alk5

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.

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.

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.

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.

ALK5-IN-79 (compound 57), an ALK inhibitor, exhibits anticancer activity by inhibiting the TGF-β1 SMAD signaling pathway. It effectively reduces the production of extracellular matrix (ECM) and collagen deposition. Moreover, ALK5-IN-79 demonstrates satisfactory pharmacokinetic (PK) properties and favorable in vivo tolerance.

ALK5-IN-9 is a potent, orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation (IC50: 25 nM) and inhibits NIH3T3 cell activity (IC50: 74.6 nM). ALK5-IN-9 has shown research potential in cancer diseases.

ALK5-IN-29 is a selective inhibitor of activin receptor-like kinase (ALK).ALK5-IN-29 inhibits activin receptor-like kinase activity (IC50 ≤ 10 nM).AALK5-IN-29 inhibits tumour growth and can be used in the study of proliferative diseases such as cancer.

ALK5-IN-31 is a selective inhibitor of ALK-5 (IC50≤10 nM) and also inhibits TGF-β-induced SMAD signalling.ALK5-IN-31 has the potential to inhibit tumour growth in vivo.ALK5-IN-31 can be used in the study of proliferative diseases (e.g. cancer, fibrotic diseases, systemic sclerosis).

ALK5-IN-6 is a potent inhibitor of ALK5 with potential applications for TGF-β-related diseases and conditions, including tumors, inflammatory diseases, fibrotic diseases, and autoimmune diseases. Transforming growth factor β (TGF-β) is a multifunctional cytokine that regulates cell proliferation, differentiation, and apoptosis through a complex receptor signaling pathway on the cell surface in an autocrine, paracrine, and endocrine manner.

ALK5-IN-8 is a highly effective inhibitor of TGFβRI (ALK5). It hinders the phosphorylation of ALK5 on downstream signaling proteins (Smad2 or Smad3) by obstructing the interaction between TGFβRI and ligands. Consequently, it disrupts or prevents TGF-β signaling. ALK5-IN-8 shows promise in the study of diverse diseases associated with ALK5-mediated pathways[1].

ALK5-IN-30 (EX-07) is a potent inhibitor of ALK, demonstrating inhibitory effects on ALK5 and TGFβ-R1 with IC50 values of less than 10 nM.

ALK5-IN-84 (Compound 23) is an ALK5 inhibitor with a pKi value of 9.35 for hALK5. Administered via inhalation, ALK5-IN-84 exhibits significant ALK5 inhibitory activity. This compound holds potential for research in developing inhalable ALK5 inhibitors.

ALK5-IN-34 is a selective, orally active inhibitor of activin receptor-like kinase (ALK), which inhibits the activity of activin receptor-like kinase (IC50 ≤ 10 nM) and also inhibits tumour growth.

ALK5-IN-82 is a potent and selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating an IC50 value of 9.1 nM. This compound effectively suppresses the expression of α-smooth muscle actin (α-SMA), collagen I, and the proteinases tissue inhibitor of metalloproteinase 1 (TIMP-1) and matrix metalloproteinase 13 (MMP-13) in human umbilical vein endothelial cells induced by transforming growth factor-β. ALK5-IN-82 shows potential for use in research related to cardiac fibrosis.

ALK5-IN-33 (Compound EX-10) is an orally active and selective inhibitor of ALK-5 with an IC50 ≤ 10 nM.

ALK5 Inhibitor II is an ALK5 inhibitor. IC50: 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively.

ALK5-IN-28 is a selective inhibitor of ALK-5 with an IC50 ≤ 10 nM that inhibits TGF-β-induced SMAD signalling.ALK5-IN-28 has the potential to inhibit tumour growth in vivo.ALK5-IN-28 can be used to study proliferative diseases (e.g. cancer, fibrotic diseases, systemic sclerosis).

ALK5-IN-25 (compound EX-02) is a potent ALK-5 inhibitor (IC50<10 nM) that also inhibits ALK-2 and can be used in cancer research.

ALK5-IN-27 (Compound EX-04) is a potent inhibitor of ALK-5 (IC50 ≤ 10 nM) and also inhibits ALK-2.

D4476 (Casein Kinase I Inhibitor) is an effective, selective, and cell-permeant CK1 (casein kinase 1) inhibitor( IC50=300 nM in a cell-free assay).

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.

ALK5-IN-32 is a selective inhibitor of ALK-5 (10 nMALK5-IN-31 has the potential to inhibit tumor growth in vivo.ALK5-IN-31 can be used in the study of proliferative diseases (e.g. cancer, fibrotic diseases, systemic sclerosis). .

ALK5-IN-26 (EX-22) is an ALK (Activin receptor-like kinase) inhibitor with an IC50 ≤ 1 nM for ALK5.