TGF-beta/Smad

Oxymatrine (Oxysophoridine) is an alkaloid isolated from Sophora flavescens, used as the antibiotic.

Ponsegromab (PF 06946860), a humanized anti-GDF15 antibody, may treat cancer cachexia by blocking GDF15/GFRAL signaling.

Isoviolanthin, a flavonoid from Dendrobium Officinale, inhibits migration of TGF-β1-treated HCC cells, non-toxic to normal cells, potential HCC therapy.

Hydrochlorothiazide (HCTZ) 是一种口服有效的噻嗪类的利尿药，可抑制转化 TGF-β/Smad 信号通路。它通过打开钙激活钾 (KCA) 通道发挥直接的血管松弛作用。它改善心脏功能，减少纤维化并具有降压作用。

Garetosmab (REGN 2477), a human IgG4 monoclonal antibody, inhibits activin A for potential cancer treatment and FOP study.

Linavonkibart (SRK181) is a humanized antibody targeting TGFβ1 that blocks the release of TGF-β1 protein by specifically binding latent TGF-β1.

Sotatercept (ACE-011) is an ActRIIA-Fc fusion protein and an inhibitor of activin signaling.

Prafnosbart (DS-6016A) is a humanized IgG1-kappa monoclonal antibody targeting ACVR1 (activin A receptor type 1, ACVRLK2, ALK2, ACVR1A, SKR1), utilized in

Fresolimumab (GC1008) is a human monoclonal antibody targeting active TGFβ1, TGFβ2, TGFβ3, studied for cancer and focal segmental glomerulosclerosis.

<p>SLLK is a control peptide for LSKL.</p>

TGFβRI-IN-7 (compound 16W) is a potent inhibitor of TGFβRI. It effectively inhibits the phosphorylation of SMAD2/3 and reduces the viability of H22 cells, with IC50 values of 12 nM and 65 nM, respectively. In an H22 cell xenograft model, TGFβRI-IN-7 exhibits antitumor efficacy with a TGI of 79.6%.

ALK5-IN-83 (compound 13b) is an ALK5 inhibitor with an IC50 of 0.13 μM. It suppresses TGF-β1-induced Smad2 phosphorylation and cell motility in A549 cells.

Emugrobart is a humanized IgG1κ antibody targeted at GDF8, with HumanIgG1kappa, Isotype Control serving as its corresponding isotype control.

Tubastatin inhibits TGF-β1-induced S6K phosphorylation, HIF-1α expression and VEG F expression.

Rilogrotug is a humanized IgG1κ monoclonal antibody targeting GDF15, with its corresponding isotype control being HumanIgG1kappa, Isotype Control.

Cirevetmab (ZTS-00521426), a caninized monoclonal antibody targeting Canis lupus familiaris TGFB1, is classified as an immunoglobulin G2-kappa.

LSKL TFA (H-Leu-Ser-Lys-Leu-NH2 TFA) is a TGF-尾1 antagonist that inhibits TSP-1 binding to LAP and reduces renal interstitial fibrosis and liver fibrosis.

Lerdelimumab (CAT-152) is an IgG4 monoclonal antibody targeting TGF-β2, used in glaucoma scarring research.

Bintrafusp alfa (M7824) is a protein consisting of the extracellular structural domain of TGF-βRII with a monoclonal antibody to human immunoglobulin G1.

SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.

SRI-011381 hydrochloride, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.

Asiaticoside, in Centella asiatica, may treat wounds/burns.

Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.

(E)-SIS3 (SIS3) is a Smad3 inhibitor (IC50=3 μM) selective.inhibits the differentiation of fibroblasts into myofibroblasts via TGF-β1. High-Quality, Low-Cost!

R-268712 is a potent ALK5 inhibitor with a 2.5 nM IC50, also targeting TGF-β type I receptor orally.

SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway.

LSKL, Inhibitor of Thrombospondin TSP-1 acetate is activation of TGF-β .

Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.

ITD-1 is a potent and highly selective TGFβ pathway inhibitor.

Galunisertib (LY2157299) is a selective TGF-β receptor type I (TGF-βRI) inhibitor. Galunisertib has antitumor activity. Cost-effective and quality-assured.

Alantolactone is a selective inhibitor of STAT3 that induces cancer-associated apoptosis and has antitumor activity.Cost-effective and quality-assured.

BMP signaling agonist sb4 (SB 4) is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)

BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).

BIO-013077-01 is a potent TGFbeta family type I receptors antagonist.

TMANO Dihydrate, from trimethylamine oxidation, stabilizes proteins against sharks' urea.

LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).

SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.

Nisevokitug (anti-TGF-β mAb) neutralizes TGF-β and is being studied for its ability to modulate the immunosuppressive tumor microenvironment.

Ginisortamab (UCB6114) is a fully humanized monoclonal antibody targeting Gremlin-1, IC50=8.2 nM and 9 nM against human and mouse Gremlin-1, respectively.

Metelimumab (CAT-192) is a humanised monoclonal antibody targeting TGFβ1, which can be used to study diffuse systemic sclerosis (d-SSc).

Livmoniplimab (ABBV-151; ARGX-115) is a humanised monoclonal antibody targeting LRRC32 (GARP)/TGFβ1, which blocks TGFβ1 release mediated by LRRC32

Trevogrumab is a human monoclonal antibody that inhibits myostatin (GDF8) to promote muscle growth, and is under research for treating age-related muscle loss (sarcopenia).

Halofuginone (RU-19110) inhibits prolyl-tRNA synthetase (Ki=18.3 nM), down-regulates Smad3, and blocks TGF-β at 10 ng/ml.

Chromenone 1 is a potent potentiator of osteogenic bone morphogenetic protein (BMP).

TGFβRI-IN-1 is an oral active and selective inhibitor of TGFβ receptor type I (TGFβRI) kinase(IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII,

CJJ300 is a TGF-β inhibitor disrupting TGF-β-TβR complex formation, with an IC50 of 5.3 μM, and halts cell migration.

SIS3 free base is a potent and selective Smad3 phosphorylation inhibitor. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.

Halofuginone specifically inhibits collagen type I and MMP-2 gene expression, which may result in the suppression of angiogenesis and tumor cell growth.

<p>SJ000063181 activates BMP signaling (EC50 ≤1μM), usable as probe in zebrafish embryos.</p>

<p>DT-6, a potent TGF-β1 inhibitor, impedes M2 macrophage-induced epithelial-to-mesenchymal transition and the invasive migration of cancer cells, thereby showing</p>

3,7-Dimethylfumarate (3,7-DMF) serves as an oral inhibitor of transforming growth factor-beta 1 (TGF-β1)-mediated hepatic stellate cell (HSC) activation.

TGFβ-IN-5 (WAY-641966) is a potent TGFβ inhibitor with anti-prion activity for the study of fibroproliferative diseases associated with TGF-β signaling.

Myristoyl Tetrapeptide-12 activates SMAD2 and facilitates the association of SMAD3 with DNA, promoting eyelash hair growth [1] [2].

TP0427736: ALK5 inhibitor, IC50=2.72 nM, 300x > ALK3 selectivity; counters TGF-β in human cells, extends anagen in mice.

Kartogenin (KGN) sodium acts as an inducer of chondrogenic tissue formation (EC 50: 100 nM). It promotes chondrogenesis by binding to fibrin A, disrupting its interaction with the transcription factor core binding factor beta subunit (CBFβ), and modulating the CBFβ-RUNX1 transcriptional program. Additionally, Kartogenin sodium aids tendon-bone junction (TBJ) wound healing by stimulating collagen synthesis. It is extensively utilized in cell-free therapies for cartilage regeneration and protection, tendon-bone healing, wound healing, and limb development. The compound is also vital for cartilage repair, coordinating limb development, and osteoarthritis (OA) research [1] [2] [3] [4].

(+)-ITD-1 is an inhibitor of TGF-β, effectively inhibiting TGF-β2 with an IC50 of 0.46 μM. It promotes the degradation of the TGF-β type II receptor (TGFBR2) and the differentiation of cardiomyocytes. Additionally, it suppresses the formation of the mesoderm during the early differentiation of mouse embryonic stem cells (mESCs).

<p>CDD-1431 is a highly selective BMPR2 kinase inhibitor with a Kiapp of 20.6 nM. It inhibits BRE reporter gene activity, exhibiting an IC50 of 4.87 μM. BMPs regulate cellular processes across various tissue types such as the kidneys, skeletal muscle, heart, and reproductive organs, and can induce ectopic bone formation.</p>

TGFβ1-IN-1 is a TGF-β1 inhibitor that inhibits the production of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in cancer research.

TGFβRI-IN-3 inhibits TGFβR1 with an IC 50 of 0.79 nM with 2000-fold selectivity against MAP4K4.

Luspatercept (ACE-536), a recombinant modified ActRIIB fusion protein, selectively binds to transforming growth factor β superfamily ligands, thereby enhancing erythrocyte production and advancing the maturation of erythroid precursors. Moreover, by binding with GDF11, it inhibits Smad2/3 signaling. This compound is instrumental in anemia research [1].

<p>DCN1-IN-2, a DCN1 inhibitor, exhibits potent activity with an IC 50 of 2.96 nM. It effectively mitigates Ang II/TGFβ-induced activation of cardiac fibroblasts and diminishes ISO-induced cardiac fibrosis and remodeling in mice through the selective inhibition of cullin 3.</p>