Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro[1][2][3].
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant[1][2][3].
Rocastine is a selective, nonsedating H1 antagonist, acting as an antihistamine.
Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research[1][2][3][4].
Pivekimab is a human monoclonal IgG1 antibody targeting interleukin 3 (IL-3). Pivekimab is a CD123-targeting antibody-drug conjugate. Pivekimab can be used in research of blastic plasmacytoid dendritic cell neoplasm (BPDCN)[1].
IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg[1].
ODN 105871, a G-modified inhibitory oligonucleotide (INH-ODN), is a selective TLR7 inhibitor. ODN 105871 can be uesd for inflammatory immune responses research[1].
CMPD167 (MRK-1) is an orally acitve small molecule that binds to CCR5 to inhibit gp120 association, inhibits different stages of the virus-cell attachment and entry process (CCR5-using virus SHIV-162P3, IC50<1 nM).
Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2[1].
Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 µM and 1.2 µM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties[1][2].
Cetirizine Impurity C is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist[1][2].
Ibuprofen Impurity K is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1].
Histamine H4 receptor antagonist-1 is an antagonist of histamine H4 receptor extracted from patent WO2010108059A1 compound 60[1].
PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research[1][2].
Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (Ki: 160 nM)[1][2][3].
GNE-2256 (GNE2256) is a potent, selective inhibitor of IRAK4 with biochemical Ki of 1.4 nM.GNE-2256 displays high selectivity in the CEREP panel with off-targets with >50% inhibition are TACR1, HTR2B and ACHE.GNE-2256 is potent in the NanoBRET assay (IC50 = 3.3 nM), the IL-6 human whole blood assay (IC50=190 nM) and the IFNα human whole blood assay (IC50=290 nM).
Bavisant (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. IC50 Value: Target: H3 receptorin vitro: Bavisant completed a phase II ADHD trial, but no results have been reported [1].in vivo: Mean change from baseline in the total ADHD-RS-IV score at day 42 (primary efficacy endpoint) was -8.8 in the placebo group versus -9.3, -11.2 and -12.2 in the bavisant 1?mg/day, 3?mg/day and 10?mg/day groups, respectively; the change in the 10?mg/day group was not statistically superior to placebo (p=0.161), and hence statistical comparisons of the 1?mg/day and 3?mg/day groups with placebo based on a step-down closed testing procedure were not performed [2].Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2
Piroxicam cinnamate (Cinnoxicam) is a cyclooxygenase (COX) inhibitor, with anti-inflammatory activity. Piroxicam cinnamate is stable under gastric conditions, can be used for inflammatory-degenerative osteoarticular diseases, rheumatic disorders, and varicocele (VC) associated oligoasthenospermia research[1][2][4].
Keliximab (SB-210396) is a chimeric human/macaque IgG1 anti-CD4 monoclonal antibody with a Ki value of 1.0 nM for soluble CD4. Keliximab blocks T cell proliferation and inhibits IL-2 production. Keliximab can be used for cancer research[1][2].
CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS[1].
Efmarodocokin alfa is a fusion protein of human IL-22 and the IgG4 crystallizable fragment. Efmarodocokin alfa activates IL-22 signaling. Efmarodocokin alfa can be used for the research of severe COVID-19 pneumonia[1].
PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs[1].
A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM; prevents PMN infiltration and tissue damage in several models of IR injury in vivo; abrogates motility and induces apoptosis in cultured cutaneous and uveal melanoma cells and xenografts; also prevents inflammation-mediated damage in MLD-STZ, prevents and reverses diabetes in NOD mice. Diabetes Phase 2 Clinical
Siltuximab is an anti-IL-6 (interleukin-6) monoclonal antibody, and shows antitumor activity. Siltuximab can be used in Multicentric Castleman's Disease (MCD) and COVID-19 research[1][2][3].
TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway[1][2]. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI)[2].
C12-iE-DAP (Lauroyl-γ-D-glutamyl-meso-diaminopimelic acid) is a biological active peptide. (a lauroyl (C12) group to the glutamic residue of iE-DAP , NOD1 agonist)
Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic drug.
α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression[1].
TMX-201 is a TLR7 ligand-phospholipid conjugate. TMX-201 shows potent immune stimulatory activity. TMX-201 can be used for breast cancer and melanoma research[1].
Carboxyebselen (HOOC-Ebs) is a potent and selective inhibitor of endothelial nitric oxide synthase (eNOS)[1].