WebSep 7, 2012 · Floyd and co-workers reported that an α-secretase inhibitor, INCB3619, decreased proliferation of GBM cell lines as well as GBM stem cell lines mainly through Notch inhibition [234]. Moreover,... INCB3619 is an Orally Active ADAM Inhibitor with Anti-tumor Activity Posted On 2024-04-10 ADAM (disintegrin and metalloprotease) family consists of transmembrane proteins with a multidomain extracellular domain, a single transmembrane sequence, and a relatively short cytoplasmic domain.

ADAM17 is a tumor promoter and therapeutic target in …

Web#JHepatol: Non-alcoholic steatohepatitis (#NASH) is a chronic inflammatory disease that further progresses to cirrhosis and HCC. However, what's the key… WebApr 26, 2016 · In breast cancer cell lines, INCB3619 reduced the cleavage of both HER2 and amphiregulin, and synergized with a dual EGFR/HER2 inhibitor (GW2974; GSK) in reducing cell growth in vivo. 37 In animal models, INCB3619 has also been shown to have anti-cancer activity against malignancies of the lung (non-small cell), breast, head and neck. 35,36 An ... high point 4595 carbine

Synergistic inhibition with a dual epidermal growth factor …

WebWe found that INCB3619 treatment augmented the accumulation of VGAT puncta on HEK293 cells expressing the NL4X L593F variant (Fig. (Fig.6f, 6 f, g). Consistent with this result, the synaptogenic activity of the K651/D652 deletion mutant was also rescued by INCB3619 treatment (Fig. (Fig.5g, 5 g, h). Taken together, these data indicated that the ... WebDescription INCB3619 is a selective and orally active ADAM inhibitor with IC50 of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity [1] . In … WebAug 19, 2024 · IV-361 is an Orally Active and Selective CDK7 Inhibitor. First of all, IV-361 is an orally active and selective CDK7 inhibitor (K i ≤50 nM). Meanwhile, IV-361 has anti-tumor activity (US20240256531A1). Nonetheless, IV-361 has less inhibition on CDK2 (K i ≥1000 nM) or PLK1 (K i ≥5000 nM). high point 9 mil