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.

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.

BMY 20844 is an orally active platelet cAMP phosphodiesterase inhibitor with anti-thrombosis activity. BMY 20844 can elevate cAMP levels and activate protein kinase in platelets. BMY 20844 can be used for the research of cardiovascular disease.

MDOLL-0286 is a selective Poly(ADP-ribose) Glycohydrolase (PARG) (ARH3) inhibitor with an IC50 of 2.3μM. MDOLL-0286 can inhibit ARH3’s poly-ADP-ribose hydrolytic activity on cellular substrates. MDOLL-0286 can inhibit DNA damage response. MDOLL-0286 can be used for the research of cancer .

PARP14 inhibitor 2 (Compound 3) is an orally active and highly selective PARP14 inhibitor with an IC50 value of <30 nM. PARP14 inhibitor 2 inhibits the mono-ADP-ribosyltransferase activity of PARP14 and regulates IFN-γ and IL-4 signaling, reversing protumor macrophage polarization and inhibiting anti-tumor inflammatory responses. PARP14 inhibitor 2 is promising for research of PARP14-related diseases such as tumors, atopic dermatitis and autoimmune diseases.

Otviciclib (Compound 86) is a CDK inhibitor. Otviciclib has potent anti-proliferative activity against solid tumor cells (such as HCT116, NCIH82 and DU145 cells) with no significant toxicity to normal cells, and effectively induces the G2/M phase cells arrest and apoptosis. Otviciclib has a broad-spectrum anticancer activity, such as colon, pancreatic and lung cancer.

AXT-914 is a Calcium-sensing receptor (CaSR) inhibitor. AXT-914 has antiviral activity against the coronavirus HCoV 229E and SARS-CoV2. AXT914 reduces cytosolic calcium signalling activity of CaSR mutations. AXT-914 can be used for Bartter syndrome type 5 and autosomal dominant hypocalcemia (ADH) and coronavirus infections research.

PSD-506 (RO 3202904) is a muscarinic M2/M3 antagonist. PSD-506 has the potential to be used in studies of bladder overactivity and urinary incontinence.

MT-21 is an Apoptosis inducer and adenine nucleotide translocase inhibitor. MT-21 induces Apoptosis by activating JNK via the Krs/MST protein. MT-21 activates caspase-3 via caspase-9. MT-21 induces the release of cytochrome c. MT-21 can be used in the research of tumors.

BRL 55834 is an orally and potent potassium channel activator. BRL 55834 exhibits great bronchodilator potency but reduces tendency to lower arterial blood pressure. BRL 55834 has the potential to use as a bronchodilator.

RWJ 29009 is a highly selective ATP-sensitive potassium channel agonist. RWJ 29009 activates potassium channel in vascular smooth muscle cells, promoting potassium efflux and membrane hyperpolarization to induce coronary and peripheral vasodilation. RWJ 29009 is promising for research of cardiovascular diseases such as acute myocardial ischemia and hypertension.

LRH-0003 is an inhibitor of the Macrodomain 1 (Mac1) of nonstructural protein 3 (NSP3) from SARS-CoV-2, with an IC50 value of 1.7 μM. LRH-0003 can be used for the research antiviral infection targeting SARS-CoV-2.

GNE-5152 is an orthosteric SARM1 base-exchange (BE) inhibitor. GNE-5152 sustainably activates SARM1 at subinhibitory concentrations under mildly activating conditions, and this synergistic adverse effect increases NAD consumption, induces axon degradation and neurodegeneration and releases neurofilament-light (NfL) in cortical neurons. GNE-5152 can be used for neurodegenerative diseases research.