Brazikumab (AMG 139) is a human IgG2 monoclonal antibody, selectively binds the p19 subunit of IL-23, with a KD of 0.138 nM for human IL-23. Brazikumab can be used for the research of Crohn's disease[1].
Briquilimab (JSP-191) is a non-toxic humanized monoclonal antibody targeting CD117 (c-Kit) to deplete hematopoietic stem cell (HSC). Briquilimab has safety to clear host marrow niche space to enable sufficient donor HSC engraftment and immune reconstitution as primary method of severe combined immunodeficiency (SCID)[1].
EA-230 is a synthetic oligopeptide originally derived from beta-human chorionic gonadotropin (beta-hCG) lysates. EA-230 has anti-inflammatory effects and can be used for the research of sepsis[1].
Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.
Bisdemethoxycucurmin (p,p'-Dihydroxydicinnamoylmethane), a curcuminoid, has antioxidant and antiinflammatory activities[1][2].
Chlorpheniramine-d4 (maleate) is deuterium labeled Chlorpheniramine (maleate).
Pentosan Polysulfate is a semi-synthetic drug used to treat various medical conditions including thrombi and interstitial cystitis.
MGL-IN-1 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. MGL-IN-1 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. MGL-IN-1 displays high membrane permeability and brain penetrant[1].
Mebhydrolin is a specific histamine H1 receptor antagonist.
CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model[1].
Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways[1].
GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain[1].
BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor.
A potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice.
Voclosporin is a calcineurin (CN) inhibitor.
Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a commonly used PKC activator.
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders[1][2][3].
Clemastanin B, a lignin, has potent anti-influenza activities by inhibiting the virus multiplication, prophylaxsis and blocking the virus attachment. Clemastanin B targets viral endocytosis, uncoating or ribonucleoprotein (RNP) export from the nucleus. Clemastanin B has antioxidant and anti-inflammatory activities[1][2][3].
MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189 μM for the recombinant human MD2 (rhMD2).
sEH inhibitor-5 (compound D016) is a potent sEH (soluble epoxide hydrolase) inhibitor with an IC50 value of 0.1 nM[1].
Licochalcone D, a flavonoid compound mainly existing in the root of Glycyrrhiza inflate, is a potent inhibitor of NF-kappaB (NF-κB) p65. Licochalcone D possesses antioxidant, anti-inflammatory, anti-cancer properties[1][2].
Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties[1][2].
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, a Substance P derivative, is a biased agonist toward neuropeptide and chemokine receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P activates G12. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P binds to IL-8 and GRP receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P inhibits ERK-2 activation, activates JNK activity. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P stimulates an increase in neutrophil migration and Ca2+ mobilization. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is also a bombesin antagonist, and inhibits the growth of small cell lung cancer[1][2][3]
Cystathionine-γ-lyase-IN-1 is a selective cystathionine γ-lyase (CSE) enzyme inhibitor with an IC50 of 6.3 μM[1].
Sterculic acid is a stearoyl-CoA desaturase-1 (SCD1) inhibitor. Sterculic acid specifically inhibits the delta-9 desaturase (Δ9D) activity with an IC50 value of 0.9 μM[1].
Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
Angelicain (Norcimifugin) is a constituent of Cimicifuga foetida with anti-inflammatory activity[1].
Nargenicin A1 is an antibiotic agent against various Gram-positive bacteria. Nargenicin A1 shows anti-inflammatory activity. Nargenicin A1 protects HINAE cells against Tacrolimus (HY-13756)-induced DNA damage and apoptosis. Nargenicin A1 can also be used for the research of acute myeloid leukemia[1].
Piketoprofen is a non-steroidal anti-inflammatory reagent that can be used as a cream preparation for the study of soft tissue rheumatism[1].