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.

RMC-5127 is an orally active and brain-penetrant mutant-selective tri-complex RASG12V inhibitor. RMC-5127 non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages RASG12V(ON) to form a high-affinity tri-complex, sterically inhibiting RAS binding . RMC-5127 inhibits the RAS pathway in KRASG12V mutant cancer cells, reducing cell proliferation and inducing apoptosis. RMC-5127 is promising for research of cancers with RAS mutations, such as non-small cell lung cancer.

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.

ST1072 is a dual inhibitor of CerS4 and CerS6. ST1072 significantly reduces the ability of murine T cells to proliferate and produce IFN-γ. ST1072 can be used for hematologic malignancies research.

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).

Jun6504 is an enterovirus 2C inhibitor. Jun6504 shows potent and broad-spectrum antiviral activity against multiple strains of EV-D68 (EC50 = 250 nM), EV-A71 (EC50 = 502.4 nM), and CVB3 (EC50 = 1049 nM). Jun6504 improves paralysis score and weight gain in a neonatal mouse model of EV-D68 infection. Jun6504 reduces viral titers in the spinal cord and the infected quadriceps muscle. Jun6504 can be used for EV-D68 antiviral research.

Rilpivirine(R 278474, TMC 278) is a type of anti-HIV medicine called a non-nucleoside reverse transcriptase inhibitor (NNRTI).

MSG011 is a potent, pan AMPK isoform activator with EC50 of 140.4 nM, 248.9 nM, 553.4 nM, and 472.9 nM for α1β1γ1, α1β2γ1, α2β1γ1, and α2β2γ1, respectively.

STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a Kd value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer.

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.

GHP-88309 (GHP88309) is a non-nucleoside, broad-spectrum allosteric inhibitor of paramyxovirus polymerase with EC50 of 0.9 uM against HPIV3-JS RdRP.Demonstrates highly potent antiviral potency against HPIV3-JS and clinical isolates HPIV3-9R4 and HPIV3-10L3 in the primary cell/virus isolate system (EC50=0.07-0.08 uM), without cytotoxicity.GHP-88309 targets a conserved microdomain in the L protein, inhibiting de novo RNA synthesis.GHP-88309 is efficacious in well-differentiated human airway epithelium cultures grown at air-liquid interface (3D-ALI-HBTEC).GHP-88309 (150 mg/kg b.i.d.) is orally efficacious in HPIV disease surrogate model.GHP-88309 possesses unusual broad-spectrum activity against diverse paramyxoviruses including respiroviruses (i.e. HPIV1 and HPIV3) and morbilliviruses (i.e. MeV).

H052 is a selective Staphylococcus aureus α-hemolysin (Hla) inhibitor. H052 binds to Hla monomers, disrupts the interaction with host cell membranes to block pore formation, inhibiting calcium ion influx, cytotoxicity, and inflammatory responses. H052 exhibits potency (EC50=30 nM in U937 cells) against Hla-induced calcium influx. H052 is promising for research of lung infections caused by S. aureus.

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

INS018_055 (INS018-055) a selective small-molecule TRAF2- and NCK-interacting kinase (TNIK) inhibitor with Kd value of 4.32 nM and IC50 of 31 nM, inhibits TGF-β-induced α-SMA protein expression in MRC-5 cells with IC50 of 27.14 nM.

5-Diazomethane quinoxaline is a novel derivatization reagent. 5-Diazomethane quinoxaline is used for the detection of phosphorylated metabolites.

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

BCL6-IN-3 (example 20a) is a B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity, extracted from patent WO2018215801A1. BCL6-IN-3 (example 20a) exhibits a GI50 of 70 nM in SU-DHL4 cells.

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

(S)-SCH-23390 (hydrochloride) is the S-enantiomer of SCH-23390. SCH-23390 is a dopamine D1-like receptor antagonist (with Ki values of 0.2 nM and 0.3 nM for the D1 and D5 receptor subtypes, respectively).

SCH-23390 is a dopamine D1-like receptor antagonist (with Ki values of 0.2 nM and 0.3 nM for the D1 and D5 receptor subtypes, respectively). SCH-23390 can shorten the latency period for cocaine-induced lever pressing behavior in rats. SCH-23390 can also eliminate generalized seizures caused by chemical convulsants, such as arecoline and strychnine, and is used in research on neurological disorders related to the dopamine system.

Novel, Potent and Selective Histone Methyltransferase SET7 Inhibitor

A potent, selective, allosteric CCR2 antagonist with binding IC50 of 5.1 nM.