VA-012 is a potent, selective 5-HT2C receptor positive allosteric modulator (PAM) that exhibits dose-dependent potentiation of 5-HT efficacy with EC50 of 16 nM.

NQTrp, an aromatic naphthoquinone-tryptophan hybrid molecule, an inhibitor of the aggregation of the tau protein with generic anti-amyloidogenic effects. NQTrp inhibits the in vitro aggregation of hexapeptide (41GCWMLY46 within the N-terminus of γD-crystallin) as well as full-length γD-crystallin.

L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM respectively.

MS-0124 is a potent and selective inhibitor of G9a-like Protein (GLP) lysine methyltransferase with IC50 of 13 nM, shows >30-fold selectivity for GLP over G9a and other methyltransferases..

SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC50 of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC50 of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity.

CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.

IL-4-inhibitor-1 (compound 52) is an IL-4 inhibitor, with an EC50 of 1.81 µM.

JNJ-40355003 is a potent and selective atty acid amide hydrolase (FAAH) inhibitor.

GSK-626616 is a dual-specificity tyrosine-regulated kinase (DYRK3) inhibitor with an IC50 of 0.7 nM which is a potential therapy for the treatment of anemia.

Sulfanitran is a sulfonamide antibiotic which is used in the poultry industry. It is a component of Novastat, Polystat, and Unistat, brand names of feed additives for chickens used to control Coccidioides spp.

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research.

BMP signaling agonist sb4 is a small molecule BMP signaling agonist with EC50 of 73.6 nM, enhances the efficacy of BMPs and activates endogenous BMP4 target genes.

DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM.

S-181 (S 181) is a specific small-molecule activator (modulator) of β-glucocerebrosidase (GCase) with AC50 of 1.49 uM and a maximum activation of 780%.

Olorofim (F901318) selectively inhibits fungal dihydroorotate dehydrogenase (DHODH), a key enzyme in the pyrimidine biosynthesis pathway. Olorofim (F901318). Olorofim exhibits excellent activity against A. fumigatus and other Aspergillus spp.

Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM). Zotatifin induces cell apoptosis.

GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.

GSK864 is a potent and selective inhibitor of mutant IDH1. GSK864 inhibits IDH1 mutants R132C/R132H/R132G with IC50 values of 9/15/17 nM, respectively, and is moderately selective over wild-type IDH1 and IDH2 mutants/wild-type. Treatment of R132C IDH1 mutant HT-1080 cells for 24 hours with GSK864 results in a dose-dependent reduction of 2-hydroxyglutarate (2-HG), which is not observed with GSK990, a structurally similar compound which is inactive as an IDH1 inhibitor. GSK864 has been shown to be selective in vitro for IDH1 over other classes of proteins (7TMs, ion channels, kinases) and chemoproteomic studies with GSK321, an analog of GSK864, confirm selective binding of IDH1 by this chemical series. GSK864 has a pharmacokinetic profile suitable for in vivo studies.

HOIPIN-8 (HOIP inhibitor-8) is a potent chemical inhibitor of linear ubiquitin chain assembly complex (LUBAC, IC50=11 nM), specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the NF-kB pa

Vevorisertib (ARQ 751) (trihydrochloride) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib (trihydrochloride), as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations.

M3541 (M 3541) is a novel potent, selective and ATP-competitive ATM kinase inhibitor with IC50 of 0.25 nM (ATP, 10 uM).M3541 displays a good margin of selectivity (>60-fold) against the closely related PIKK family members with DNA-PK, PI3K isoforms, mTOR, and ATR.M3541 inhibits the phosphorylation of ATM as well as its cellular substrates CHK2, KAP1, and p53 in a concentration-dependent manner in A549 cells.M3541 inhibits double strand break repair and sensitizes cancer cells to radiation.M3541 suppresses ATM pathway activity and potentiates radiation efficacy in xenograft models of human cancer, synergizes with topoisomerase and PARP inhibitors.

RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.

X-Neu5Ac (sodium) is a substrate for chromogenic assay of neuraminidase activity in bacterial expression systems; with a Km of 0.89 mM for neuraminidase.

AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.

SPEN-IN-1 (compound X1) is an inhibitor of SPEN which is a protein factor with a Kd value of 47 nM. SPEN-IN-1 has high selectivity for RepA, a 431-nucleotide domain in Xist (a non-coding RNA prototype) that comprises 8.5 units of a GC-rich motif responsible for gene silencing.

AZ13705339 is a potent, selective PAK1 inhibitor with IC50 of 0.33 nM, displays 14-, 470-, 4100- and 2600-fold selectivity over Src, FGFR1, KDR and PAK4.

Ifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Ifidancitinib can be used in studies of allergies, asthma and autoimmune diseases.

MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease.

Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.

MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists.