alk in 5

ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of 2.9 nM.

ALK5-IN-10 is a potent ALK5 inhibitor with an IC50 of 7nM.

ALK/ROS1-IN-5 (compound X4) is a selective inhibitor of ALK and ROS1 kinases, with IC50 values of 0.512 μM for ALK and 0.766 μM for ROS1. It inhibits H2228 cells with an IC50 of 0.034 μM and induces apoptosis in cancer cells in a dose-dependent manner. Additionally, ALK/ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells.

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

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-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-32 is a selective inhibitor of ALK-5 (10 nMinhibits TGF-β-induced SMAD signaling.ALK5-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-27 (Compound EX-04) is a potent inhibitor of ALK-5 (IC50 ≤ 10 nM) and also inhibits ALK-2.

ALK-5-IN-1, an ALK-5 inhibitor, can be utilized for cancer research and studying conditions involving fibrosis [1].

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-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-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-80 (Compound 29b) is a selective ALK5 inhibitor with an IC50 of 3.7 nM, suitable for cancer research.

ALK5-IN-85 (Compound 19) is an inhibitor of TGFβRI (ALK5) with an IC50 of less than 100 nM. It can be used for the treatment of respiratory diseases such as idiopathic pulmonary fibrosis, asthma, chronic obstructive pulmonary disease, and lung cancer, as well as for research on skin and ocular fibrotic diseases.

PROTACALK degrader-5 (Compound 17) is a potent ALKPROTAC degrader with activities of 27.4 nM against EML4-ALK and 116.5 nM against NPM-ALK. It exhibits strong antiproliferative effects on H3122 and Karpas 299 cell lines and effectively inhibits the phosphorylation of ALK and STAT3. This compound is applicable for studying ALK-driven malignancies, such as human non-small cell lung cancer and anaplastic large cell lymphoma.

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

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-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-7 is an effective inhibitor of ALK5. Transforming growth factor β (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation, and apoptosis through autocrine, paracrine, and endocrine pathways using complex receptor signaling pathways on the cell surface. ALK5-IN-7 has the potential to perform research on TGF-β-related diseases and conditions (including but not limited to tumor, fibrosis, inflammatory diseases, autoimmune diseases, etc.).

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.