An inhibitor of ALK5 (TGFBR1)
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GW 788388

Item No. 16255

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide
CAS Number
452342-67-5
Molecular Formula
C25H23N5O2
Formula Weight
425.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
261 nm
SMILES
O=C(C1=CC=C(C2=NC=CC(C3=CNN=C3C4=CC=CC=N4)=C2)C=C1)NC5CCOCC5
InChi Code
InChI=1S/C25H23N5O2/c31-25(29-20-9-13-32-14-10-20)18-6-4-17(5-7-18)23-15-19(8-12-27-23)21-16-28-30-24(21)22-3-1-2-11-26-22/h1-8,11-12,15-16,20H,9-10,13-14H2,(H,28,30)(H,29,31)
InChi Key
SAGZIBJAQGBRQA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $63

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).1 It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.1 As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.2,3,4 GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.5 Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gellibert, F., de Gouville, A.C., Woolven, J., et al. Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): A potent, selective, and orally active transforming growth factor-β type I receptor inhibitor. J. Med. Chem. 49, 2210-2221 (2006).

    2. Lagares, D., García-Fernández, R.A., Jiménez, C.L., et al. Endothelin 1 contributes to the effect of transforming growth factor β1 on wound repair and skin fibrosis. Arthritis Rheum. 62(3), 878-889 (2010).

    3. Tan, S.M., Zhang, Y., Connelly, K.A., et al. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am. J. Physiol. Heart Circ. Physiol. 298(5), H1415-H1425 (2010).

    4. de Oliveira, F.L., Araújo-Jorge, T.C., de Souza, E.M., et al. Oral administration of GW788388, an inhibitor of transforming growth factorβsignaling, prevents heart fibrosis in Chagas disease. PLoS Negl. Trop. Dis. 6(6), 1-14 (2012).

    5. Noma, K., Smalley, K.S.M., Lioni, M., et al. The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis. Gastroenterology 134(7), 1981-1993 (2008).

    6. Frazier, K., Thomas, R., Scicchitano, M., et al. Inhibition of ALK5 signaling induces physeal dysplasia in rats. Toxicol. Pathol. 35(2), 284-295 (2014).