GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase with Ki value of 0.5 nM.

M-MoDE-A (2) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).

D-MoDE-A (1) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).

VRK-IN-1 is a potent and selective inhibitor of vaccinia-related kinases 1 (VRK1), with an IC50 of 150 nM. VRK1 is human Ser/Thr protein kinases associated with increased cell division and neurological disorders.

Olorofim (F901318) selectively inhibits fungal dihydroorotate dehydrogenase (DHODH), a key enzyme in the pyrimidine biosynthesis pathway. Olorofim (F901318). Olorofim exhibits excellent activity against A. fumigatus and other Aspergillus spp.

AUR1545 is a selective degrader of KAT2A and KAT2B. AUR1545 can be used in the cancer research, including studies on AML (Acute myeloid leukemia), SCLC (Small-cell carcinoma), and NEPC (Neuroendocrine Prostate Cancer).

(3S) ALG-05 is a potent pan-inhibitor of gut microbia tryptophan-indole-lyases (TILs, E.C. 4.1.99.1), exhibits inhibitory activity across TILs with Ki of 7-11 uM.

Sitagliptin, also known as MK-0431, is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts. Sitagliptin is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.

OV329 (OV 329) is a highly potent inactivator of gamma-aminobutyric acid aminotransferase (GABA-AT) with Ki of 9.69 uM.

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs used as an anti-inflammatory and immunosuppressant.

Novel Sirtuin1 Activator, Down-Regulating Sclerostin and Rescuing Ovariectomy-Induced Bone Loss

ARC39 is acid sphingomyelinase inhibitor (IC50 =20 nM).

Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.

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

Secreted frizzled-related protein-1 (sFRP-1) modulaitor

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.

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.

CLinDMA, a cationic lipid known to potentially trigger inflammatory responses, is utilized in the synthesis of LNP201. This liposome-based assembly is specifically designed for the systemic delivery of siRNA.

QC-01-175 is a hetero-bifunctional molecule designed to engage both tau and Cereblon (CRBN) to trigger tau ubiquitination and proteasomal degradation (tau PROTAC).QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal cell models, with minimal effect on tau from neurons of healthy controls.QC-01–175 also rescued stress vulnerability in FTD neurons, phenocopying CRISPR-mediated MAPT-knockout.

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

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.

PEG-8 laurate is a single chain surfactant. PEG-8 laurate reduces the skin barrier, and acts as a penetration enhancer. PEG-8 laurate can be used to synthesize elastic vesicles.

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

Novel selective NaV1.7 inhibitor, blocking the extracellular vestibule of the channel with an IC50 of 72 nM and greater than 200-fold selectivity over off-target sodium channel isoforms, NaV1.1-1.6 and NaV1.8