VTI-1002 is a potent and specific inhibitor of human (K i = 4.4 ± 2.0 nM) and murine (IC 50 = 179 ± 18 nM) GzmB, with minimal activity (IC 50 > 300 nM) against Cathepsin-G, neutrophil elastase and caspases (−3, −4, −5, −7, −8 and −9). In addition to its high specificity for GzmB, VTI-1002 is retained in murine skin for up to 24 hours and exhibits minimal toxicity in vivo with no observed adverse effects after 30 consecutive days of systemic administration in mice [31]. VTI-1002-mediated GzmB inhibition was first reported to augment type I collagen fibrillogenesis and improve tensile strength in a murine diabetic burn model, notably by preventing decorin cleavage and dermal fibrillar collagen network disorganization.

ABT-719 is a potent bacterial DNA gyrase inhibitor.

ABT-719 is a potent bacterial DNA gyrase inhibitor.

IPA (Inhibitor of Priming Activity) is a small-molecule compound that binds Sec18 (Kd=3.84 uM) and blocks SNARE activation, inhibits vacuole fusion at the SNARE priming stage with IC50 of 50 uM.

IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, no inhibition to group II PAKs (PAKs 4-6).

KB-208 is a phagocytosis inhibitor that improves immune thrombocytopenia (ITP) in mouse models at a dose of 1 mg/kg. KB-208 does not affect other blood parameters and does not elevate serum toxicity biomarkers. KB-208 can be used in immunology research.

Bumadizone is a non-steroidal anti-inflammatory drug (NSAID) and can relieve pain.

Novel influenza A hemagglutinin (HA) fusion inhibitor (EC 50 = 1.9 ± 0.3 μM), preventing HA from transitioning to the postfusion state at pH 5.0

FTT5 is a lipid-like compound for efficient delivery of long mRNAs in vivo.

CX08005 is a competitive PTP1B inhibitor. CX08005 can directly enhance the action of insulin in vivo and in vitro and improve insulin resistance.

Amthamine is a histamine receptor (H1R-H4R) agonist. Amthamine can produce liver congestion and necrosis of liver cells. Amthamine can be used to study the induction effect of H1R-H4 agonist on hepatotoxicity.

SOD1-Derlin-1 inhibitor-1 (compound 56-20) is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor-1 inhibits SOD1G93A-Derlin-1 complex with an IC50 value of 7.11 μM.

Merck-22-6(compound 7) is an allosteric dual Akt1 and Akt2 inhibitor (IC50=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells

Novel, Potent and Selective Histone Methyltransferase SET7 Inhibitor

Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue.

SOD1-Derlin-1 inhibitor 56-59 is a cell-permeable, small molecule inhibitor of SOD1-Derlin-1 interaction, target SOD1 DBR and clearly attenuates the interactions of Derlin-1 with 122 types of SOD1mut in the cell-based co-immunoprecipitation assay.

GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC50s of 26 and 3.2 nM in the β-arrestin and Ca2+ release assay, respectively.

NCRW0005-F05 is a small-molecule inhibitor reported to target the Wnt/β-catenin signaling pathway with activity in vitro. It suppresses β-catenin–dependent transcription in a concentration-dependent manner, with reported IC50 values in the low micromolar range (~1–10 µM) in reporter assays. NCRW0005-F05 reduces expression of Wnt target genes such as c-Myc and cyclin D1, leading to decreased proliferation in Wnt-driven cancer cell models.

ONT-093, also known as OC-144-093, is an orally bioavailable P-glycoprotein pump inhibitor, for the potential reversal of multidrug resistance in patients undergoing cancer chemotherapy. ONT-093 could inhibit P-gp and reverse multidrug resistance at nM concentrations with no effect on paclitaxel pharmacokinetics. OC144-093 is the least non-specifically toxic Pgp inhibitor described to date, with an average cytostatic IC50 of >60 microM in 15 cell types. OC144-093 may represent an ideal candidate for use in enhancement of AED blood-brain barrier penetration.

Etavopivat is a potent, selective, orally bioavailable red blood cell (RBC) pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects.

ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA. ARN19702 has pain relief effects.

KCNQ2/3 activator-1 is an activator of Kv7.2/Kv7.3 (KCNQ2/3) potassium channel. KCNQ2/3 activator-1 has the potential in relieving pain (the main problem from medical treatment) (extracted from patent WO2021113757A1, compound A).

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor.

503O13 is a next-generation, biodegradable lipid nanoparticle (LNP) engineered for highly efficient and targeted siRNA delivery. Designed through rational structure-activity criteria—including optimal tail length (O13), tertiary amines, and a surface pKa ≥5.5—this single-component LNP achieves unparalleled gene silencing with an ultra-low EC50 of 0.01 mg/kg in preclinical models.503O13 outperforms non-degradable counterparts (e.g., C12-200) with improved toxicity profiles—no hepatic necrosis or pancreatic inflammation—while maintaining rapid blood clearance (t1/2: 6 min) and organ-specific accumulation (liver/spleen).

Quorum sensing modulator as a PqsR antagonist

Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.

α-Spinasterol-3-O-β-D-glucoside is a sterol glucoside that can be isolated from the seeds of Momordica cochinchinensis.

Flagelin 22 TFA, a fragment of bacterial flagellin, is an effective elicitor in both plants and algae.

3-O-galloylmucic acid is a natural flavonoid that can be found in Ardisia splendens.

Tectochrysin (Techtochrysin) is one of the major flavonoids of Alpinia oxyphylla Miquel. Tectochrysin inhibits activity of NF-κB.