as 19

AS19 is a potent, selective 5-HT7 receptor agonist (IC50: 0.83 nM; Ki: 0.6 nM) with demonstrated selectivity for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis: 89.7 nM, 490 nM, 6.6 nM, and 98.5 nM, respectively).

Tocilizumab (Anti-Human IL6R) is a neutralizing antibody against human interleukin-6 receptor (IL-6R) that blocks the binding of IL-6 to IL-6R, thereby inhibiting both classical and trans signaling. It can be used to study rheumatoid arthritis and has been suggested as a possible drug for the treatment of severe COVID-19.

AZ10606120 dihydrochloride is a selectable, potent, high-affinity receptor antagonist with K D values of 1.4 and 19 nM at human and rat P2X 7 receptors, respectively. AZ10606120 dihydrochloride inhibits tumor growth and has anti-angiogenic activity. AZ 10606120 acts as a negative allosteric modulator when bound to a site coupled to the ATP binding site.

Imiquimod (R 837) is an immune response modifier that acts as a toll-like receptor 7 agonist.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

Molnupiravir (EIDD-2801) is an isopropyl ester prodrug of the ribonucleoside analog EIDD-1931 with oral bioavailability. Molnupiravir can be used in the study of COVID-19, seasonal and pandemic influenza, and has broad-spectrum antiviral activity against multiple coronaviruses and influenza viruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV.

Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol) (HCQ) is an alkalinizing lysosomatropic drug that acts by inducing apoptosis of renal cancer cells in vitro and inhibiting TLR7 9. It is a medication used to prevent and treat malaria, and it's also being studied as an experimental treatment for COVID-19.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+ K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

Ned 19, a selective membrane-permeant non-competitive antagonist of NAADP, strongly inhibits tumor growth, vascularization, and lung metastases in mice.

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Protein Kinase C 19-31 acetate, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate

Eurifoloid Q is a natural product that can be used as a reference standard. The CAS number of Eurifoloid Q is 1629153-19-0.

Zapotin is a natural product that can be used as a reference standard. The CAS number of Zapotin is 14813-19-5.

L-671329 is a natural product that can be used as a reference standard. The CAS number of L-671329 is 120692-19-5.

PDE4-IN-19 (compound 1) acts as a PDE4 inhibitor and exhibits potent inhibition with IC 50 values below 10 nM for PDE4B1 and between 10-100 nM for PDE4D3.

NMS-P626 functions as an inhibitor targeting TRKA, TRKB, and TRKC, exhibiting IC 50 values of 8 nM, 7 nM, and 3 nM respectively. It effectively suppresses KM12 cell growth by inhibiting the phosphorylation of TPM3-TRKA and the subsequent downstream signaling, demonstrating an IC 50 of 19 nM specifically for KM12 cells. This compound is applicable in the study of colorectal cancer.

Compound (−)-19, also known as (-)-5-HT2C agonist-3, is a selective 5-HT2C agonist exhibiting a preference for Gq signaling. It demonstrates efficiency with EC50 values for 5-HT2 receptor subtypes as follows: 5-HT2C at 103 nM, 5-HT2B at 570 nM, and 5-HT2A at 72 nM. This compound is utilized in research on antipsychotics.

Keap1-Nrf2-IN-22 (compound 19) acts as a Keap1-Nrf2 inhibitor with a KD2 value of 42.2 nM. It is utilized in research focused on acute lung injury (ALI) and cerebral ischemia reperfusion (I R) injuries.

PROTAC SMARCA2 degrader-19 (Compound 46) acts as a degrader of SMARCA2, demonstrating degradation capabilities in A549 and MV411 cells with a DC50 of less than 100 nM. Additionally, this compound degrades SMARCA4 in MV411 cells, but with a significantly higher DC50 of over 1000 nM.

UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 values of 15 nM and 19 nM, respectively. It is effective in inhibiting invasion and migration of TNBC cells in vitro. Additionally, UNC0638 hydrate acts as an inhibitor of EHMT1 2 and induces the expression of fetal hemoglobin (HbF) in cultures of human erythroid progenitor cells. Furthermore, it exhibits antiviral activity against FMDV (foot-and-mouth disease virus) and VSV (vesicular stomatitis virus), demonstrating remarkable potency and selectivity across various epigenetic and non-epigenetic targets.

PROTAC MPS1 degrader 1 (Compound 19) acts as a potent degrader of Monopolar spindle 1 (Mps1, TTK), AURKA, and AURKB, with DC50 values of 17.7, 108.7, and 570.3 nM respectively. It is utilized in the study of acute myeloid leukemia. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase)

(6S)-CP-470711 (Compound 8) acts as an inhibitor of sorbitol dehydrogenase (SDH) in both humans and rats, exhibiting inhibitory concentrations (IC50) of 19 nM and 27 nM, respectively. Additionally, (6S)-CP-470711 has been shown to ameliorate diabetes in rats induced by Streptozotocin.

RR-49 is an innovative difluorinated analogue. This compound demonstrates exceptional pH sensitivity, showing the same efficacy for DAMGO in MOR cAMP assays at pH 6.5 as it does at pH 7.4, but with a 19-fold increase in potency (IC50). It holds significant promise as an analgesic for treating inflammatory pain with a lower potential for abuse.

VR17-04, a metabolite of Enisamium, inhibits the incorporation of GTP and UTP during RNA synthesis. Its mechanism of action was elucidated through docking and molecular dynamics simulations. These findings suggest that VR17-04 could serve as a potential antiviral strategy for managing COVID-19.