Psoriasis

Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC₅₀ of 0.2 nM and a K_i of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus.

Propranolol is a nonselective and BBB-permeable β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.

Bimekizumab (Anti-Human IL17A/IL-17F Recombinant Antibody) is a humanised monoclonal antibody, can selectively neutralises IL-17A and IL-17F. Both of them are pro-osteogenic with respect to human periosteum-derived cell (hPDC) differentiation. Thus Bimekizumab blocks the inflammation-driven osteogenic differentiation.

Ustekinumab is an anti-IL-12/IL-23 IgG1κ human monoclonal antibody.

Secukinumab (AIN457) is a high affinity, human monoclonal antibody targeted against interleukin (IL)-17A. Secukinumab is the first-in-class anti-IL-17 agent used for the research of plaque psoriasis, ankylosing spondylitis and psoriatic arthritis.

Isosorbide di-(methyl fumarate) (IDMF), topical DMF (HY-17363) derivative, is an NRF2/ARE pathway activator. Isosorbide di-(methyl fumarate) downregulates ANCR targets, modulates epithelial differentiation, represses proinflammatory cytokine genes, IL-17A- and TNF-induced keratinocyte genes, psoriatic skin lesion-specific genes, and immune response genes. Isosorbide di-(methyl fumarate) stimulates oxidative stress response gene transcription, reduces erythema and scaling in Imiquimod (HY-B0180)-induced psoriasiform lesions. Isosorbide di-(methyl fumarate) exhibits no genotoxicity or radiation sensitivity in skin fibroblasts, is nonirritating and nonsensitizing in rodent models. Isosorbide di-(methyl fumarate) can be used for the research of psoriasis vulgaris.

Icotrokinra (JNJ-77242113) hydrochloride is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra hydrochloride inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC₅₀=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC₅₀ of 18.4 pM. Icotrokinra hydrochloride exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra hydrochloride can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease.

TAVO101 is a humanized anti-TSLP antibody with an EC₅₀ of 0.19 nM against hTSLP. TAVO101 inhibits STAT5 activation and CCL17 release. TAVO101 carries Fc region mutations that enhance its binding to FcRn while reducing its binding to FcγRI, FcγRIIIA and C1q, thereby attenuating effector functions. TAVO101 reduces the levels of inflammatory markers, cell infiltration and histopathological damage in preclinical models of asthma, psoriasis and atopic dermatitis. TAVO101 can be used for research related to asthma, psoriasis and atopic dermatitis.

Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (K_d <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC₅₀ = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis.

Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with K_d values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research.

Brodalumab (AMG 827) is a human anti-interleukin-17-receptor IgG2 monoclonal antibody that can be used for the research of moderate-to-severe plaque psoriasis and rheumatoid arthritis.

Vixarelimab (KPL-716) is a human anti-oncostatin M (OSM) receptor β subunit monoclonal antibody. Vixarelimab inhibits IL-31 and OSM signalling. Vixarelimab can be used in studies of inflammatory skin diseases such as atopic dermatitis and itchy nodular rash.

Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.

Calcipotriol monohydrate is a synthetic VitD3 analogue with a high affinity for the vitamin D receptor.

Tildrakizumab (SCH 900222) is a humanized anti-IL-23 (p19 subunit) monoclonal antibody. IL-23 is a critical cytokine to maintain the Th17 cell phenotype. Tildrakizumab has high-affinity for single-chain IL-23 (K_d: 136 pM). Tildrakizumab is effective against moderate to severe plaque psoriasis.

PD 151746 is a selective calpain-1 inhibitor with an IC₅₀ of 260 nM. PD 151746 binds μ-calpain Ca²⁺-binding sites, and shows selectivity over cathepsin B, papain, trypsin, thermolysin, and basal calcineurin. PD 151746 reduces Oxidized low-density lipoprotein (oxLDL)-induced cytotoxicity, apoptotic DNA fragmentation, and blocks IL-1α maturation. PD 151746 can be used for the research of atherosclerosis and psoriasis.

Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19.

RDN2150 TFA is a ZAP-70 inhibitor with an IC₅₀ of 14.6 nM, and it exhibits selectivity for Syk over other kinases. RDN2150 TFA inhibits signal transduction and activation of T cells/CAR-T cells, reduces the phosphorylation level of Erk1/2, suppresses the induction of CD69 and IL-2, and downregulates phosphotyrosine signaling pathways including hnRNP sites in T cells. RDN2150 TFA can be used for psoriasis-related research.

Khasianine is a steroidal glycoalkaloid. Khasianine alleviates psoriasis-like skin inflammation by inhibiting the TNF-α/NF-κB axis. Khasianine can downregulate the RhoA pathway and exhibits potential antimetastatic activity. Khasianine upregulates the expression of TNFR I and TNFR II without inducing apoptotic effects. Khasianine can be used in studies related to psoriasis, pancreatic ductal adenocarcinoma, and liver cancer.

B3GNT2-IN-1 is a β-1,3-N-acetylglucosaminyltransferase 2 (B3GNT2) inhibitor with an IC₅₀ of 0.009 μM. B3GNT2-IN-1 is applicable to research related to rheumatoid arthritis, ankylosing spondylitis and psoriasis.