GW788388

SKU: orb1307416

Description

GW788388 is a potent small molecule inhibitor primarily targeting ALK5 (TGF-β type I receptor), with additional activity against TGF-β type II and activin type II receptors. It is widely used in biochemical and cellular assays to study TGF-β and activin signaling pathways in fibrosis, cancer, and cardiovascular disease research, both in vitro and in vivo.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 452342-67-5
• MW: 425.48
• Purity: 99.58% (May vary between batches)
• Formula: C₂₅H₂₃N₅O₂
• SMILES: O=C(NC1CCOCC1)c1ccc(cc1)-c1cc(ccn1)-c1c[nH]nc1-c1ccccn1
• Target: TGF-beta/Smad,ALK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.35 mM);DMSO:10 mg/mL (23.5 mM)

Bioactivity

• Target IC50:
  ALK5:18 nM
• In Vivo:
  GW788388 effectively inhibits ALK5, ALK4, ALK7, and TGF-β-regulated growth. In cellular assays (IC50=93 nM), it demonstrates an inhibition of TGF-β-induced Smad activation and suppresses the expression of target genes.
• In Vitro:
  In a model of kidney fibrosis induced by puromycin aminonucleoside, GW788388 (10 mg/kg) was shown to induce the expression of collagen A1 mRNA. In rodents with advanced diabetic nephropathy, GW788388 reduced fibrotic responses by diminishing TGF-β signaling. Furthermore, in a mouse model of myocardial infarction, treatment with GW788388 significantly inhibited contractile function, reduced cardiac hypertrophy, and decreased levels of activated Smad2 and α-SMA.
• Cell Research:
  Cell viability/proliferation assays are done according to the manufactures instructions (CellTiter 96 Aqueous One Solution Cell Proliferation Assay). Viability and proliferation are measured after 72 hours GW788388 treatment in the presence or absence of TGF-β.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ALK5, inhibit, GW788388, GW-788388, GW 788388, Inhibitor, Smad, TGFβ, TGF-β Receptor, TGF-β/Smad, TGF-beta, TGFbeta/Smad, TGF-b/Smad, TGFbeta, TGFb, Transforming growth factor beta receptors

Compound Identifiers

PubChem CID

10202642