrations 5 μM
Incubation Time 1 h
Results Subsequently, we analyzed the effects of the ALK4/5/7-kinase inhibitor SB-505124, the ALK1/2/3-kinase inhibitor LDN-193189 and the TAK1-kinase inhibitor (5Z)-7-Oxozeaenol on TGFβ1-induced R-Smad phosphorylation
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 335.4
Formula C20H21N3O2
CAS Number 694433-59-5
Purity >99%
Solubility DMSO 60 mg/mL
Ethanol 60 mg/mL
Storage at -20°C
References

SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7.
DaCosta Byfield S, et al. Mol Pharmacol. 2004 Mar;65(3):744-52. PMID: 14978253.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB-505124 supplier, TGF-beta/Smad, inhibitors

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