2. TGF-beta/Smad
  3. TGF-β Receptor
  4. GW788388

GW788388 

Cat. No.: HY-10326 Purity: 99.92%
COA 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 (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 87 In-stock
Solid
5 mg USD 79 In-stock
10 mg USD 119 In-stock
50 mg USD 343 In-stock
100 mg USD 515 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

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

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

    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.

    View All TGF-β Receptor Isoform Specific Products:

    View All Isoforms
    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 ACVR2A ACVR2B

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    425.48

    Appearance

    Solid

    Formula

    C25H23N5O2
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (58.76 mM; Need ultrasonic)

    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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.92%

    COA (249 KB)

    Handling Instructions (2659 KB)
    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
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    × = ×
    C1   V1   C2   V2

    Keywords:

    GW788388452342-67-5GW 788388GW-788388TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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