Inhibitor of receptors ALK4, ALK5, and ALK7
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SB-431542 (hydrate)

Item No. 13031

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]-benzamide, hydrate
Molecular Formula
C22H16N4O3 • XH2O
Formula Weight
384.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 2 mg/ml
λmax
329 nm
SMILES
NC(C(C=C1)=CC=C1C2=NC(C3=CC=C(OCO4)C4=C3)=C(C5=CC=CC=N5)N2)=O.O
InChi Code
InChI=1S/C22H16N4O3.H2O/c23-21(27)13-4-6-14(7-5-13)22-25-19(20(26-22)16-3-1-2-10-24-16)15-8-9-17-18(11-15)29-12-28-17;/h1-11H,12H2,(H2,23,27)(H,25,26);1H2
InChi Key
WQUIJVKNPYBZOF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    SB-431542 is a potent and selective inhibitor of the TGF-β1 receptor ALK5 (IC50 = 94 nM)1. It is a less potent antagonist of ALK4 (IC50 = 140 nM)2 and ALK7.3 It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested.3 SB-431542 specifically blocks Smad signaling, reducing gene expression relevant to fibrosis and cancer.3 Through its effects on ALK/Smad signaling, SB-431542 suppresses renewal in embryonic and induced pluripotent stem cells and promotes their differentiation.4,5 This product is also available as part of Cayman's Stem Cell Expansion Reagent Kit (SCB) (Item No. 502886), Fibroblast Reprogramming Reagent Kit (SB/XAV) (Item No. 502888), and Hepatocyte Maintenance Reagent Kit (Item No. 44676).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Callahan, J.F., Burgess, J.L., Fornwald, J.A., et al. Identification of novel inhibitors of the transforming growth factor ß1 (TGF-ß1) type 1 receptor (ALK5). J. Med. Chem. 45(5), 999-1001 (2002).

    2. Laping, N.J., Grygielko, E., Mathur, A., et al. Inhibition of Transforming Growth Factor (TGF)-ß1-Induced Extracellular Matrix with a Novel Inhibitor of the TGF-ß Type I Receptor Kinase Activity: SB-431542. Mol. Pharmacol. 62(1), 58-64 (2002).

    3. Inman, G.J., Nicolás, F.J., Callahan, J.F., et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol. Pharmacol. 62(1), 65-74 (2002).

    4. James, D., Levine, A.J., Besser, D., et al. TGFß/activin/nodal signaling is necessary for the maintenance of pluripotency in human embryonic stem cells. Development 132, 1273-1282 (2005).

    5. Chambers, S.M., Fasano, C.A., Papapetrou, E.P., et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. Nat. Biotechnol. 27(3), 275-280 (2009).