ALK

F-1: Potent ALK/ROS1 inhibitor with 2.1-3.9 nM IC50s; suppresses p-ALK signaling.

LDN-193189 2HCl inhibits BMP signaling (ALK1/2/3/6), IC50: 0.8-16.7 nM; selective over TGF-β by 200-fold in C2C12 cells.

ZX-29: Strong ALK inhibitor; IC50 - ALK 2.1 nM, L1196M 1.3 nM, G1202R 3.9 nM; triggers autophagy; anti-cancer.

MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.

Ascrinvacumab (PF-03446962): humanized IgG2 anti-ALK-1 antibody, Kd 7 nM, inhibits TGF-β, for HCC research.

ALK inhibitor 1 is a selective ALK kinase inhibitor.

ALK inhibitor 2 is a new-type and selective inhibitor for the ALK kinase.

CEP-28122 mesylate salt (1022958-60-6 free base) is a highly selective orally active ALK inhibitor (IC50: 1.9 nM in an enzyme-based TRF assay).

ALK-IN-26 is an ALK inhibitor with potential anticancer activity.ALK-IN-26 shows antiproliferative activity against glioblastoma.

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that effectively impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2.

ALK-IN-12: potent ALK inhibitor (IC50: 0.18 nM), affects IGF1R and InsR (IC50: 20.3/90.6 nM), potential for cancer therapy.

ALKBH5-IN-5 is a highly selective, potent and covalently binding ALKBH5 inhibitor that alters m6A levels on mRNA, induces apoptosis, antitumo.

CPD-1224, an oral ALK inhibitor derivative, binds cereblon, targets EML4-ALK fusions, and degrades ALK plus L1196M/G1202R mutants.

TL13-112 is a selective degrader of ALK-PROTAC and inhibits ALK activity (IC50: 0.14 nM).

SIAIS164018 hydrochloride is a PROTAC-based degrader targeting ALK and EGFR, exhibiting IC50 values of 2.5 nM for ALK and 6.6 nM for ALK G1202R.

ALK-IN-9 effectively inhibits cell growth with IC50 <0.2 nM for Ba/F3-EML4-ALK, KM12, KG-1.

Zilurgisertib fumarate is a selective ALK2 inhibitor that modulates iron metabolism and improves anemia by inhibiting SMAD phosphorylation and hepcidin production.

ALK2-IN-6 is a potent and selective ALK2 inhibitor with an IC50 of 9 nM. ALK2-IN-6 exhibits excellent brain permeability and effectively suppresses bone morphogenetic protein signaling across various preclinical cancer models for the treatment of diffuse intrinsic pontine glioma.

ALK degrader 2 is an orally active ALK degrader that reduces EML4-ALK protein levels (DC50= 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50= 102 nM). It facilitates ALK degradation through the Hsp70 chaperone system and the ubiquitin-proteasome pathway. In H3122 cells, ALK degrader 2 causes significant cell cycle arrest at the S phase and induces apoptosis. Additionally, it demonstrates antitumor activity in mice with H3122 xenograft tumors. ALK degrader 2 is a useful compound in researching non-small cell lung cancer (NSCLC).

A unique collection of xnum kinase inhibitors/regulators for specific targeting of kinases, ready for high-throughput screening and high-content screening.