TGF-β Receptor Inhibitor

TGF-β Receptor Inhibitors (108):

Cat. No.	Product Name	Effect	Purity

HY-13226

Galunisertib	Inhibitor	99.95%
Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC₅₀ of 56 nM.

HY-12273

DMH-1	Inhibitor	99.95%
DMH-1 is a potent and selective BMP inhibitor with IC₅₀s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.

HY-12043

SB 525334	Inhibitor	99.97%
SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC₅₀ of 14.3 nM.

HY-12075

LY2109761	Inhibitor	99.72%
LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with K_is of 38 nM and 300 nM, respectively.

HY-12071B

LDN-193189 dihydrochloride	Inhibitor	99.75%
LDN-193189 (dihydrochloride) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC₅₀ values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.

HY-P991254

VPI-2690B	Inhibitor
VPI-2690B is a human monoclonal antibody (mAb) targeting Integrin aVb3. VPI-2690B inhibits TGF-β signaling. VPI-2690B can be used in Diabetic nephropathies research.

HY-178191

SGC stimulator 1	Inhibitor
sGC stimulator 1 is a carbonyl sulfide (COS)/H₂S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC₅₀ = 496 nM). sGC stimulator 1 exhibits a well-characterized H₂S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H₂S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H₂S. sGC stimulator 1 can be used for the study of heart failure (HF).

HY-13521

SB-505124	Inhibitor	99.73%
SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC₅₀s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

HY-13462

LY-364947	Inhibitor	99.14%
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC₅₀ of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.

HY-13227

SD-208	Inhibitor	99.87%
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC₅₀ of 48 nM, and > 100-fold selectivity over TGF-βRII.

HY-10326

GW788388	Inhibitor	99.92%
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.

HY-12278

K02288	Inhibitor	99.65%
K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC₅₀s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC₅₀s of of 5-34 nM.

HY-N1472

Levistolide A	Inhibitor	99.34%
Levistolide A is an apoptosis inducer and a PEDV virus inhibitor. Levistolide A can induce apoptosis in colon cancer cells and suppress the replication of porcine epidemic diarrhea virus (PEDV) by promoting ROS generation. Levistolide A activates peroxisome proliferator-activated receptor γ (PPARγ) in N2a/APP695swe cells and reduces excessive phosphorylation of tau through the GSK3α/β pathway, improving symptoms in Alzheimer’s mice. Levistolide A improves kidney damage in 5/6 nephrectomy (Nx) mice by inhibiting the RAS,TGF-β1/Smad, and MAPK pathways.

HY-P99632

Garetosmab	Inhibitor	99.57%
Garetosmab (REGN 2477) is a fully human IgG4 monoclonal antibody that specifically inhibits activin A. Garetosmab can be used for fibrodysplasia ossificans progressiva (FOP) research.

HY-12704

ITD-1	Inhibitor	99.41%
ITD-1 is the first selective TGFβ receptor inhibitor with an IC₅₀ of 460 nM.

HY-P99590A

Sotatercept (mIgG2a)	Inhibitor	99.93%
Sotatercept (mIgG2a) (RAP-011), the murine homolog of Sotatercept (ACE-011) (HY-P99590), is a soluble activin receptor type IIA (ActRIIA) ligand trap. Sotatercept (mIgG2a) inhibits the binding of activin A and other members of the TGF-β superfamily (such as Activin A/B, GDF11 and BMP9/10) to their receptors by combining and neutralizing them, thereby regulating cell proliferation and differentiation. Sotatercept (mIgG2a) mainly inhibits the SMAD2/3 signaling pathway, and can be used in various diseases such as chronic kidney disease. Sotatercept (mIgG2a) reduces the expression of erythropoietic hepcidin (ERFE), regulates iron metabolism, and promotes red blood cell production. Sotatercept (mIgG2a) has a dual effect of promoting bone formation (anabolic) and inhibiting bone resorption (catabolic).

HY-103021

LY3200882	Inhibitor	99.87%
LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC₅₀ of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.

HY-151427

TGFβ1-IN-1	Inhibitor	99.47%
TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies.

HY-136244

PF-06952229	Inhibitor	99.92%
PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.?PF-06952229 is a promising antineoplastic?agent for the study solid tumors, especifically metastatic breast cancer.

HY-13012G

RepSox (GMP)	Inhibitor
RepSox (E-616452) (GMP) is a RepSox (HY-13012) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RepSox is a potent and selective TGF-β-RI/ALK5 inhibitor.

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