Immethridine dihydrobromide is a selective histamine H3 receptor (H3R) agonist. Immethridine dihydrobromide displays 300-fold selectivity over the H4 receptor and does not bind to H1 or H2 receptors. Immethridine dihydrobromide can be used for experimental autoimmune encephalomyelitis (EAE) research[1].
BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor. BMS-37 can be used as PD-L1 ligand to synthesize PROTAC molecules[1].
SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines[1][2].
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide inhibits [3H]histamine synthesis with a Ki of 31 nM[1].
Gefurulimab (ALXN-1720) is a human-derived bispecific antibody against complement C5 and albumin that binds C5 and blocks its activation[1].
Immuno modulator-1 (compound 22) inhibits TNFα and IL-2 secretion in human peripheral blood mononuclear cells (hPBMC), with IC50 values of 4.7 and 26 nM, respectively. Immuno modulator-1 shows hERG potassium channel blocking effect, with Inhibitory percentage of 20% at 3 μM[1].
Buclizine is an orally active antihistamine antiallergic compound. Buclizine is a potent teratogen in the rat and shows anti-tumor activity[1][2][3].
Indomethacin sodium hydrate (Indometacin sodium hydrate) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin sodium hydrate disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
Vipoglanstat (BI 1029539, GS-248), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat (BI 1029539, GS-248) also has anti-inflammatory activity[1][2].
Mebhydrolin napadisylate is a specific histamine H1 receptor antagonist.
Bendazol is a hypotensive drug which can also enhance NO synthase activity in renal glomeruli and collecting tubules.
Semapimod, an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod has potential in a variety of inflammatory and autoimmune disorders[1][2][3].
OSM-SMI-8 (NSC642624) is a potent OSM (oncostatin M) antagonist. OSM-SMI-8 has the potential for the research of cancer[1].
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models[1][2][3][4].
CU-CPT17e is a multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.
Sasanlimab (PF-06801591) is a humanized IgG4-κ antibody targeting PD-1. Mainly expressed by CHO (Chinese Hamster Ovary) cells[1].
Chitohexaose hexahydrochloride is a chitosan oligosaccharide with anti-inflammatory effect. Chitohexaose binds to the active sites of TLR4 and inhibits LPS induced inflammation[1][2].
Ketotifen-d3 (HC 20511-d3) fumarate is the deuterium labeled Ketotifen fumarate. Ketotifen (HC 20511) fumarate is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks[1][2].
GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM).
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
IRAK4-IN-16 (compound 4) is a potent IRAK4 (interleukin-1 receptor associated kinase 4) inhibitor, with an IC50 of 2.5 nM. IRAK4-IN-16 shows cytotoxicity activity against OCI-LY10, TMD8, Ramos and HT cells, with IC50 values of 0.2, 0.2, 0.6, and 2.7 μM, respectively[1].
Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity[1].
RIG012 is a potent RIG-I inhibitor with an IC50 of 0.71 μM using the NADH-coupled ATPase assay. RIG012 inhibits IFN-β and ISG hRsad2 expression[1].
TLR7/8 agonist 3 is a potent TLR7 and TLR8 agonist, extracted from patent WO2016057618 (compound of formula (II))[1].
Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium dihydrate is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium dihydrate can reduce atherosclerosis and shows antitumor activity[1][2][3][4].
Nanrilkefusp alfa (SO-C101; SOT101) is fusion protein, is a selective and potent agonist fusion protein of IL-15 and IL-15Rα sushi+ domain. Nanrilkefusp alfa inhibits tumor by inducing proliferation and activation of memory CD8+ T cells, natural killer (NK) cells, γ/δ T cells and NKT cells. Nanrilkefusp alfa exhibits excellent anti-metastatic activity against melanoma and suppresses tumor growth in various mouse tumor models[1][2].
IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.
IL-17 modulator 3 is an IL-17 modulator (US20200247785A1). IL-17 modulator 3 can be used for the research of inflammation, cancer and autoimmune diseases[1].
Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar[1].