psoriatic

12R-LOX-IN-2 is an inhibitor of 12R-lipoxygenase (12R-LOX).12R-LOX-IN-2 inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and inhibits colony formation.12R-LOX-IN-2 also decreases the protein level of Ki67 and the mRNA expression of IL-17A in IMQ-induced cells. 12R-LOX-IN-2 may be useful in the study of psoriasis and other skin-associated inflammatory diseases.

SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).

Efalizumab, a novel potent regulator of T cells, is a humanized LFA-1 α subunit (CD11a) monoclonal antibody. Efalizumab has inhibitory effects on T cell activation, skin T cell transport, and T cell adhesion to keratinocytes, and can be used to study plaque psoriasis and psoriatic arthritis.

Halometasone is a synthetic corticosteroid.1,2Formulations containing halometasone have been used in the treatment of psoriasis vulgaris and eczematous dermatoses. 1.de la Brassine, M., Kint, A., Lachapelle, J.M., et al.Halomethasone (C 48.401-Ba) for the topical treatment of common dermatosesJ. Int. Med. Res.12(5)307-309(1984) 2.Zhu, J.-W., Wu, X.-J., Lu, Z.-F., et al.Role of VEGF receptors in normal and psoriatic human keratinocytes: Evidence from irradiation with different UV sourcesPLoS One8(1)e55463(2013)

QL-1200186 is an orally active, selective TYK2 inhibitor that, upon dose-dependent oral administration, suppresses interferon-γ (IFNγ) production following interleukin-12 (IL-12) stimulation and markedly improves skin lesions in a psoriatic mouse model [1].

12R-LOX-IN-1 (Compound 4a), with an IC50 of 28.25 µM, is an inhibitor of 12R-LOX. It suppresses the hyperproliferative condition and the ability to form colonies in Imiquimod-induced psoriatic keratinocytes, as well as reducing levels of reactive oxygen species, Ki67, IL-17A, TNF-α, and IL-6. This compound has utility in antipsoriatic research [1].

(±)13-HODE is one of the two racemic monohydroxy fatty acids resulting from the non-enzymatic oxidation of linoleic acid. It is the principle hydroxylated fatty acid in human psoriatic skin scales, with a mean concentration of 17 ng/mg.[1]

Clazakizumab, a monoclonal antibody, demonstrates high affinity and specificity towards the interleukin-6 (IL-6) cytokine, potentially inhibiting the cytokine response in COVID-19 caused by SARS-CoV-2. It is also under research for treating psoriatic arthritis (PsA) and renal antibody-mediated rejection [1] [2].

Perakizumab (RG4934), a humanized IgG1κ monoclonal antibody targeting IL-17A (Interleukin Related), is utilized in the study of autoimmune conditions, including psoriatic arthritis [1].

Guselkumab (CNTO 1959) is a recombinant human IgG1 monoclonal antibody targeting the IL-23p19 subunit. Guselkumab binds to human cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab can inhibit the production of cytokines downstream of IL-23 signaling pathway, and can be used in the study of psoriatic arthritis.

Netakimab, an anti-IL-17 monoclonal antibody, is utilized in the research of ankylosing spondylitis, psoriatic arthritis, and moderate-to-severe plaque psoriasis [1] [2].

IRAK4-IN-21 is a selective, orally active, potent IRAK4 inhibitor that acts on IRAK4 (IC50: 5 nM) and TAK1 (IC50: 56 nM). IRAK4-IN-21 exhibits potent inhibition of IL-23 production with an IC50 value of 0.17 μM. can be used to study autoimmune diseases, such as plaque psoriasis and psoriatic arthritis.

Leflunomide-d4 is a deuterated compound of Leflunomide. Leflunomide has a CAS number of 75706-12-6. Leflunomide is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis.

IL-17 Modulator 1 (disodium) is a potent, orally active compound, known for its high efficacy in modulating IL-17. This compound is extensively utilized for researching various diseases such as psoriasis, ankylosing spondylitis, and psoriatic arthritis[1].

Neihulizumab (ALTB-168), an immune checkpoint agonistic antibody, targets and binds to human CD162 (PSGL-1), resulting in the downregulation of activated T-cells. It is utilized in research aimed at treating steroid-refractory acute graft-versus-host disease (SR-aGVHD), psoriasis, psoriatic arthritis, and ulcerative colitis [1].

IRAK4-IN-22 is a selective, orally active, potent IRAK4 inhibitor that acts on IRAK4 (IC50: 3 nM) and TAK1 (IC50: 17 nM). IRAK4-IN-21 exhibits potent inhibition of IL-23 production with an IC50 value of 0.10 μM. IRAK4-IN-21 can be used to study autoimmune diseases, such as plaque psoriasis and psoriatic arthritis.

Apremilast, (+/-)-, is a small molecule inhibitor of phosphodiesterase 4 (PDE4) with oral activity. It is used to treat psoriatic arthritis.

Dithranol (cignoline) is an anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially PSORIASIS. It may cause FOLLICULITIS.

β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-2 induces IL-31 production by human peripheral blood-derived mast cellsin vitrowhen used at a concentration of 10 μg/ml and by rat mast cellsin vivofollowing a 500 ng intradermal dose.4Expression of β-defensin-2 is increased in psoriatic skin and chronic wounds.5,6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 3.Niyonsaba, F., Ushio, H., Nakano, N., et al.Antimicrobial peptides human β-defensins stimulate epidermal keratinocyte migration, proliferation and production of proinflammatory cytokines and chemokinesJ. Invest. Dermatol.127(3)594-604(2007) 4.Niyonsaba, F., Ushio, H., Hara, M., et al.Antimicrobial peptides human β-defensins and cathelicidin LL-37 induce the secretion of a pruritogenic cytokine IL-31 by human mast cellsJ. Immunol.184(7)3526-3534(2010) 5.Huh, W.-K., Oono, T., Shirafuji, Y., et al.Dynamic alteration of human β-defensin 2 localization from cytoplasm to intercellular space in psoriatic skinJ. Mol. Med. (Berl.)80(10)678-684(2002) 6.Butmarc, J., Yufit, T., Carson, P., et al.Human β-defensin-2 expression is increased in chronic woundsWound Repair Regen.12(4)439-443(2004)

Leflunomide (HWA486) is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis.

Risankizumab (BI 655066) is a humanized IgG monoclonal antibody (Kd <10 pM) targeting the IL-23 p19 subunit. Risankizumab inhibits IL-17 production induced by human IL-23 in mouse splenocytes with an IC50 value of 2 pM.Risankizumab is used for the prevention and treatment of immune and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis, and erythrodermic psoriasis.

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.

Vunakizumab is a humanized IgGκ monoclonal antibody targeting IL-17A, which is often linked to interleukin 22 to form Vunakizumab-IL22 for the study of influenza virus-induced lung immune injury Vunakizumab is used in the study of psoriatic arthritis and works by binding to IL-17A.