Non-canonical p38α inhibitor NC-37 (NC-p38i NC-37) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM.

[SER140]-PLP(139-151) is a polypeptide fragment of the lipid protein of myelin.

Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

Gap 27 is a synthetic connexin-mimetic peptide and acts as a gap junction inhibitor. Gap 27 is highly effective in interrupting co-operative cell-cell interactions, such as the synchronous beating of embryonic cardiomyocytes.

Taspoglutide is a glucagon-like peptide-1(GLP-1) agonist for treatment of type 2 diabetes.

DSHN is a novel activator of small heterodimer partner (SHP, NR0B2). DSHN transcriptionally activates SHP mRNA, but also stabilizes the SHP protein by preventing its ubiquitination and degradation.

TVB-2640 is an orally bioavailable fatty acid synthase (FASN) inhibitor, with potential antineoplastic activity.

THK-5470(THK 5470), a monoamine oxidase-B (MAO-B) imaging probe, could be used for neurological diseases study. THK-5470 shows remarkably high binding affinity against MAO-B with an IC50 value of 4.2 nM, low binding affinity against tau with an IC50 value of 4462 nM. THK-5470 has high selective binding property and high affinity (from patent EP2019-846498).

DI-87 ((R)-DI-87) is a highly potent, specific, orally bioavailable deoxycytidine kinase (dCK) inhibitor with IC50 of 3.15 nM.

FT234 (FT-234) is a selective HDAC11 inhibitor.FT234 demonstrated significant reduction in self-renewal stem-like SP cells with 2 uM FT234 or FT895, as well as the formation of vascular networks by SP cells at 5 uM compound treatment.FT234 significantly decreased the mRNA of Sox2 as well as its target genes like HK2 and PDK2 in SPAdh cells.FT234 compound inhibited the growth and viability by 60–80% in both A549 and H1650 cells at 5-10 uM, inhibited the viability of cancer cell lines A549 and H1650 ranged from 4.663–6.594 uM, reduced the viability of chemo-resistant cancer cells as well as chemo-insensitive CSCs.FT234 selectively prevent growth of cancer cells in presence of cancer associated fibroblasts (CAFs).

LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.

(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM.

cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.

3’3’-cGAMP Fluorinated (c-[2'FdGMP]-[2'FdAMP]) is a synthetic analog of cyclic guanosine monophosphate- adenosine monophosphate (cyclic GMP-AMP, cGAMP) with a fluorine atom at 2’ position of the nucleosides. 3’3’-cGAMP is a cyclic di-nucleotide produced by bacteria. It is also referred to as "canonical" cGAMP due the presence of the classical 3’-5’ phosphodiester linkages between the guanosine and the adenosine. It has been reported that cGAMP binds STING (stimulator of IFN genes) and subsequently induces TBK1-IRF3-dependent production of IFN-β [1]. The incorporation of fluorine into biologically active molecules is commonly used in medicinal chemistry to improve their metabolic stability or to modulate physicochemical properties such as lipophilicity [2, 3]. Moreover, the introduction of a fluorine atom can change the biological activities of a molecule. Interestingly, when used at low concentrations in various cellular assays, 3’3’-cGAMP Fluorinated induces higher levels of type I IFNs than does cGAMP. STING ligands such as cGAMP induce type I IFNs and activate interferon stimulated genes (ISG) through IRFs. To facilitate their study, InvivoGen has developed stable reporter cells in two well established immune cell models: THP-1 human monocytes and RAW 264.7 murine macrophages. These cells express a reporter gene (SEAP or Lucia luciferase), under control of an IRF-inducible promoter.

Tat-NR2B9c (NA-1) is a neuroprotective agent.

Selective serotonin reuptake inhibitor

5-HT2 receptor agonist, inhibiting TNF-α-mediated proinflammatory signaling cascades and inflammation via 5-HT2A receptor activation and preventing the development of, and inflammation associated with, acute allergic asthma

Novel Covalent Inhibitor of Ca -Bound S100B

Promising therapeutic tool for AMPH-induced addiction, reducing the oxidative stress, attenuating evoked (MA and heat HA) and spontaneous pain (FST) phenotypes, and all phases of morphine-induced behavioral locomotor sensitization in mice

Estrogen receptor α (ERα) ligand as potent antiestrogen; Metabolite of tamoxifen

Novel anti-thrombosis agent, orally inhibiting venous thrombosis and arterial thrombosis in vivo, showing no bleeding risk

Novel lysophosphatidic acid receptor 3 (LPA3) agonist

Orphan nuclear receptor DAF-12 ligand, inhibiting the dauer-promoting activity of DAF-12

Novel water-sensitive probe, demonstrating superior sensitivity for detecting modulation of water microsolvation, structural conformation during oligomer formation and 5FUrd binding to both wild type and mutant SOD1

Building Block

Negative control for RSL3

Potent antagonist of GluN2B-NMDA receptors (Ki = 5.8 nM), inhibiting ion flux in two-electrode voltage clamp experiments (IC50 = 223 nM)

Novel prodrug of the sigma (σ) ligand haloperidol metabolite II conjugated with the histone deacetylase (HDAC) inhibitor valproic acid, demonstrating antiangiogenic activity

Novel profluorescent RAMOSUS3 (RMS3) probe with strigolactone-like bioactivity

Potent and selective 5-HT2 serotonin receptor agonist