EYE-003 is an orally active RPE65 inhibitor with an IC50 of 102 nM. EYE-003 regulates the visual cycle in mice by reducing 11-cis-retinal (11cRAL)) synthesis and increasing all-trans-retinyl esters (atREs). EYE-003 suppresses scotopic ERG b-wave amplitude and exerts protective effects against retinal degeneration in Abca4⁻/⁻ Rdh8⁻/⁻ mice (a STGD1 model) by reducing retinal autofluorescent puncta and preserving outer nuclear layer (ONL) thickness in a dose-dependent manner. EYE-003 can be used for the study of visual cycle-associated retinopathies, such as Stargardt disease type 1 (STGD1).

EYE-002 is a RPE65 inhibitor with an IC50 of 69 nM. EYE-002 promotes recovery of scotopic ERG a-/b-wave amplitudes. EYE-002 regulates the visual cycle in mice by reducing 11-cis-retinal (11cRAL)) synthesis and increasing all-trans-retinyl esters (atREs). EYE-002 exerts protective effects against photic retinal damage in mice. EYE-002 can be used for the study of visual cycle-associated retinopathies, such as Stargardt disease type 1 (STGD1).

A-72055 is a partial agonist of muscarinic receptors. A-72055 has binding activity to both M1 and M2 receptors, with Ki values of 32 nM and 30 nM, respectively. A-72055 can enhance cognitive function and improve learning and memory deficits. A-72055 has better security. A-72055 can be used for research on neurological disorders such as cognitive impairment.

CDK9 ligand-Linker Conjugate is a synthesized CDK9 ligand-linker conjugate that can be used for synthesis of dCDK9-202. dCDK9-202 is a potent CDK9 PROTAC degrader with anti-tumor activity.

(±)-Tuaimenal A ((+)-1) is a secondary metabolite and a derivative of Sesamol. (±)-Tuaimenal A has potent inhibitory activity against SARS-CoV-2 3CLpro with an IC50 of 33.3  μM. (±)-Tuaimenal A can be used for SARS-CoV-2 infection research.

CPD-2828 is an orally active and selective IRE1α inhibitor with an IC50 value of 1.2 μM. CPD-2828 is promising for research of endoplasmic reticulum stress-related diseases (e.g., cancer, neurodegenerative diseases).

ML121 is a selective and potent VIM-2 inhibitor with an IC50 of 54 nM and a Ki of 148 nM. ML121 shows inactive in IMP-1 and TEM-1 beta-lactamase assays. ML121 can potentiate the antibiotic activity of Imipenem in VIM-2 transformed E.coli.

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].

NCGC00685960 is a Nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 < 10  nM. NCGC00685960 has potent antitumor activity. NCGC00685960 increases H3K27 trimethylation levels in ovarian cancer cells and inhibits α-SMA expression in NNMT-expressing ovarian fibroblasts. NCGC00685960 reduces 1-MNA levels, reverses SAM and H3K27 hypomethylation and significantly impairs collagen contractility in cancer-associated fibroblasts (CAFs). NCGC00685960 can be used for cancers research.

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.