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.

TGFβRI-IN-2 is a selective, potent and orally active inhibitor of (Activin-Like Kinase 5) ALK 5(pIC50 and pEC50 values of 7.6 and 6.63, respectively).

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.

Trk-IN-7 (compound I-6) is a highly potent TRK inhibitor, with IC50 values of 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. It also shows significant inhibition of EML4-ALK (IC50 <15 nM) and ALK mutations G1202R, C1156Y, R1275Q, F1174L, L1197M, and G1269A (IC50 = 5-50 nM) [1].

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.

CEP-14513 is a potent ALK inhibitor. CEP-14513 displayed potent ALK inhibitory activity in both in vitro enzymatic assay (IC50 = 5 nM) and cell-based assays of ALK tyrosine phosphorylation (IC50 = 30 nM).

M4K2234 (Compound 26b) is a selective inhibitor of ALK2, displaying IC50 values of 5 nM for ALK2 and 2144 nM for ALK5. As a chemical probe for ALK1 and ALK2 kinases, it is used in mechanistic studies of BMP signaling and in cancer research where dysregulated ALK2 activity is implicated. Its high selectivity profile supports targeted investigations into ALK-mediated pathways.

Zilurgisertib fumarate (INB-000928 fumarate) is a potent and selective inhibitor of Activin Receptor-Like Kinase 2 (ALK2/ACVR1). It significantly inhibits ALK2 kinase activity (IC50 = 15 nM) and downregulates BMP-6-induced SMAD1/5 phosphorylation (IC50 = 63 nM). By blocking ALK2-mediated signaling, Zilurgisertib suppresses the production of hepcidin in hepatocytes (IC50 = 20 nM), thereby modulating iron metabolism. In preclinical studies, Zilurgisertib demonstrates the potential to improve anemia in cancer-induced models by effectively increasing hemoglobin levels.

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

XMU-MP-5 acts as a selective inhibitor of ALK. It inhibits ALK-mutant Ba/F3 cells with an IC50 ranging from 4-50 nM and induces apoptosis in EML4-ALK Ba/F3 cells. Additionally, XMU-MP-5 demonstrates antitumor activity in mice.

Entrectinib-d4 is the deuterium-labeled isotope of Paquinimod. Entrectinib is an orally active inhibitor of TrkA/B/C, ROS1, and ALK, capable of crossing the blood-brain barrier and possessing central nervous system activity, with IC50 values of 1, 3, 5, 12, and 7 nM, respectively. It induces apoptosis and cell cycle arrest in cancer cells, exhibits antitumor efficacy, and mitigates bleomycin-induced pulmonary fibrosis in mice.

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is the deuterated form of Entrectinib. Entrectinib (NMS-E628) is an orally bioavailable inhibitor that effectively crosses the blood-brain barrier and exhibits central nervous system activity. It targets TrkA/B/C, ROS1, and ALK with IC50 values of 1, 3, 5, 12, and 7 nM, respectively. Entrectinib induces apoptosis and cell cycle arrest in cancer cells, demonstrates antitumor properties, and alleviates bleomycin-induced pulmonary fibrosis in mice.