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TGF-β/Smad Inhibitors

TGF-β/Smad inhibitors block transforming growth factor beta (TGF-β) signaling at its receptor kinases or Smad proteins. TGF-β binds a type II receptor kinase, which then phosphorylates the type I receptor, activin receptor-like kinase 5 (ALK5). The activated type I receptor phosphorylates Smad2 and Smad3, which join Smad4 and move into the nucleus to regulate transcription. SB 431542 and A 83-01 inhibit ALK5 together with the related receptors ALK4 and ALK7. RepSox and galunisertib also target the TGF-β type I receptor, while SIS3 blocks Smad3 downstream. LDN193189 instead inhibits ALK2 and ALK3, type I receptors for bone morphogenetic proteins.

Cat. No.

A24705

CAS No.

2347517-69-3

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine functions as a dual-target PROTAC, effectively inducing ubiquitination and degradation of Smad3 while simultaneously enhancing HIF-α protein levels. This compound exhibits multi-pathway anti-fibrotic activity and renal protective properties, making it valuable for research on renal anemia. Additionally, it has potential applications in studying prostate cancer and other malignancies, contributing to a deeper understanding of cancer biology and treatment modalities.

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1 mg

$70.00

5 mg

$215.00

All 6 sizes

TGF-β/Smad Inhibitors

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine