1. TGF-beta/Smad
  2. TGF-β Receptor

GW788388 

Cat. No.: HY-10326 Purity: 99.64%
Data Sheet SDS 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 $66 In-stock
5 mg $60 In-stock
10 mg $90 In-stock
50 mg $260 In-stock
100 mg $390 In-stock
200 mg   Get quote  
500 mg   Get quote  

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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].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Animal Administration
[2]

GW788388 is formulated in 1% carboxymethyl cellulose solution.

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

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

Solvent & Solubility

DMSO: ≥ 48 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.64%

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