T6376

Allopurinol Sodium is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM.

3CPLro-IN-2 is a potent, orally active inhibitor of SARS-CoV-2 3CLpro (IC50: 1.55 μM, Ki: 6.09 μM). 3-Chymotrypsin-like cysteine protease (3CLpro) is an essential protein for viral replication and is a potential drug target against COVID-19.

ACT-660602 is an orally active chemokine receptor CXCR3 antagonist (IC50: 204 nM) that inhibits T cell migration and has demonstrated significant efficacy in an in vivo model of acute lung injury. It is useful for studying autoimmune diseases.

AMG-548 dihydrochloride is a selective, orally active p38α inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38β (Ki=36 nM) and >1000-fold selectivity for p38γ and p38δ. AMG-548 dihydrochloride exhibits inhibition of whole blood LPS-stimulated TNFα with an IC50 value of 3 nM. AMG-548 dihydrochloride directly inhibited casein kinase 1 isoforms δ and ε, and inhibited Wnt signaling.

WDR5-IN-5 is a selective, orally active inhibitor targeting the WD repeat domain 5 (WDR5) WIN site.WDR5-IN-5 exhibits high affinity for WDR5 (Ki<0.02 nM).WDR5-IN-5 exhibits anti-cancer cell proliferation and a good pharmacokinetic profile.

hCA XII/II/IX-IN-1 is a potent inhibitor of human carbonic anhydrase (hCA), acting on hCA I (IC50: 2.6 μM), hCA II (IC50: 0.004 μM), hCA IX (IC50: 0.005 μM), and hCA XII (IC50: 0.001 μM). hCA XII/II/IX-IN-1 exhibited anticancer effects.

L5-DA is a G-quadruplex (G4) ligand that selectively stabilizes G4s, exhibiting significant cytotoxicity to HeLa cells with an IC50 value of 4.3 μM. It stabilizes G4s in HeLa cells, blocking the cell cycle and inducing apoptosis.

MrgprX2 antagonist-7 is an anti-allergic agent with significant anti-allergic effects and inhibits mast cell degranulation.

P300 bromodomain-IN-1 is a potent inhibitor of p300 (EP300) bromodomain (IC50: 49 nM). p300 bromodomain-IN-1 blocks c-Myc expression and induces cell cycle arrest at G1/G0 phase and apoptosis in OPM-2 cells. apoptosis).

Antitumor agent-78 inhibits GPx-4 and elevates COX2, leading to ferroptosis. antitumor agent-78 activates the tumor cell intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and inhibits the epithelial mesenchymal transition (EMT) process in tumor cells. Antitumor agent-78 exhibits antitumor effects and inhibits the growth and migration of cancer cells.

EGFR-IN-60 is an effective, orally active, safe antitumor agent. EGFR-IN-60 significantly inhibits EGFRWT (IC50: 83 nM), EGFRT790M (IC50: 26 nM), EGFRL858R (IC50: 53 nM) and JAK3 (IC50: 69 nM). IN-60 inhibited H1975 cells carrying the EGFRT790M mutation (IC50: 1.32 μM) and A431 cells overexpressing EGFRWT (IC50: 4.96 μM). EGFR-IN-60 increased the Bax/Bcl-2 ratio, which induced apoptosis induction and cell death.