T6041

Oprozomib (PR-047) (ONX 0912) , an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has potential antineoplastic activity.

ART-IN-1 (compound 7) is a selective inhibitor of PARP with IC50 values of 19 μM for PARP2, 22 μM for TNKS2, 2.4 μM for PARP10, >100 μM for PARP14, and 1.1 μM for PARP15 [1].

Primaquine is an antimalarial compound and a gametocytocide, clearing liver schizonts and dormant forms of Plasmodium vivax.

BPN-15477 is a splicing modulator compound (SMC) that restores the correct splicing of ELP1 exon 20. It can be used for frontotemporal dementia research. BPN-15477 corrects the splicing of the ELP1 transcript which significantly increases the level of functional protein in vivo in all tissues, including the brain [1].

HIF-IN-1 is a potent inhibitor of hypoxia-inducible factor (HIF-1), which is associated with tumor and cancer cell proliferation and inhibits HIF-1α protein aggregation.

Antibacterial agent 73 (compound 7a) exhibits antitubercular, antibacterial, and antifungal activities, with promising antitubercular activity (MIC of 0.65 μg/mL) against Mtb H37Rv, and also demonstrates cytotoxicity in MCF-7 breast cancer cell lines (IC 50 of 8.20 μM) [1].

DS34942424 is an orally potent analgesic that does not exhibit mu opioid receptor agonist activity.

CRM1 degrader 1 (1l) is a low-toxicity CRM1 degrader that induces apoptosis in gastric carcinoma and selectively inhibits the proliferation of gastric cancer[1].

Fenspiride is an antagonist of H1-histamine receptors. Fenspiride is an orally active non-steroidal anti-inflammatory agent that can be used for the treatment of respiratory tract infections and otitis media. Fenspiride inhibited phosphodiesterase 4 and phosphodiesterase 3 activities with -logIC50 values of 4.16+/-0.09 and 3.44+/-0.12, respectively. Phosphodiesterase 5 activity was also inhibited with a -logIC50 value of approximately 3.8.

Ropinirole (SKF 101468) is an orally active and potent D3/D2 receptor agonist with anti-amyotrophic lateral sclerosis effects. Ropinirole is used in the study of Parkinson's disease.

Cyclic HPMPC is a potent antiviral agent that increases arterial oxygen saturation in mice infected with the lethal vaccinia virus (IHD strain) and reduces viral replication in guinea pigs, thereby improving outcomes in congenital guinea pig cytomegalovirus (GPCMV) infection [1] [2].