T6183

ISRIB (trans-isomer) is a potent inhibitor of PERK (IC50=5 nM) that restores protein translation and prevents SG formation in the presence of P-eIF2α.

NS1-IN-1 is a potent NS1 inhibitor.NS1-IN-1 displays antiviral activity by inhibiting mTORC1 activity in a TSC1-TSC2-dependent manner.NS1-IN-1 reduces the level of viral proteins and contributes to the reduction of viral replication.

MAO-B-IN-10 (compound 4f) is a highly potent and selective MAO-B (monoamine oxidase-B) inhibitor that effectively penetrates the blood-brain barrier, exhibiting an IC50 of 5.3 μM. It demonstrates the ability to inhibit self-mediated Aβ (amyloid β) aggregation by 58.2% and disaggregate it by 43.3%, holding promise for Alzheimer's disease research [1].

hCAI/II-IN-3 (compound 5b) is a highly effective dual inhibitor of hCA I/II enzymes, exhibiting Ki values of 51.25, 13.15, and 42.18 nM for hCA I, hCA II, and hCA Ⅸ, respectively. It demonstrates anti-hypoxic properties against acute mountain sickness (AMS) and exhibits low cellular activity [1].

Tovinontrine (IMR-687) (IMR-687) is a potent and selective inhibitor of phosphodiesterase-9 (PDE9), designed to target sickle cell disease treatment. It exhibits high efficacy, with IC 50 values of 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively [1].

Trans-substituted cephalosporin is an efficient inhibitor of NDM-1, demonstrating an IC50 value of 0.13 μM.

Samuraciclib (CT7001) is a potent, selective, and orally active CDK7 inhibitor with an ATP-competitive nature, effectively inhibiting CDK7 with an IC50 of 41 nM. It demonstrates 45-fold, 15-fold (IC50 of 578 nM), 230-fold, and 30-fold selectivity over CDK1, CDK2, CDK5, and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values of 0.2-0.3 μM and possesses anti-tumor effects [1] [2].

Pioglitazone potassium (U 72107) is an orally active, selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting high-affinity binding to the ligand-binding domain of PPARγ with EC50 values of 0.93 μM for human and 0.99 μM for mouse PPARγ. It has applications in diabetes research [2] [3] [4].

5-HT6/5-HT2AR antagonist-1 is a potent dual antagonist for the 5-HT6 and 5-HT2A receptors, demonstrating high efficacy with K_i values of 11 nM and 39 nM, respectively [1].

Pencitabine (Pen) is an orally bioavailable antineoplastic compound that impedes DNA synthesis by inhibiting various nucleotide-metabolizing enzymes and incorporating itself erroneously into DNA [1].