tgfbeta/smad

A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12 45 7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

Trimethylamine N-oxide (TMAO) is a colorless amine oxide produced from choline, betaine, and carnitine via intestinal microbial metabolism that accumulates in tissues of marine animals and prevents the protein-damaging effects of urea.Trimethylamine N-oxide induces inflammation through activation of ROS NLRP3 inflammasomes, which can induce fibroblast differentiation and cardiac fibrosis.

Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.

Galunisertib (LY2157299) is a TGF-β receptor type I (TGF-βRI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.

Pirfenidone (AMR69) inhibits the production of CCL2 and CCL12 in fibroblasts and also decreases TGF-β2 protein levels. Pirfenidone is an antifibrotic agent that is commonly used in studies related to pulmonary fibrosis and also has anti-inflammatory activity.

LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8 0.8 5.3 16.7 nM for ALK1 2 3 6).

RepSox (ALK5 Inhibitor II) is a TGFβR-1 ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23 4 nM). RepSox induces adipogenesis in MEFs cells.

SB-431542 is an inhibitor of ALK5 TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.

Monocrotaline (Crotaline) is a pyrrolizidine alkaloid extracted from the seeds of the Crotalaria plant. Monocrotaline has certain cellular activity against HepG2 cells and can induce pulmonary hypertension in rodents.

Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.

Trimethylamine N-oxide dihydrate (TMANO Dihydrate), a product of the oxidation of trimethylamine, is considered as a protein stabilizer that may serve to counteract urea, the major osmolyte of sharks, skates and rays.

LDN-212854 (BMP Inhibitor III), a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versus ALK1 3 compared to other inhibitors.

BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.

Hydroxysafflor yellow A (Safflomin A) inhibits adipogenesis by increasing HSL promoter activities, effectively protects the liver from long-term alcohol injury by enhancing antioxidant capacity and inhibiting the expression of TGF-β, prevents steroid-induced avascular necrosis of the femoral head by inhibiting primary bone marrow-derived mesenchymal stromal cells, and exhibits anti-tumor effects.

Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.

DT-6, a potent TGF-β1 inhibitor, impedes M2 macrophage-induced epithelial-to-mesenchymal transition and the invasive migration of cancer cells, thereby showing potential for cancer research applications [1].

Ponsegromab (PF 06946860) is a selective and effective humanized anti-GDF15 antibody inhibitor with anti-cachexic activity. It binds to GDF15, preventing its interaction with GFRAL and disrupting GDF15 GFRAL mediated signaling. Ponsegromab has potential anticancer activity and can be used to treat cancer patients with cancer anorexia cachexia syndrome.

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

ML347 (LDN 193719)(DN193719) is a highly specific ALK1 2 inhibitor ( IC50: 46 32 nM), and the selectivity for ALK2 is >300-fold than ALK3.

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

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. By inducing antioxidant gene expression and scavenging reactive oxygen species (ROS), 3,7-DMF is useful for researching liver fibrosis [1].

Nisevokitug (NIS-793) is an IgG2λ human monoclonal antibody that targets TGF-β (TGFB1 TGFB2). It is produced in CHO-K1 cells [1].

CIB-L43 is an orally active TRBP inhibitor (KD = 4.78 nM) that disrupts the TRBP-dicer interaction (IC50 = 2.34 μM). It suppresses the biosynthesis of oncogenic miR-21, elevates PTEN and Smad7 expression, and inhibits AKT and TGF-β signaling, thereby reducing the proliferation and migration of HCC cells.

NOX4-IN-1 (Compound 14m) is an inhibitor of NADPH oxidase 4 (NOX4) that reduces the production of reactive oxygen species (ROS). It also inhibits the TGF-β1 Smad signaling pathway, leading to decreased expression of fibrosis-related proteins. Additionally, NOX4-IN-1 impedes the migration of NRK-49F cells.