BMS-347070 is an inhibitor of COX-2. BMS-347070 can be studied in research on Pluronic®-bassed nano-crystalline drug-polymer solid dispersions.

AVI-6451 is a novel orally effective SARS-CoV-2 Mac1 (IC50 = 28 nM) inhibitor. AVI-6451 can reduce viral load. AVI-6451 can be used for research on viral infections.

MM927 is a potent NVL inhibitor, with an IC50 of 0.053 μM. MM927 blocks 60S ribosomal subunit biogenesis in the nucleolus. MM927 induces half-mer polysomes, cell cycle arrest at G1/S and G2/M and apoptosis in cells. MM927 demonstrates antitumor efficacy in MOLM-13 AML and HCT116 CRC xenograft models. MM927 can be used for the study of cancers such as acute myeloid leukemia (AML) and colorectal cancer (CRC).

Besonprodil (CI-1041) is a potent NMDA antagonist.

Batoprazine (8-(1-piperazinyl)-2H-1-benzopyran-2-one)) is a 5-HT1A,1B receptor agonist. Batoprazine can replace the behavioral stimulus of eltoprazine in the two-lever operant discrimination test between eltoprazine and deionized water in rats (ED50: 0.20 mg/kg).

RuOPt is a photoactivatable Ru(II)-Pt(IV) complex with reduced dark toxicity. Under irradiation, RuOPt induces apoptosis, generates ROS, and inhibits tumor spheroid growth, demonstrating comparable phototoxicity.

AGN192093 is a TP agonist (EC50 = 1.3 nM). AGN192093 exhibits potent and selective thromboxane analog activity in rat blood vessels.

OUL312 is a potent PARP10 inhibitor (IC50 = 20 nM), showing more than 75-fold greater selectivity for PARP15(IC50 = 1500 nM). OUL312 is also at least 18-fold higher than all other human enzymes in the family. OUL312 has a good ADME profile, is able to enter cells, is not toxic, and effectively rescues human cells from PARP10-induced apoptosis at sub-micromolar concentrations. OUL312 can be used for the study of cervical cancer.

JGK-263 is an orally active Glycogen synthase kinase-3β (GSK-3β) inhibitor. JGK-263 exhibits neuroprotective effect and can improve motor function. JGK-263 can be used for the research of neurological disease, such as amyotrophic lateral sclerosis (ALS).

XC-12 is an orally active and potent small-molecule CD73 inhibitor (an immune checkpoint) with IC50 values of 12.36 nM and 1.29 nM against soluble and membrane-bound CD73 forms, respectively. XC-12 is promising for research of cancers.

L 652813 is a quaternary ammonium heterocyclic amino β-lactam compound. L 652813 exhibits inhibitory activity against a broad spectrum of aerobic and anaerobic bacteria in vitro. L 652813 also exhibits good antibacterial activity in a mouse experimental bacteremia model.

GSK-163090 (dihydrochloride) is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4, 8.5 and 9.7, respectively. GSK-163090 (dihydrochloride) inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK-163090 (dihydrochloride) has antidepressant and anxiolytic activities.

iRucaparib-TP3 is a selective PARP1 degrader (DC50=36 nM). iRucaparib-TP3 is promising for research of oncology (e.g., BRCA-mutated cancers) and neurodegenerative diseases.

CGP 12177 ((±)-CGP 12177) is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 is a β3-AR (Ki = 88 nM) agonist with β1/β2-AR (Ki = 0.9 nM for β1; Ki = 4 nM for β2) antagonist action. CGP 12177 exhibits partial agonist properties for α1-AR in rat pulmonary artery. CGP 12177 regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 can be used for cardiovascular and metabolic disease research[1][2][3][4].

DC-015 is a selective and orally active alpha 1-adrenoceptor antagonist on plasma lipid and vascular reactivity in hyperlipidaemic rodent model. DC-015 is a synthesized quinazoline derivative. DC-015 decreases mean arterial pressure in rats. DC-015 has antihypertensive activity.

5-Chloro-1,4-dihydro-2,3-quinoxalinedione (Compound 72) is a weak NMDA inhibitor with an IC50 of 56.3 μM. 5-Chloro-1,4-dihydro-2,3-quinoxalinedione can be used for the research of neurological disease.

GSK2181306A is a pan-FIKK inhibitor with an EC50 value of 0.16 μM for parasite growth inhibition. GSK2181306A can be used to study Plasmodium infection.

PNR-3-82 is a selective Apoptotic endonuclease G (EndoG) inhibitor with an IC50 of 0.61  μM for EndoG over DNase I. PNR-3-82 does not inhibit five cell death-related enzymes including DNase II, RNase A, proteinase, lactate dehydrogenase and superoxide dismutase 1. PNR-3-82 has a cytoprotective activity and blocks Cisplatin and Docetaxel-induced cell death. PNR-3-82 can be used for cell injuries research.

PNR-3-80 is a selective Apoptotic endonuclease G (EndoG) inhibitor with an IC50 of 0.67  μM for EndoG over DNase I. PNR-3-80 does not have inhibitory activities for DNase II, RNase A, proteinase, lactate dehydrogenase and superoxide dismutase 1. PNR-3-80 has a potent cytoprotective activity, and it significantly protects human prostate carcinoma cells from Cisplatin and Docetaxel-induced cell death and represses Etoposide-induced DNA damage and autophagy. PNR-3-80 can be used for cell injuries research.

M 16209 is an orally active aldose reductase (AR) inhibitor. M 16209 inhibits partially purified AR from various sources with IC50 values of 0.12, 0.24, 4.5, 1.2 and 9.3 μM for rat lens AR, bovine lens AR, bovine kidney AR, canine lens AR and human placental AR. M 16209 can be used for the research of metabolic disease, such as diabetes.

CEP-6800 is an inhibitor of PARP-1 with chemopotentiating ability. CEP-6800 attenuates irinotecan- and Temozolomide-induced poly(ADP-ribose) accumulation in LoVo as well as HT29 xenografts. CEP-6800 can suppress Calu-6 tumor growth. CEP-6800 can be studied in anti-cancer research.

CK-2289 is an inhibitor of type III cyclic 3'5'-adenosine monophosphate phosphodiesterase (PDE). CK-2289 can inhibit platelet aggregation and decreases mean arterial blood pressure. CK-2289 can be used for the research of cardiovascular disease, such as congestive heart failure.

CHNQD-01426 (Compound 4a) is an anticancer agent. CHNQD-01426 has cytotoxic activities against cancer cells. CHNQD-01426 significantly inhibits hepatocellular carcinoma cells proliferation via arresting S and G2/M phase cell cycle and induces apoptosis by inducing ROS production and elevating apoptosis-related proteins expression. CHNQD-01426 potently inhibits tumor growth in HepG2 xenograft mice model.

Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor (IC50: < 10  nM) with high selectivity of MMP-1, -2, -3, -7, -9, -10 and -14. Linvemastat significantly attenuates lung fibrosis in Bleomycin) induced unilateral lung fibrosis mice model and potently reduces kidney damage, interstitial inflammation or fibrosis in kidney fibrosis model of unilateral ureteral occlusion. Linvemastat can be used for inflammatory diseases research, such as idiopathie pulmonary fibrosis (IPF), inflammatory bowel disease (IBD) and asthma.

TSAO-T is a HIV-1 reverse transcriptase inhibitor. TSAO-T can be used in the research of HIV infection.

PBD derivative-1 (Compound 7-8) is a derivative of PBD, and PBD is the payload in antibody-drug conjugates (ADCs). PBD derivative-1 can be used for the synthesis of ADCs.

SL-251131 is a reversible non-specific MAO inhibitor. SL-251131 temporarily blocks both MAO-A and MAO-B enzymes, which are responsible for breaking down neurotransmitters like dopamine. SL-251131 can be used for the study of Parkinson's disease.

HW201877 is a potent and orally active 15-prostaglandin dehydrogenase (15-PGDH) inhibitor with an IC50 of 3.6 nM. HW201877 demonstrates robust cellular efficacy in elevating PGE2 levels in A549 cells and exhibits remarkable efficacy in animal models of tissue injury and fibrosis. HW201877 can be used for the study of inflammatory bowel disease (IBD), idiopathic pulmonary fibrosis (IPF) and Crohn’s disease (CD).

TP-9201 is a platelet glycoprotein (GP) IIb/IIIa receptor antagonist. TP-9201 inhibits the interaction between GPIIb/IIIa and fibrinogen, thereby suppressing platelet aggregation. TP-9201 exhibits similar inhibitory activity on adenosine diphosphate (ADP)-induced platelet aggregation in humans, baboons, and dogs (IC50 = 1-3 μM), while showing lower activity in rabbits (IC50 = 45 μM) and rats (IC50 = 20 μM). TP-9201can be used in studies related to the prevention of rethrombosis after arterial thrombolysis.

FK 089 is an antibacterial Agent. FK 089 can be used for the research of infection.