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.

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

A unique collection of xnum kinase inhibitors/regulators for high throughput screening and high content screening for drug discovery in kinase related diseases;

Entrectinib-D8 is the deuterated form of Entrectinib. Entrectinib (T3678) (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 (T3678) induces apoptosis and cell cycle arrest in cancer cells, demonstrates antitumor properties, and alleviates bleomycin-induced pulmonary fibrosis in mice.

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).

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.

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.

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

TL13-12 is a selective degrader of ALK-PROTAC and inhibits ALK activity (IC50: 0.69 nM).

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

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.

Negative control for TL 13-112 . Displays no degradation of ALK in cell lines. Highly potent ALK inhibitor (IC50 = 0.34 nM).