T6170

Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.

PIM1-IN-7 (compound 6c) is a potent PIM-1 inhibitor with an IC50 of 0.67 μM, and it also shows notable cytotoxicity against HCT-116 and MCF-7 cells, with IC50 values of 42.9 and 7.68 μM, respectively [1].

SHP2-IN-9 is a potent inhibitor (IC50 = 1.174 μM) specifically targeting the SHP2 protein, displaying improved penetration across the blood-brain barrier. It exhibits a remarkable 85-fold selectivity for SHP2 over SHP1. By inhibiting SHP2-mediated cell signal transduction and impairing cancer cell proliferation, SHP2-IN-9 effectively suppresses the growth of both cervix cancer tumors and glioblastoma in vivo [1].

SRI-37240 is a potent inhibitor of premature termination codons (PTCs) with read-across activity that induces a prolonged pause at the termination codon and inhibits PTCs associated with cystic fibrosis.SRI-37240 can be used to study PTC-related diseases.

GAK inhibitor 2 (Compound 14g) is a highly potent inhibitor of cyclin G-associated kinase (GAK) with an IC50 of 0.024 μM and exhibits remarkable antiviral activity against dengue virus (DENV) with an EC50 of 1.049 μM [1].

RSV-IN-6 (Compound 53) is a specific inhibitor of the respiratory syncytial virus (RSV) that targets the M2-1 protein, demonstrating strong potency with EC50 values of 4.4 μM against RSV-A and 1.3 μM against RSV-B strains [1].

MIF-IN-6 (compound 2d) is an effective inhibitor of macrophage migration inhibitory factor (MIF), with an IC50 of 1.4 μM and a Ki value of 0.96 μM. It effectively reduces MIF-induced ERK phosphorylation and impedes A549 cell proliferation [1].

α-Amylase/α-Glucosidase-IN-2 (compound 5) exhibits strong inhibition of α-amylase and α-glucosidase enzymes, with IC50 values of 13.02 μM and 13.09 μM, respectively, showing promise for investigating diabetic complications [1].

FAAH/MAGL-IN-2, a potent and reversible inhibitor of FAAH and MAGL, demonstrates oral activity and the ability to cross the blood-brain barrier. It exhibits IC50 values of 11 nM for FAAH and 36 nM for MAGL (Ki values of 28 nM and 60 nM, respectively). This compound shows promise for neuropathic pain research, without impairing locomotion [1].

AZD 2066 hydrate is a selective, orally active, brain-penetrant mGluR5 antagonist with antinociceptive effects [1].

AMS-17 is a potent NLRP3 inhibitor that effectively suppresses microglia activation both in vitro and in vivo. Moreover, AMS-17 exhibits inhibitory effects on various cytokines, such as caspase-1, TNF-α, IL-1β, and inducible nitric oxide synthase (iNOS), in N9 cells, making it a promising tool for investigating inflammation-associated neurological disorders [1].