​​B355252​​ is a novel neuroprotective compound that demonstrates dual mechanisms of action to support neuronal survival and regeneration.

​​MK-0343 (MRK-409)​​ represents a novel class of benzodiazepine-site ligands with unique GABAA receptor subtype selectivity.

​​CDE-096​​ is a highly effective plasminogen activator inhibitor-1 (PAI-1) antagonist with broad-spectrum inhibitory activity.

​​2-Hydroxysaclofen​​ is a selective and pharmacologically active antagonist of the GABAB receptor subtype, demonstrating multiple functional effects in neuropharmacological studies.

​​GB1107​​ is a novel small-molecule inhibitor specifically designed to target galectin-3 (Gal-3), demonstrating high binding affinity and oral bioavailability.

​​RO5263397​​ is a novel, orally active trace amine-associated receptor 1 (TAAR1) agonist demonstrating high potency and species-specific activity.

A competitive inhibitor of HMG-CoA reductase that acts as a lipid-lowering agent for prevention of events associated with cardiovascular disease..

Magnesium ionophore III is an onophore used in solvent polymeric membrane electrodes for the assay of Mg2+ activities in blood serum in vitro.

ICA135 (ICA-135, ICA 135) is a broad-spectrum inhibitor against human enteroviruses that inhibits Coxsackievirus A10 (CV-A10) replication in RD cells with IC50 of 1.446 uM.

ZHAWOC8697 is a small molecule dual inhibitor of sentrin-specific protease SENP1 and SENP2 with IC50 of 8.6 and 2.3 uM, respectively, a valuable tool for the study of SUMOylation processes.

EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer.

HC-258 is a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells. Co-crystallization with hTEAD2 confirmed that HC-258 binds within TEAD’s PA pocket, where it forms a covalent bond with its cysteine.

Oligopeptide-10, also known as granactive oligopeptide-10, is a synthetic bio-active peptide composed of 15 amino acids. it can help manage acne-causing bacteria, both on its own and in conjunction with anti-acne superstar exfoliant salicylic acid.

FDW028 is a potent and highly selective small-molecule inhibitor of fucosyltransferase 8 (FUT8) with binding KD value of 5.486 uM, displays no affinity against other FUTs, shows potent anti-CRC activities.

GLPG3667 is an oral, reversible, and selective tyrosine kinase 2 (TYK2) inhibitor. It is being developed to treat inflammatory and auto-immune diseases. Biochemical assays showed that GLPG3667 displayed nanomolar potency on TYK2 with a selectivity over other JAK kinases >3-fold. In human PBMC, GLPG3667 showed comparable potency on the IFNα and IL-23 pathways (around 50 nM). Selectivity for TYK2 on the IFNα pathway was >14-fold and >19-fold toward the IL-2 and GM-CSF pathways in human PBMC and whole blood, respectively. Dermal ear inflammation in a mouse model of psoriasis driven by IL-23 was prevented by GLPG3667 with a minimal effective dose of 3 mg/kg given orally once daily. This effect was associated with a decrease in neutrophil infiltration and STAT3 phosphorylation at sites of inflammation. In healthy HV, GLPG3667 completely inhibited IFNα-induced STAT1 and STAT3 phosphorylation but did not impact IL-2- and GM-CSF-induced STAT5 phosphorylation.

ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.

ML162 is a covalent inhibitor that specifically targets ​glutathione peroxidase 4 (GPX4), a key regulator of ferroptosis. This compound exhibits ​selective cytotoxicity against cancer cell lines harboring ​mutant RAS oncogenes, making it a promising candidate for precision oncology.

Pyrinuron is an inhibitor of NAMPT and NMNAT2.Pyrinuron is used as a model compound in studies of urea derivatives and their reactivity.Research has explored the effects of this compound on insulin-producing beta cells, providing insights into diabetes mechanisms.Although not used therapeutically, this compound’s ability to selectively destroy beta cells has implications for understanding and potentially treating type 1 diabetes.

Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription. Lycorine is also a melanoma vasculogenic inhibitor. Lycorine can be used for the study of prostate cancer and metabolic diseases.

Mifepristone (RU-486) is a potent steroidal antagonist exhibiting subnanomolar affinity for progesterone receptors (PR IC₅₀ = 0.2 nM) and nanomolar activity against glucocorticoid receptors (GR IC₅₀ = 2.6 nM). This dual-receptor modulator competitively blocks endogenous hormone binding while inducing distinct conformational changes that prevent coactivator recruitment, demonstrating differential antagonism between PR and GR signaling pathways.

XEN-602 represents a breakthrough in DMT1 pharmacology as a picomolar-range inhibitor of divalent metal transporter 1 (SLC11A2), demonstrating unprecedented selectivity for manganese transport blockade (IC₅₀ = 300 pM in HEK293 cells). This structurally optimized small molecule achieves complete suppression of DMT1-mediated Mn²⁺ uptake while maintaining exceptional target specificity, as evidenced by minimal interference with other metal transporters. Its unmatched potency enables precise interrogation of DMT1's physiological roles and therapeutic exploration for manganese dysregulation disorders.

DOCK5-IN-C21 functions as an allosteric inhibitor targeting the guanine nucleotide exchange factor DOCK5, effectively modulating its activity through a non-competitive mechanism.

VU0466551 is a targeted activator that specifically modulates homomeric G protein-gated inwardly rectifying potassium (GIRK1) channels, demonstrating its selectivity for this ion channel subtype.

DG-172 is a cutting-edge compound designed as a selective ligand for PPARβ/δ, exhibiting remarkable binding affinity with an IC50 value of 27 nM. It demonstrates robust inverse agonistic activity, positioning it as a promising candidate for research targeting PPARβ/δ signaling pathways.

Cediranib maleate (AZD-2171 maleate) is a highly effective, orally administered inhibitor targeting VEGFR with remarkable potency. It demonstrates IC50 values of less than 1 nM for Flt1, below 3 nM for KDR, 5 nM for both Flt4 and PDGFRα, 36 nM for PDGFRβ, and 2 nM for c-Kit, showcasing its broad inhibitory activity across multiple kinase targets.

BHC, a small-molecule inhibitor of skeletal muscle myosin, effectively suppresses muscle activity by targeting myosin function without altering membrane currents. This compound emerges from a screening process aimed at identifying molecules capable of modulating muscle movement through myosin inhibition. By specifically inhibiting myosin, BHC provides a unique mechanism for controlling muscle contractions while maintaining the integrity of cellular electrical properties.

LTX-401 is a novel oncolytic amino acid derivative that specifically targets the Golgi apparatus, demonstrating significant potential in cancer therapy. In vitro studies reveal that LTX-401 effectively reduces the viability of various tumor cell lines, exhibiting cytotoxic activity across a range of concentrations. Notably, it shows the highest potency against the human malignant melanoma cell line MDA-MB-435S (IC50 = 13.5 μM) and the lowest activity against the human hepatocellular carcinoma cell line HEPG2 (IC50 = 35.4 μM). For other cell lines, the IC50 values fall within a narrow range of 19-32 μM. Importantly, LTX-401 does not induce hemolysis in red blood cells at concentrations effective for cancer cell death, with hemolytic activity only observed at much higher concentrations (400 μg/mL = 1087 μM). Additionally, LTX-401 demonstrates cytotoxicity against non-malignant cell lines, including HUV-EC-C endothelial cells, HaCat keratinocytes, and MRC-5 fibroblasts, suggesting a broad but selective mechanism of action.

Edonerpic, also known as T-817, is a neuroprotectant. Edonerpic is a candidate therapeutic agent for Alzheimer's disease that inhibits oxidative stress and nitric oxide-induced neurotoxicity and acts as a neurotrophic factor. Edonerpic protects against MPTP-induced neurotoxicity by blocking lipid peroxidation in the SNc, and imply that this compound may be useful for treating neurodegenerative disorders related to oxidative stress, such as Parkinson's disease.

DC-Chol is a cationic cholesterol derivative. DC-Chol, as a component of lipoplexes with DOPE, has been used for transfection of mRNA into A549 cells without affecting cell viability. Incubation of DC-chol/DOPE liposomes or lipoplexes with human whole blood has no effect on neutrophil elastase or β-thromboglobulin levels or the number of platelets and red and white blood cells, indicating hemocompatibility. DC-Chol has also been widely used in the synthesis of liposomes for the delivery of siRNA, DNA, and chemotherapeutic agents into cells and mice.

TAMRA-PEG4-NHS ester is a TAMRA red fluorescent dye derivative containing an NHS ester group which can be used to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.