TGF-beta/Smad

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

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

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

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,

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

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

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

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

<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>

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.

<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.

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).

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>