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.

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).

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.

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)

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.

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

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.

SKI-178 is a potent, specific, non-lipid SphK1 inhibitor with Ki of 1.33 uM, displays no significant activity for SphK2 (IC50>25 uM).

SW-100 (SW100) is a potent, selective, brain penetrable HDAC6 inhibitor with IC50 of 2.3 nM, displays >1,000-fold selectivity over all other class I, II, and IV HDAC isoforms.

Adaphostin is a novel activator of Fas-mediated death pathway in Bcr/Abl-positive leukaemia.

M351-110 is a V-domain immunoglobulin suppressor of T-cell activation (VISTA) agonist that enhances immune responses, making it a promising candidate for cancer immunotherapy research.

ML202 represents a selective allosteric modulator of human pyruvate kinase M2 (hPK-M2) that specifically enhances phosphoenolpyruvate (PEP) binding cooperativity without significantly affecting adenosine diphosphate (ADP) binding kinetics.

Phevamine A is a phytotoxic secondary metabolite produced by Pseudomonas syringae. This small molecule compound facilitates bacterial proliferation through its ability to suppress host plant defense mechanisms.

VU-29 (DPAP) is a potent, selective and allosteric potentiator of rat mGlu5 receptor with EC50 of 9 nM, displays >50-fold selectivity over mGlu1 and mGlu2 receptor (EC50=557 nM and 1.51 uM).

Hydrophobic inducer of the degradation of stabilized proteins, degrading HaloTag2 fusion proteins

ARN-21934 is a novel potent and highly selective inhibitor for human topoisomerase II α over β.

AGI-001 is an orally bioavailable, competitive antagonist of 5-HT1A/1B receptors with reversible binding properties. This compound also functions as a partial agonist at β-adrenergic receptors, making it a valuable pharmacological tool for investigating neurological disorders.

ElteN378 is a selective FKBP12e inhibitor with potential therapeutic applications in neurodegenerative disorders and oncology. This compound shows particular relevance for research involving Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), as well as various proliferative disorders and malignancies.

GSK3987 functions as a dual agonist for both LXRα and LXRβ nuclear receptors, demonstrating potent activation with EC50 values of 50 nM (LXRα-SRC1) and 40 nM (LXRβ-SRC1). This compound effectively upregulates key metabolic regulators ABCA1 and SREBP-1c, while simultaneously promoting cholesterol efflux from cells and stimulating intracellular triglyceride deposition.

L82-G17 is a selective, uncompetitive inhibitor that specifically targets DNA ligase I (Lig I). This compound uniquely blocks the final stage of the ligation process by interfering with phosphodiester bond formation. Due to its specific mechanism of action, L82-G17 serves as a valuable molecular probe for studying ligase catalytic activity.

LASV inhibitor 3.3 (LAMP1 inhibitor 3.3) is a specific inhibitor of Lassa fever virus (LASV, IC50=1.8 uM), inhibits LASV GP-mediated infection and cross-links to the LASV receptor, LAMP1, in cells; does not inhibits the GP-mediated infection of LCMV, LuJo

SSAA09E3 is a potent viral entry inhibitor that effectively blocks SARS-CoV infection. In cellular assays, it demonstrates inhibitory activity against SARS/HIV pseudotyped viruses in 293T cells (EC50 = 9.7 μM) and shows even greater potency against authentic SARS-CoV in Vero cells (EC50 = 0.15 μM).

STING-IN-2 (C-170) is a covalent-binding small molecule that potently suppresses STING activity. It demonstrates effective inhibition against both murine (mmSTING) and human (hsSTING) variants, making it a valuable tool for investigating autoinflammatory disorders.

PKZ18 is a novel antibiotic that effectively suppresses bacterial growth, exhibiting MIC values ranging from 32 to 64 μg/mL against a broad spectrum of Gram-positive bacteria. Its mechanism involves the selective inhibition of glycyl-tRNA synthetase mRNA transcription and translation in vivo. PKZ18 specifically targets stem I specifier loops in Gram-positive bacteria, disrupting T-box-mediated transcriptional read-through of downstream genes. By interfering with codon-anticodon recognition, it blocks essential tRNA binding and demonstrates a high barrier to resistance development.