ACTR-IA Inhibitors
ACTR-IA inhibitors are a class of chemical compounds that target the activin receptor type IA (ACTR-IA), a transmembrane serine/threonine kinase receptor. ACTR-IA is part of the transforming growth factor-beta (TGF-β) superfamily, specifically involved in mediating signaling pathways for activins and other related ligands. These signaling pathways are crucial for regulating various cellular processes such as proliferation, differentiation, apoptosis, and homeostasis in different tissues. By inhibiting ACTR-IA, these compounds interfere with the receptor's ability to propagate signals from activin ligands to downstream intracellular pathways, disrupting key biological processes controlled by the TGF-β signaling network.
The mechanism of ACTR-IA inhibitors typically involves binding to the receptor's kinase domain, preventing its phosphorylation and subsequent activation of downstream signaling molecules like SMAD proteins. This blockade stops the transmission of signals that normally lead to gene expression changes in response to activin and related ligands. ACTR-IA inhibitors can also act by obstructing the ligand-receptor interaction, making it difficult for activins to bind and activate the receptor. These inhibitors are essential tools for studying the functional roles of ACTR-IA in cellular signaling and its contribution to processes like tissue development, cell cycle regulation, and immune responses. By blocking the signaling cascade initiated by ACTR-IA, researchers can gain insights into the intricate network of cellular communications governed by the TGF-β superfamily and the specific impact of activin receptor activity on physiological and developmental outcomes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
SB 431542 | 301836-41-9 | sc-204265 sc-204265A sc-204265B | 1 mg 10 mg 25 mg | $82.00 $216.00 $416.00 | 48 | |
SB 431542 selectively targets ALK5, ALK4, and ALK7 kinase activity, which could lead to a downregulation of ACTR-IA expression by disrupting the autocrine loop of TGF-beta signaling essential for maintaining ACVR1 gene transcription. | ||||||
4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline | 1062368-24-4 | sc-476297 | 5 mg | $240.00 | ||
As a potent antagonist of ALK2 and ALK3, 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline could decrease ACTR-IA expression levels by hindering the bone morphogenetic protein (BMP) signaling, which shares downstream effectors with ACVR1, including SMAD proteins. | ||||||
BML-275 | 866405-64-3 | sc-200689 sc-200689A | 5 mg 25 mg | $96.00 $355.00 | 69 | |
BML-275 blocks BMP signaling by inhibiting BMP type I receptors, which could lead to a decrease in ACTR-IA expression by attenuating the phosphorylation of SMAD1/5/8, molecules shown to be essential for the transcriptional activity of ACVR1. | ||||||
DMH-1 | 1206711-16-1 | sc-361171 sc-361171B sc-361171A sc-361171C | 10 mg 25 mg 50 mg 100 mg | $213.00 $318.00 $632.00 $1047.00 | 2 | |
DMH-1 preferentially targets ALK2, potentially leading to a reduction in ACTR-IA expression by interfering with the BMP signaling pathway and the subsequent nuclear translocation of SMAD1/5/8, which can promote ACVR1-related gene expression. | ||||||
A 83-01 | 909910-43-6 | sc-203791 sc-203791A | 10 mg 50 mg | $202.00 $811.00 | 16 | |
A 83-01 can disrupt signaling processes by inhibiting ALK5, ALK4, and ALK7, potentially leading to a reduced expression of ACTR-IA, as these kinases are part of the signaling cascade that converges on the transcription factors regulating ACVR1 gene expression. | ||||||
LY 364947 | 396129-53-6 | sc-203122 sc-203122A | 5 mg 10 mg | $107.00 $156.00 | 4 | |
LY 364947 is an inhibitor targeting ALK5, which could reduce ACTR-IA expression by preventing the phosphorylation and activation of SMAD2/3 proteins, thereby disrupting the transcriptional responses typically upregulated by TGF-beta signaling. | ||||||
TGF-β RI Kinase Inhibitor V | 627536-09-8 | sc-203294 | 2 mg | $88.00 | 3 | |
SD-208, by inhibiting TGF-beta receptor I kinase, could decrease ACTR-IA levels by blocking the SMAD-dependent transcription that is initiated by TGF-beta signaling and known to enhance ACVR1 gene expression. | ||||||
EW-7197 | 1352608-82-2 | sc-507465 | 5 mg | $345.00 | ||
EW-7197 prevents the kinase activity of ALK5, which could lead to a decrease in ACTR-IA expression by intervening in the autocrine secretion of TGF-beta ligands, thereby reducing the signal transduction necessary for ACVR1 mRNA synthesis. | ||||||
ALK5 Inhibitor II | 446859-33-2 | sc-221234 sc-221234A sc-221234B sc-221234C sc-221234D sc-221234E sc-221234F | 1 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 g | $77.00 $153.00 $219.00 $663.00 $1248.00 $4382.00 $7850.00 | 8 | |
ALK5 Inhibitor II inhibits ALK5, which could lead to decreased ACTR-IA expression by attenuating the TGF-beta-induced phosphorylation events required for the stabilization of ACVR1 mRNA and its translation efficiency. | ||||||
LY2157299 | 700874-72-2 | sc-391123 sc-391123A | 5 mg 10 mg | $213.00 $359.00 | 3 | |
LY2157299 targets TGF-beta receptor I (ALK5), potentially leading to reduced ACTR-IA expression by diminishing the transcriptional activation of genes downstream of the TGF-beta/SMAD pathway, which includes the ACVR1 gene. | ||||||