A potent, selective inhibitor of HIV integrase (IC50=8-15 nM) with potent antiviral activity in cell culture and good pharmacokinetic properties.

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.

IC8 is an ionizable cationic lipid. It has been used in combination with other lipids for the formation of lipid nanoparticles (LNPs). Immunization with severe acute respiratory coronavirus 2 (SARS-CoV-2) spike glycoprotein mRNA in IC8- and manganese-containing LNPs induces IgG responses to SARS-CoV-2 Delta and Omicron variants in mice.1 Administration of mRNA encoding B7-H3 X CD3 bispecific T cell engaging (BiTE) antibodies in IC8-containing LNPs reduces tumor growth in MV4-11 and A375 mouse xenograft models.

PAANIB-1 is a brain-penetrant PAAN/MIF nuclease inhibitor that prevents neurodegeneration that prevents neurodegeneration induced by α-syn PFF, AAV-α-syn overexpression, or MPTP intoxication in vivo.

VL285 is a potent VHL ligand, degrading HaloTag7 fusion proteins.

E3 ligase Ligand-Linker Conjugates 17 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

VH032-linker 5 is a derivative of the proteolysis-targeting chimera technology (PROTAC) for PROTAC research and development; by incorporating an E3 ligase ligand and an alkyl C4 linker with terminal carboxylic acid, it is ready for conjugation to a target protein ligand.

MS4078 is a novel PROTAC (degrader) of ALK, potently decreases cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells (DC50=11 nM).

MZ1 is a PROTAC that tethers JQ1 to a ligand for the E3 ubiquitin ligase VHL, triggers, induces degradation of the BET bromodomain BRD4.

A potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays.

JQ-35, (S)- is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins with potential antineoplastic activity.

CW4142 (CW 4142) is a small molecule SC4MOL inhibitor that enhances oligodendrocyte formation.

PMX53 (Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)) is a potent C5a receptor (CD88) antagonist with IC50 of 20 nM, also is an agonist for Mas-related gene 2 (MrgX2) in human mast cells; PMX-53 (10 nM) inhibited C5a-induced Ca(2+) mobilization in HMC-1 cells, but at higher concentrations (>30 nM) it caused degranulation in LAD2 mast cells, CD34(+) cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2; inhibits zymosan-, carrageenan-, LPS- and antigen-induced hypernociception in rats.

Maytansinoid DM4, a chemical derivative of maytansine, is a potent and selective cytotoxic agent with promising anticancer properties. Anticancer properties of maytansinoids have been attributed to their ability to disrupt microtubule function. Maytansin

Sodium taurocholate is a GPBAR1 protein agonist potentially for the treatment of type 2 diabetes and obesity in rats.

GGACK (H-Glu-Gly-Arg-CMK) hydrochloride is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor.

7,4'-Dimethoxy-3-hydroxyflavone is an orally active PAR4 antagonist. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation with an IC50 of 1.4 μM. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation and PAR4 signaling pathways, including NF-κB, Ca2+/protein kinase C, Akt, ERK and p38. 7,4'-Dimethoxy-3-hydroxyflavone prevents vascular PAR4 expression, endothelial dysfunction and ameliorates oxidative stress in Streptozotocin (STZ)-induced diabetic mice. 7,4'-Dimethoxy-3-hydroxyflavone prevents thrombosis in mice without affecting bleeding time[1][2].

Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X. Tecarfarin has the antithrombotic activity .

EVT0185 is an orally active ATP citrate lyase (ACLY) inhibitor. EVT0185 is converted to a CoA thioester in the liver by SLC27A2 and interacts with the CoA-binding site of ACLY. EVT0185-CoA inhibits ACLY activity with an IC50 of 2.5 μM. EVT0185 can phenocopy the immune and antitumour effects of genetic ACLY deletion. EVT0185 can increase tumour-infiltrating B cells and chemokine CXCL13 levels. EVT0185 can be used for the research of cancer, such as hepatocellular carcinoma (HCC).

JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC50 values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity.

Conophyllidine, a bisindole alkaloid, is a selective M2 polarization inhibitor. Conophyllidine inhibits histone acetylation by targeting the histone acetyltransferase domain of the P300/CBP proteins. Conophyllidine inhibits IL-4-induced arginase with an IC50 of 0.31 μM. Conophyllidine effectively induces a phenotypic switch in tumor-associated macrophages (TAMs) from an anti-inflammatory to an inflammatory type, thereby enhancing cytotoxic CD8+ T cell recruitment and functionality within the tumor microenvironment. Conophyllidine can be used for the study of TAMs.

Allotrap 07 is a synthetic peptide composed of residues 75-84 of HLA-B7, a class I MHC molecule. Allotrap 07 combined with Cyclosporin A induces donor-specific tolerance in rat cardiac allografts, significantly prolonging graft survival.

FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a Kd of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as 177Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with 111In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.

Hydroxylamine is a selective Monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxylamine is a intermediate of nitrogen cycle in aerobic ammonium oxidizers microorganisms, such as ammonium oxidizing bacteria (AOB), ammonium oxidizing archaea (AOA) and complete ammonium oxidizing bacteria (comammox). Hydroxylamine impacts NO and N2O emissions by aerobic ammonium oxidizers microorganisms and inhibits nitrite oxidizing bacteria (NOB) activity.

YTK-1305 is a p62 ligand compound that promotes cellular autophagy.

DBM-819 is a reversible inhibitor of H⁺/K⁺-ATPase (H+/K+-ATPase), with an IC50 value of 5 μM. DBM-819 can reversibly block gastric acid secretion by inhibiting the proton pump in the gastric mucosa. It shows significant protective effects against duodenal ulcers induced by Cysteamine, gastric ulcers induced by Indomethacin, and gastric ulcers induced by Aspirin, with EC50 values of 6, 3.1, and 4 mg/kg respectively. DBM-819 can be used in ulcer prevention research.

KI-TOX-A3 is a selective protein-protein interaction (PPI) inhibitor targeting TOX protein (with an IC50 value of 0.51 μM for TOX-KAT7 interaction). KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reversing CD8+ T cell exhaustion and inhibiting T-cell acute lymphoblastic leukemia (T-ALL) cell proliferation. KI-TOX-A3 is promising for research of hematological tumors (e.g., T-ALL).

PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC is an ADC linker that can be combined with the TLR7/8 agonist for the synthesis of a linker-payload conjugate.

(R)-thioxo-Dxd is a Camptothecin derivative. (R)-thioxo-Dxd can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. (R)-thioxo-Dxd can be used for research on tumors with high HER2 or TROP2 expression.

thioxo-Dxd is a Camptothecin derivative. thioxo-Dxd can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. thioxo-Dxd can be used for research on tumors with high HER2 or TROP2 expression.