AZ3976 is a selective PAI-1 inhibitor that exhibits potent profibrinolytic effects, with IC50 values of 26 μM (chromogenic assay) and 16 μM (plasma clot lysis assay). Unlike conventional inhibitors, it does not target active PAI-1 but instead binds reversibly to the latent form, accelerating the transition of active PAI-1 to its inactive state.

WQ-2101 (WQ2101, PKUMDL-WQ-2101) is a specific, allosteric inhibitor of PHGDH with IC50 of 34.8 uM (WT PHGDH), shows dramatically reduced potenecy for mutants R134A (IC50 =141 uM) and K57AT59A (IC50=128 uM).

ZLD1039 is a novel, orally active EZH2 inhibitor demonstrating high selectivity and potency. It effectively suppresses PRC2 enzymatic activity across wild-type EZH2 (IC50 = 5.6 nM) and mutant forms (Y641F: 15 nM; A677G: 4.0 nM), while exhibiting significant anti-tumor and anti-metastatic effects in breast cancer models.

Novel Inhibitor of Monoubiquitinated Proliferating Cell Nuclear Antigen (PCNA), inhibiting Repair of Interstrand DNA Crosslink, enhancing DNA Double-strand Break, and sensitizing Cancer Cells to Cisplatin.

LY305 is a potent non-steroidal SARM exhibiting high androgen receptor binding affinity (Ki = 2.03 nM) and strong agonist activity in C2C12 cells (EC50 = 0.499 nM), demonstrating its selective modulation capabilities.

corticotropin releasing factor (CRF) antagonist.

Protonstatin-1 is a selective small-molecule inhibitor of PM H+ -ATPase activity that inhibits auxin transport.

SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).

EX229 is a small molecule AMPK activator that dose-dependently increases AMPK activity of α1-, α2-, β1- and β2-containing complexes at 50 uM

Sufugolix(TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for affinity and in vitro inhibition, respectively).

NNK is a procarcinogen, a major tobacco-specific toxicant that inhibits the expression of lysyl oxidase, a tumor suppressor.

CYM 50769 is a small-molecule, selective NPBWR1 antagonist that effectively inhibits NPW-23-stimulated proliferation in ATDC5 cells, making it a valuable tool for studying endochondral ossification processes.

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

SSAA09E2 is a novel inhibitor of SARS-CoV replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2)

FPPS-IN-11 represents a novel class of non-bisphosphonate inhibitors that allosterically target farnesyl pyrophosphate synthase (FPPS), demonstrating potent activity with an IC50 value of 200 nM.

Novel inhibitor of TRPM6, promoting mesoderm and definitive endoderm differentiation of human embryonic stem cells through alteration of magnesium homeostasis

NSC-2805 is a WWP2 ubiquitin ligase inhibitor.

VK-28 is a brain-penetrant iron chelator that effectively suppresses mitochondrial lipid peroxidation, whether induced by Fe/ascorbate or occurring basally (IC50 = 12.7 μM). It demonstrates notable neuroprotective activity in ICV-6-OHDA models, making it a promising candidate for Parkinson’s disease and related neurodegenerative disorder research.

Tradipitant (VLY-686) is a selective neurokinin-1 (NK-1) receptor antagonist with potential therapeutic applications.

Azo-Resveratrol is an analog of Resveratrol used as a potent tyrosinase inhibitor.

KYN-101 (KYN101) is a potent, selective synthetic antagonist of aryl hydrocarbon receptor (AHR) with IC50 of 22 nM in human HepG2 DRE-luciferase reporter assay and 23 nM in murine Hepa1 Cyp-luc assay.KYN-101 reverses IDO/TDO-mediated tumor progression and improves the efficacy of PD-1 blockade in B16 IDO tumor-bearing mice, as well as CT26 colorectal cancer model expressing endogenous high levels of IDO.

K-975 is a first-in-class TEAD inhibitor, directly inhibiting YAP/TAZ-TEAD protein-protein interaction and showing a potent anti-tumor effect in malignant pleural mesothelioma. K-975 was covalently bound to an internal cysteine residue located in the palm