1. TGF-beta/Smad
  2. TGF-β Receptor

GW788388 

Cat. No.: HY-10326 Purity: 99.84%
Handling Instructions

GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.

For research use only. We do not sell to patients.

GW788388 Chemical Structure

GW788388 Chemical Structure

CAS No. : 452342-67-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 312 In-stock
Estimated Time of Arrival: December 31
100 mg USD 468 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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    GW788388 purchased from MCE. Usage Cited in: Org Lett. 2017 Jan 6;19(1):286-289.

    Compounds 1−4 inhibit fibrogenic action of TGF-β1 in rat renal proximal tubular cells. Cell lysates after treatments as indicated are immunoblotted with antibodies against fibronecitn, collagen I, α-SMA, and α-tubulin. GW: GW788388.

    GW788388 purchased from MCE. Usage Cited in: Org Lett. 2017 Jan 6;19(1):286-289.

    Cell lysates after various treatments are immunoblotted with antibodies against phosphorylated Smad2, phosphorylated Smad3, total Smad2/3, and β-actin. GW: GW788388.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.

    IC50 & Target

    IC50: 18 nM (ALK5)

    In Vivo

    GW788388 given orally for 5 weeks significantly reduces renal fibrosis and decreased the mRNA levels of key mediators of extracellular matrix deposition in kidneys in db/db mice[1]. GW788388 (50 mg/kg/day, p.o.) significantly attenuates systolic dysfunction in the MI animals, together with the attenuation of the activated (phosphorylated) Smad2 (P < 0.01), α-smooth muscle actin (P < 0.001), and collagen I (P < 0.05) in the noninfarct zone of MI rats[2]. GW788388 reduces the expression of collagen IA1 by 80% at a dose of 1 mg/kg twice a day (b.i.d.). GW788388 significantly reduces the expression of collagen IA1 mRNA when administered orally at 10 mg/kg once a day (u.i.d.) in a model of puromycin aminonucleoside-induced renal fibrosis[3].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 48 mg/mL (112.81 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3503 mL 11.7514 mL 23.5029 mL
    5 mM 0.4701 mL 2.3503 mL 4.7006 mL
    10 mM 0.2350 mL 1.1751 mL 2.3503 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Animal Administration
    [2]

    One week postsurgery, sham-operated (N=6) and infarcted animals (N=10) are randomized to treatment with the ALK5 inhibitor GW788388 (GSK) at a dosage of 50 mg/kg/day by gavage, which has been shown to significantly attenuate collagen overexpression in a rodent model of dimethylnitrosamine-induced liver disease. Untreated rats, that is, sham-operated (N=9) and MI animals (N=15), are gavaged with vehicle (1% carboxymethyl cellulose solution). Four animals with < 25% infarct size as determined postmortem by histology are excluded from further analyses.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    425.48

    Formula

    C₂₅H₂₃N₅O₂

    CAS No.

    452342-67-5

    SMILES

    O=C(C1=CC=C(C=C1)C2=NC=CC(C3=CNN=C3C4=NC=CC=C4)=C2)NC5CCOCC5

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.84%

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    Product Name:
    GW788388
    Cat. No.:
    HY-10326
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    GW788388

    Cat. No.: HY-10326