An ALK5 and ALK4 inhibitor
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Alternative(s)
11793SB-505124
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SB-505124 (hydrochloride)

Item No. 42056

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-(1,3-benzodioxol-5-yl)-2-(1,1-dimethylethyl)-1H-imidazol-5-yl]-6-methyl-pyridine, monohydrochloride
CAS Number
356559-13-2
Synonyms
  • TGF-β Receptor Type I Kinase Inhibitor III
  • TGF-β RI Kinase Inhibitor III
Molecular Formula
C20H21N3O2 • HCl
Formula Weight
371.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/ml
SMILES
CC1=NC(C2=C(C3=CC(OCO4)=C4C=C3)NC(C(C)(C)C)=N2)=CC=C1.Cl
InChi Code
InChI=1S/C20H21N3O2.ClH/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15;/h5-10H,11H2,1-4H3,(H,22,23);1H
InChi Key
BTUOOXPZOVNPMF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    SB-505124 is an inhibitor of activin receptor-like kinase 5 (ALK5), also known as TGF-β receptor type 1 (TGF-βRI), and ALK4 (IC50s = 47 and 129 nM, respectively).1 It is selective for ALK5 and ALK4 over a panel of 27 kinases at 10 µM. SB-505124 (5 µM) also inhibits ALK7-induced increases in phosphorylated SMAD2 levels in COS-1 cells overexpressing ALK7. It inhibits TGF-β-induced but not TNF-α-induced apoptosis in Fao hepatocellular carcinoma cells when used at a concentration of 1 µM. SB-505124 (5 mg/eye) decreases intraocular pressure (IOP) and subconjunctival immune cell infiltration in a rabbit model of trabeculectomy.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. DaCosta Byfield, S., Major, C., Laping, N.J., et al. SB-505124 is a selective inhibitor of transforming growth factor- ß type I receptors ALK4, ALK5, and ALK7. Mol. Pharmacol. 65(3), 744-752 (2004).

    2. Sapitro, J., Dunmire, J.J., Scott, S.E., et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor. Mol. Vis. 16, 1880-1892 (2010).