T6048

Dalcetrapib (RO4607381), a rhCETP inhibitor (IC50=0.2 μM), increases the plasma HDL cholesterol.

GABAA receptor agent 4 (compound 1e) is a potent antagonist of γ-GABAAR, exhibiting a Ki of 0.18 µM, and demonstrates immunomodulatory potential by effectively rescuing the inhibition of T cell proliferation [1].

Pilsicainide (SUN 1165 free acid) is a potent class Ic antiarrhythmic agent and a sodium channel blocker[1][2].

Fasedienol is a neurochemical stimulator of the vomeronasal organ (VON) that alleviates symptoms of premenstrual dysphoric disorder (PMS) and anxiety [1].

DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].

Mycobactin-IN-1 (compound 44) is a pyrazoline analogue. Mycobactin-IN-1 binds to salicyl-AMP ligase (MbtA) which is a key enzyme in the mycobactin biosynthetic pathway. Mycobactin-IN-1 is an inhibitor of mycobactin biosynthesis that against mycobacteria [1].

DDO-7263 is a 1,2,4-Oxadiazole derivative that upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 is a potent Nrf2 activator that activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity [1].

Ganciclovir (BW 759) hydrate is a nucleoside analogue that is an orally active antiviral agent with anti-cytomegalovirus activity. Ganciclovir hydrate is also active against members of the herpes group and some other DNA viruses in vitro. Ganciclovir hydrate inhibits the replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28 in vitro. Ganciclovir hydrate also has an IC 50 of 5.2 μM against feline herpesvirus type-1 ( FHV-1 ) and can diffuse into the brain [1] [2] [3].

hMAO-B/MB-COMT-IN-1 is a dual MAO-B/MB-COMT inhibitor with IC50s of 2.5 μΜ for hMAO-B and 3.84 μΜ for MB-COMT. hMAO-B/MB-COMT-IN-1 protects cells from oxidative damage and can be utilized in neurodegenerative disease research, such as Parkinson's Disease (PD) [1].