Novel MmpL3 inhibitor

Anethole trithione, a sulfur heterocyclic choleretic, is a bile secretion-stimulating agent. Anethole trithione enhances salivary secretion and increases mAChRs, and can be used for dry mouth research.

Novel inhibitor of the heat shock protein 70 (Hsp70) with anti-proliferative activity in breast and prostate cancer cells

Dynein2-IN-37 (Ciliobrevin analog 37) is a potent, selective cytoplasmic dynein 2 ATPase activity antagonist with IC50 of 11 uM, shows weak inhibition for dynein 2 (IC50=280 uM).

Syn-TEF1 is a molecule actively enables transcription across repressive GAA repeats that silence frataxin expression in Friedreich's ataxia, license transcription elongation at targeted genomic loci.

DBCO-PEG4-NHS Ester is a PEG derivative containing NHS ester that is able to react specifically and efficiently with primary amines (e.g. the side chain of lysine residues or aminosilane-coated surfaces) at neutral or slightly basic condition to form a covalent bond. The hydrophilic PEG spacer arm improves water solubility and provides a long and flexible connection that minimizes steric hindrance involved with ligation.

Piperaquine phosphate is a bisquinoline antimalarial agent. Piperaquine phosphate can be used in antimalarial research in combination with Artemisinin.

AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice.

NY0128 (NY 0128) is a small molecule neuromedin U receptor 2 (NMUR2) with EC50 of 29.99 uM for hNMUR1 and 10.30 uM for hNMUR2 in intracellular calcium mobilization assays.

NY0116 (NY 0116) is a small molecule neuromedin U receptor 2 (NMUR2) with EC50 of 27.76 uM for hNMUR1 and 13.61 uM for hNMUR2 in intracellular calcium mobilization assays.

A quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine.

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.