T21419

Diphenhydramine (Syntedril), a first-generation antihistamine possessing antiemetic, antitussive, anticholinergic, and sedative properties, is mainly used in the treatment of allergies. Diphenhydramine is also used in the management of drug-induced parkinsonism and other extrapyramidal symptoms.

1-(1-Naphthyl)piperazine is a modulator of 5-HT receptors, acting both as a 5-HT2A receptor antagonist and a 5-HT1A receptor agonist, with a human 5-HT6 receptor binding constant (Ki) of 120 nM. It partially inhibits forskolin-stimulated adenylate cyclase activity in bovine substantia nigra and can suppress UV radiation-induced immunosuppression. Additionally, 1-(1-Naphthyl)piperazine induces S-phase cell cycle delay, apoptosis, and increases reactive oxygen species (ROS) levels, leading to the inhibition of MNT-1 cell proliferation. This compound is utilized in melanoma research.

UAMC-00050 free base is an effective inhibitor of trypsin-like serine proteases. It is applicable in research related to dry eye syndrome and ocular inflammation.

LOXL2/sGC modulator-2 (Compound 9k) is a selective, orally active dual-target modulator of lysyl oxidase-like protein 2 (LOXL2) and soluble guanylate cyclase (sGC). It inhibits LOXL2 with an IC50 of 0.1 μM and acts as an sGC activator. This compound can improve vascular remodeling and reduce pulmonary arterial pressure while downregulating PKG1, PCNA, α-SMA, collagen I, and fibronectin levels. LOXL2/sGC modulator-2 is useful for studying pulmonary arterial hypertension.

D2R/D3R/5-HT1AR agonist 1 (compound 22b) is an orally active tri-target agonist with EC50 values of 1.29, 1.05, and 153.5 nM for D2R, D3R, and 5-HT1AR receptors, respectively. This compound improves MPTP-induced behavioral disorders and exhibits antidepressant properties, making it relevant for research in Parkinson's disease and depression.

Janagliflozin is an orally active and highly selective inhibitor of sodium-glucose co-transporter protein 2 (SGLT2) with an IC50 value of 0.0058 μM, and an IC50 of 4.802 μM for SGLT1. It inhibits SGLT2 in the proximal renal tubules, reducing glucose reabsorption and promoting urinary glucose excretion (UGE), thereby lowering blood glucose levels. Janagliflozin holds potential for research in treating type 2 diabetes.

LCI133 is an innovative, highly potent, and selective multi-target kinase inhibitor effective at the nanomolar level. It targets CDK4/6/9 and AURKA/B with IC50 values of 4.7/10.2/4.1 nM and 2.8/10.6 nM, respectively. In MYCN-amplified neuroblastoma BE(2)-C cells, LCI133 induces S/G2 phase arrest and triggers significant apoptosis (apoptosis). Moreover, LCI133 demonstrates substantial antitumor efficacy in BE(2)-C neuroblastoma xenograft models.

MPXV p37 protein-IN-1 is a potent and orally effective inhibitor of the monkeypox virus (MPXV) p37 protein. It exhibits significant antiviral activity against MPXV, with an EC50 of 12.14 nM, and shows low cytotoxicity (CC50= 304.63 μM). In mice, MPXV p37 protein-IN-1 demonstrates low toxicity and good tolerability. This compound can be utilized for research into anti-monkeypox virus drugs.

Alcudacigib (Compound 9) TFA is an inhibitor of DGKz. It can be utilized in research related to cancers associated with immune cell activation or cancers resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapies.

DL78 is a potent antimitotic agent that induces mitotic arrest, mitotic catastrophe, and apoptosis in cancer cells by disrupting the interaction between Myc and α-tubulin. It exhibits broad anticancer activity, particularly targeting cancer cells characterized by chromosomal instability and MYC overexpression. In the OV81.2 xenograft model, DL78 significantly reduces tumor burden. DL78 can be employed in ovarian cancer research.

Decarboxy ciprofloxacin (Decarboxylated ciprofloxacin) is an antibacterial agent. It exhibits antibacterial activity against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecium, Bacillus subtilis, Enterobacter cloacae, and Serratia marcescens, with particularly strong efficacy against Escherichia coli.