Psoriasis

Tyk2-IN-28 is an orally active and selective TYK2 inhibitor with an IC₅₀ of 0.9 nM. Tyk2-IN-28 also inhibits JAK2 kinase activity with an IC₅₀ of 4 nM. Tyk2-IN-28 blocks inflammatory cytokine signaling. Tyk2-IN-28 reduces paw swelling in mouse models. Tyk2-IN-28 can be used for research on psoriasis.

LC-MI-3 is an orally active IRAK4 PROTAC degrader with an IC₅₀ of 57.2 nM and high selectivity among human protein kinases. LC-MI-3 eliminates IRAK4 kinase and scaffolding functions via the cereblon E3 ubiquitin ligase and ubiquitin-proteasome systems. LC-MI-3 inhibits downstream nuclear factor-κB and IRAK4-mediated inflammatory signaling pathways. LC-MI-3 can be used for the research of acute lung injury, sepsis, psoriasis, and inflammatory diseases.

MPiN is a KV1.3 potassium channel inhibitor. The IC₅₀ values of MPiN for inhibiting Kv1.3 currents are 1.1 μM (at -90 mV) and 0.6 μM (at -35 mV). MPiN exhibits in vivo efficacy in a mouse psoriasis model. MPiN can be used for the research of psoriasis.

Khasianine (Standard) is the analytical standard of Khasianine (HY-N2322). This product is intended for research and analytical applications. 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.

Euphoscopin A (2-epi-Euphornin I) is a toxic lathyrane diterpene with Kv1.3 potassium channel inhibitory activity, can be found in fresh leaves and roots of Euphorbia helioscopia and aerial parts of Euphorbia fischeriana.

G9a ligand-1 is a target protein ligand that targets G9a, and it can be used in PROTAC-related research, such as serving as the PROTAC target protein ligand for PROTAC G9a degrader-1 (HY-187214).

Thalidomide-4-O-C10-piperidine-NHBoc is an intermediate in the synthesis of G9a-targeting PROTAC, and serves as the E3 ligase ligand-linker conjugate moiety for PROTAC G9a degrader-1 (HY-187214).

PROTAC G9a degrader-1 is a selective and orally active G9a PROTAC degrader with a DC₅₀ of 1.29 μM. PROTAC G9a degrader-1 inhibits the NF-κB signaling pathway, suppresses the proliferation and migration of cancer cells, promotes apoptosis and cell cycle arrest, and reduces the expression level of H3K9me2. In in vivo models, PROTAC G9a degrader-1 alleviates skin inflammation, reduces epidermal hyperplasia, and decreases Ki67 expression. PROTAC G9a degrader-1 can be used for the research of triple-negative breast cancer and psoriasis.

PI3K/AKT/JAK2-IN-1 is a potent multi-target inhibitor of the PI3K/AKT/JAK2 signaling pathway. PI3K/AKT/JAK2-IN-1 suppresses NO production (IC₅₀ = 1.0 μM), reduces pro-inflammatory cytokines (TNF-α, IL-6, IL-1β, IL-17A, IL-22), and inhibits keratinocyte hyperproliferation by downregulating Ki67 and PCNA. PI3K/AKT/JAK2-IN-1 can be used for psoriasis research.

(±)-Methotrexate-¹³C,d₃ disodium ((±)-Amethopterin-¹³C,d₃ disodium; (±)-CL14377-¹³C,d₃ disodium; (±)-WR19039-¹³C,d₃ disodium) is the deuterated, ¹³C-labeled (±)-Methotrexate (HY-121151). (±)-Methotrexate is the racemate of Methotrexate (HY-14519). Methotrexate is an orally active antifolate (Antifolate). Methotrexate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.

PDE4-IN-36 is a phosphodiesterase 4 (PDE4) inhibitor with significant inhibitory activity at 10 μM. PDE4-IN-36 can be used in the research of psoriasis and atopic dermatitis.

RORγt inverse agonist 37 is an orally active RORγt inverse agonist with an IC₅₀ of 10.8 nM against human targets. RORγt inverse agonist 37 destabilizes helix 12 of RORγt in the agonist-bound conformation, thereby inhibiting transcriptional activity. RORγt inverse agonist 37 inhibits the secretion of IL-17 in cells and in LPS-induced systemic inflammation mouse models. RORγt inverse agonist 37 improves disease-related symptoms in mouse models of psoriasiform dermatitis. RORγt inverse agonist 37 can be used in research related to psoriasiform dermatitis and systemic inflammation.

IMG-008 is a fully human antagonistic antibody targeting IL-36R, acting as a high-affinity IL-36R inhibitor (K_d = 6.23 pM). IMG-008 competitively blocks the pro-inflammatory signaling pathway mediated by human IL-36R, inhibiting receptor activation and the production of inflammatory cytokines. IMG-008 suppresses Imiquimod (HY-B0180)-induced skin inflammation in humanized mice, and Fc modification increases its serum exposure and prolongs its half-life. IMG-008 can be used in studies related to IL-36R-mediated inflammatory diseases such as psoriasis.

MOR102 is a fully human IgG4 monoclonal antibody and an ICAM-1 inhibitor, lacking cross-reactivity with ICAM-2 and ICAM-3. MOR102 binds to the LFA-1 binding site within ICAM-1 domain 1, blocks ICAM-1/LFA-1 interaction, binds human keratinocytes with increased binding to interferon-γ-stimulated keratinocytes. MOR102 inhibits lymphocyte adhesion, reduces lymphocyte proliferation, prevents local T-cell activation, reduces inflammatory infiltrate, restores orthokeratotic differentiation, and reduces epidermal thickness. MOR102 can be used for the research of psoriasis.

iNOs-IN-9 is a selective inducible nitric oxide synthase (iNOS) inhibitor with an IC₅₀ of 82 nM against hiNOS. iNOs-IN-9 reduces cytokine-induced inflammatory responses and cell necrosis in inflammatory cell models. iNOs-IN-9 can be used for research related to psoriasis.

Sotrastaurin (AEB071) acetate is a selective, orally active PKC inhibitor. Sotrastaurin acetate inactivates NF-κB by inhibiting PKC α, β, θ, γ subtypes, thereby reducing the transcription levels of immune response-related genes. Sotrastaurin acetate effectively inhibits alloreactive T cell proliferation, conventional T cell activation, as well as the production of pro-inflammatory cytokines and B lymphocytes. Sotrastaurin acetate also maintains the functional and phenotypic stability of regulatory T cells, enhances Foxp3 expression and restores the balance of helper T lymphocytes. Sotrastaurin acetate can prolong the survival time of allografts, and alleviate inflammatory responses and myasthenic symptoms by reducing anti-AChR antibody levels. Sotrastaurin acetate is widely used in studies related to kidney transplantation, psoriasis and myasthenia gravis.

HZD37-5 is a humanized monoclonal antibody specifically recognizing N78 loci of IL-17A. HZD37-5 binds to human and rhesus monkeys, blocks IL-17 induced signal transduction and the release of IL-6, IL-8, CXCL-1 and GM-GSF. HZD37-5 significantly inhibited human IL-17A induced-keratinocyte chemoattractant secretion. HZD37-5 can be used for the research of autoimmune diseases including psoriasis and psoriatic arthritis.

TLR7 antagonist-1 (Compound 44#) is an orally active, selective TLR7 antagonist with an IC₅₀ value of 0.3 nM against TLR7. TLR7 antagonist-1 selectively binds to TLR7, inhibits its activation, and downregulates the c-Rel signaling pathway. TLR7 antagonist-1 downregulates the mRNA levels of proinflammatory cytokines IL-1β, IL-6, and TNF-α. TLR7 antagonist-1 alleviates Imiquimod (HY-B0180)-induced psoriasis-like skin lesions. TLR7 antagonist-1 is applicable to research related to psoriasis.

PROTAC IRAK4 degrader-14 is an orally active IRAK4 PROTAC degrader with a DC₅₀ of 2.4 nM. PROTAC IRAK4 degrader-14 inhibits proinflammatory responses in multiple cell types including T cells, monocytes and keratinocytes. PROTAC IRAK4 degrader-14 is applicable to research related to psoriasis.

Deucravacitinib analog 1 (compound 3), Deucravacitinib (HY-117287) derivative, is a TYK2 allosteric ligand. Deucravacitinib analog 1 binds to the JH2 domain of TYK2. Deucravacitinib analog 1 serves as a starting point for development of TYK2-targeting PROTAC degraders. Deucravacitinib analog 1 can be used for the researches of psoriasis and cancer.