tgfβ

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.

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.

DMH-1 is a potent and selective Bone Morphogenetic Protein (BMP) inhibitor.

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.

BMT-124110 Formate is a selective AAK1 inhibitor (IC50: 0.9 nM) with anti-injury sensory activity.BMT-124110 Formate inhibits the BMP-2-inducible protein kinase BIKE with an IC50: 17 nM.BMT-124110 Formate inhibits the cell-cycle protein G-related BMT-124110 Formate inhibits the cell cycle protein G-associated kinase GAK with an IC50:99 nM.

AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM. It exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.

Chromenone 1 is a potent potentiator of osteogenic bone morphogenetic protein (BMP). Chromenone 1 induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.

CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 μM, disrupting the TGF-β-TβR-I-TβR-II signaling complex and inhibiting cell migration.

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.

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].

TGFβ-IN-2 (Compound 9d) effectively inhibits TGF-β-induced accumulation of total collagen in NRK-49F cells, with an IC50 value of 4.31 μM. It also suppresses the TGF-β-induced in vitro expression of COL1A1, α-SMA, and p-Smad3. Additionally, TGFβ-IN-2 shows promise as a potential anti-fibrosis compound for in vivo applications through oral administration [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.

Clematichinenoside AR exerts anti-inflammatory and immunosuppressive properties, it has anti-arthritic effects on PI3K Akt signaling pathway and TNF-α± associated with collagen-induced arthritis.