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].
Olaptesed pegol (NOX-A12) L-oligoribonucleotide aptamer targeting CXCL12 based on a pegylated structure. Olaptesed pegol neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment[1].
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].
Rafutrombopag is a thrombopoietin (TPO) agonist extracted from patent CN113929668 A.
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].
5(S)15(S)-DiHETE is an “activated” intermediate, inhibits platelet aggregation with an IC50 of 1.3 μM. 5(S)15(S)-DiHETE enhances the rate of either LXA4 or LXB4 biosynthesis[1].
Factor B-IN-4 (Example 13 target compound) is a potent complement factor B inhibitor, with an IC50 of 1 μM. Factor B-IN-4 can be used for the research of diseases related to inflammation and immunity[1].
Chlorpheniramine maleate is an histamine H1 receptor antagonist with IC50 of 12 nM.Target: Histamine H1 ReceptorChlorpheniramine inhibits the proliferation of MCF-7, MDA-MB 231, and Ehrlich cells in a dose-response manner, and significantly reduces the ornithine decarboxylase mRNA translation by 50%-70% at the 250 μM [1]. Chlorpheniramine displaces of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells with IC50 of 66 nM. Chlorpheniramine displays antimalarial activity against CQS strain (D6) and MDR strain (Dd2) of P. falciparum with IC50 of 61.2 uM and 3.9 uM, respectively. Chlorpheniramine displays cytotoxicity against the proliferation of concanavalin A-induced murine splenic lymphocytes with IC50 of 33.4 μM [2].Oral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg [3]. Oral administration of Chlorpheniramine (10 mg/kg) significantly inhibits short-duration scratching in BALB/c mice stimulated by ovalbumin active cutaneous anaphylaxis and in ICR mice subcutaneously injected with histamine, but not long-duration scratching seen in NC/Nga mice, in contrast to that of dexamethasone or tacrolimus [4].
4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever[1][2][3]. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties[2].
Polvitolimod is a TLR7 agonist for treatment of cancer and infectious disease.
SC144 is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.IC50 value: < 1 uM (Cell assay) [1]Target: gp130 inhibitorSC144 shows greater potency in human ovarian cancer cell lines than in normal epithelial cells. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. In addition, SC144 shows potent inhibition of gp130 ligand-triggered signaling. Oral administration of SC144 delays tumor growth in a mouse xenograft model of human ovarian cancer without significant toxicity to normal tissues.
Nizatidine is a histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion.Target: Histamine H2 ReceptorNizatidine, a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion, with IC50 of 0.9 nM. Nizatidine exhibits maximal inhibition of gastric acid in rats within the first hour of drug administration, with EC50 of 1.383 μmol/kg [1]. Nizatidine also reversibly inhibits acetylcholinesterase (AChE), with IC50 of 6.7 μM, and the inhibition is noncompetitive, with a Ki value of 7.4 μM. Nizatidine (0.3-3 mg/kg, i.v.) significantly increases the motor index of gastrointestinal (GI) motility in a dose-dependent manner. Nizatidine inhibits gastric acid secretion with ED50 and ED90 of 0.18 and 3.22 mg/kg in dogs, and 2.94 and 19.6 mg/kg in rats, respectively [2].
ODN 2216 is a TLR9 (toll-like receptor 9) ligand or agonist. ODN 2216 induces high amounts of IFN-α and IFN-β. ODN 2216 induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 can activate NK cells and promote IFN-γ production of TCR-triggered CD4+ T cells[1][2][3][4].
Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.
ADU-S100 is an inducer of STING (stimulator of interferon genes). ADU-S100 has enhanced binding affinity to STING and activate all known human STING alleles.
Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.
S 38093 hydrochloride is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.
Sonelokimab (ALX 0761; M 1095) is a trivalent nanobody comprised of monovalent camelid-derived nanobodies specific to human interleukin (IL)-17A, IL-17F, and human serum albumin VHHs. Sonelokimab has the potential for plaque-type psoriasis research[1][2].
Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs)[1][2][3].
PF06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), and used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas.
Licarin A ((+)-Licarin A), a neolignan isolated from various plants, significantly and dose-dependently reduces TNF-α production (IC50=12.6±0.3 μM) in dinitrophenyl-human serum albumin (DNP-HSA)-stimulated RBL-2H3 cells. Anti-allergic effects. Licarin A reduces TNF-α and PGD2 production, and COX-2 expression[1]。
ODN 20844, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 20844 disrupts TLR7- and TLR9-mediated immune cell immune responses. ODN 20844 sequence: 5'-TCCTGGCGc7GGGAAGT-3'[1].
Tazofelone (LY 213829) is a cyclooxygenase-II (COX-II) inhibitor. Tazofelone transform into sulfoxide and quinol metabolites is primarily mediated by CYP3A. Tazofelone can be used for the research of inflammatory bowel disease[1][2].
Sphondin, isolated from Heracleum laciniatum, possesses an inhibitory effect on IL-1β-induced increase in the level of COX-2 protein and PGE2 release in A549 cells[1].