PLN-1474 (compound 1) is an orally active and selective avß1 integrin inhibitor with an IC50 value of ＜50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or treating a fibrotic or cirrhotic disease or disorder[1].
Maraviroc is a selective CCR5 antagonist with activity against human HIV.
PLP(139-151) is a fragment of myelin proteolipid protein, induce experimental autoimmune encephalomyelitis (EAE).
Danshenol A, an abietane-type diterpenoid, is an aldose reductase (AR) inhibitor with an IC50 of 0.1 μM. Danshenol A can protect endothelial cells from oxidative stress by directly scavenging ROS. Danshenol A has anti-inflammatory and antitumor properties. Danshenol A can be used for atherosclerosis research[1][2][3][4].
Abrilumab is a fully human monoclonal antibody directed against α4β7. Abrilumab selectively binds the α4β7 integrin heterodimer. Abrilumab can be used for the research of inflammatory bowel disease (IBD)[1].
ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor (IC50=1.7 nM).
6-Aminochrysene (6-Aminochrysene) is an aromatic amine used as a chemotherapeutic agent in the treatment of splenomegaly, myeloid leukemia, and breast cancer.
4,6-Dichloroguaiacol induces biochemical and morphological changes in human peripheral blood lymphocytes in vitro[1].
Diclofenac-13C6 (Sodium) is the 13C6 labeled Diclofenac (Sodium). Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen[1][2].
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[1][2]. Phenidone is used as a photographic developer[3].
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM)[1]. CLP-3094 is a selective, potent GPR142 antagonist[2].
RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC50 of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders[1].
Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research[1].
Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis[1][2].
Bimosiamose disodium (TBC-1269Z) is a nonoligosaccharide pan-selectin inhibitor with IC50s of 88 μM, 20 μM, and 86 μM for E-selectin, P-selectin, and L-selectin, respectively. Bimosiamose disodium has anti-inflammatory effects[1].
Cortistatin-14, a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties[1][2][3][4].
Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects[1].
1-Pentadecanol is a naturally occurring antiacne agent[1].
S1P5 receptor agonist-1 (example 6) is a potent and selective agonist of S1P5 receptor with an EC50 value of 20 nM[1].
L-Lysine-13C6,15N2 hydrochloride is the 13C- and 15N-labeled L-Lysine hydrochloride. L-lysine hydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.
Liriope muscari baily saponins C is one of major active compounds of L. muscari (Decne.) Baily. Liriope muscari baily saponins C possesses strong anti-inflammatory, immunopharmacological and cardioprotective activities. Liriope muscari baily saponins C has been studied as a candidate drug for cancer metastasis[1].
Tuparstobart (Incagn-02385) is an IgG1κ antibody targeting LAG-3. LAG-3 is an immune checkpoint receptor protein mainly expressed on activated T cells, NK cells, B cells and plasmacytoid dendritic cells[1].
Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol[1]. Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin[2][3].
4-Phenyl-7,8-dihydroxycoumarin is a coumarin derivative and can be used for bronchiectasiss research[1].
Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer[1].
Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP) (extracted from patent WO2021076124A1)[1].
3,5,7-Trimethoxyflavone, a flavonoid compound, can inhibit the TNF-α-induced high expression and secretion of MMP-1 by cells. 3,5,7-Trimethoxyflavone can be used to ameliorate skin damage[1].
CpG ODN 10101, a synthetic oligodeoxynucleotide (ODN), is a toll-like receptor 9 (TLR9) agonist. CpG ODN 10101 is a potent inducer of cytokine/chemokine expression ex vivo when used in combination with HH2(VQLRIRVAVIRA-NH2). CpG ODN 10101 induces IFN- secretion from dendritic cells (DCs) and stimulates B-cells.CpG ODN 10101 has antiviral and immunomodulatory properties that can influence chronic infection with HCV[1][2].