systemic lupus erythematosus

Paquinimod (ABR 25757) is a S100A9 inhibitor preventing S100A9 binding to TLR-4.

Mefloquine (Ro 215998), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus, and cancer research.

TLR7/8/9 antagonist 2 is an orally active and highly bioavailable vTLR7/8/9 antagonist. TLR7/8/9 antagonist 2 inhibits HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50s of 0.011 μM, 0.029 μM and 0,052 μM, respectively. TLR7/8/9 antagonist 2 can be used to study auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.

Solcitinib (GLPG-0778) (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus erythematosus.

Abetimus (LJP 394 free base), an immunosuppressant composed of four double-stranded DNA (dsDNA) oligonucleotides, can crosslink anti-dsDNA antibodies on B cell surfaces and reduce anti-dsDNA antibody levels, offering research potential for systemic lupus erythematosus [1].

C5aR1 antagonist peptide, a biologically active linear peptide originating from the C-terminus of the chemokine complement fragment 5 anaphylatoxin (C5a), inhibits C5a binding and activity at human and rat C5a receptors. Overexpression of C5a is linked to various immunoinflammatory diseases, including arthritis, Alzheimer’s disease, cystic fibrosis, and systemic lupus erythematosus.

Frentizole, an immunosuppressive agent, is an inhibitor of the Aβ-ABAD interaction

Forigerimod (IPP-201101), a potent CD4 T-cell modulator, is a 21-amino-acid fragment of the U1 small nuclear ribonucleoprotein 70 kDa, phosphorylated at Ser140, known for its ability to inhibit autophagy effectively. It has applications in researching autoimmune disorders, including systemic lupus erythematosus (SLE) [1] [2] [3] [4].

Valziflocept (BAX1810; TAK-752) is a recombinant soluble human FcγRIIb receptor designed to act as a decoy or scavenger by targeting Fc and FcγR, binding and neutralizing pathogenic IgG. Its utility lies in mitigating the impact of autoimmune diseases, making it a focus in systemic lupus erythematosus (SLE) research [1].

Rontalizumab, a humanized IgG1 monoclonal antibody, targets IFN-α and is utilized in research on systemic lupus erythematosus[1].

Belimumab(LymphoStat B) is a human IgG1λ monoclonal antibody that inhibits B-cell activating factor (BAFF).Belimumab is used in the study of fatigue and in the treatment of lupus nephritis and systemic lupus erythematosus.

Ruplizumab (BG 9588), a humanized monoclonal IgG1κ antibody targeting CD40L (TNF Receptor), holds promise for research in systemic lupus erythematosus disease [1].

PAD-IN-2 is a potent inhibitor of pad4 with an IC50 value <1 μM and can be used to study autoimmune diseases and cancers such as rheumatoid arthritis, vasculitis, systemic lupus erythematosus, cutaneous lupus erythematosus, cystic fibrosis, ulcerative colitis, asthma, multiple sclerosis, and psoriasis.

Edratide (TV 4710), a 19-amino-acid synthetic peptide derived from the complementarity-determining region 1 (CDR1) of a human anti-DNA antibody that exhibits the 16/6 Id idiotype, has been found to lower apoptosis rates and regulate the expression of caspase-8 and caspase-3 downward, while increasing Bcl-xL expression. It shows promise for systemic lupus erythematosus (SLE) research [1] [2] [3].

Forigerimod TFA (IPP-201101 TFA), a CD4 T-cell modulator, is a phosphorylated 21-amino-acid fragment derived from U1 small nuclear ribonucleoprotein 70 kDa, specifically at Ser140. It notably inhibits autophagy and is utilized in researching autoimmune disorders, including systemic lupus erythematosus (SLE) [1] [2] [3] [4].

Paramethasone Acetate is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive effects that can be used in the treatment of systemic lupus erythematosus.

Feeblin（IRF5-IN-1） is a protein degradation inducer that specifically blocks pro-inflammatory signaling pathways associated with autoimmune diseases and can be used to study immune system disorders in the class of systemic lupus erythematosus.

KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1].KZR-616 is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 and PR-924 [3]. KZR-616 (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1]. [1]. Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143. [2]. Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Diseases 2018;77:685. [3]. Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646.

ODN 21595, a guanine-modified inhibitor targeting TLR7 and TLR9, effectively inhibits the release of IFN-α and IL-6 without exhibiting cytotoxicity. It also reduces the expression of CD86 and HLA-DR, showcasing potential for systemic lupus erythematosus (SLE) research [1].

Lupus autoantigen peptide (LAP), a derivative of the autoantigen La found in systemic lupus erythematosus (SLE) patients, spans amino acids 11-28 of La and functions as an antiviral peptide. It primarily blocks the hepatitis C virus (HCV) from interacting with internal ribosome entry site (IRES) trans-acting factors (ITAFs), notably the polypyrimidine tract-binding protein (PTB) and poly(rC)-binding protein 2 (PCBP2). In a Huh7 cell-based reporter assay, LAP at a concentration of 60 µM effectively hampers HCV IRES-mediated translation, a process reversible by adding recombinant forms of PTB and PCBP2.

(R)-Elsubrutinib ((R)-ABBV-105), a Btk inhibitor, is employed in research related to immune disorders (including rheumatoid arthritis, psoriasis, ankylosing spondylitis, asthma, systemic lupus erythematosus) and cancer.

Toralizumab (IDEC-131), a humanized monoclonal antibody (mAb) directed against CD40L (CD154), consists of human gamma 1 heavy chains and human kappa light chains. Specifically targeting CD40L on T cells, it inhibits CD40 signaling, acting as an immunosuppressive agent with potential applications in systemic lupus erythematosus (SLE) research [1] [2].

Tabalumab (LY2127399), a humanized monoclonal antibody (IgG4 type) targeting B-cell activating factor (BAFF), exhibits neutralizing activity against both membrane-bound and soluble BAFF. This compound is relevant for research into autoimmune diseases, including rheumatoid arthritis, renal failure, and systemic lupus erythematosus [1].

Anifrolumab（MEDI-546） is a potent type I interferon (IFN) receptor antagonist, a human monoclonal antibody that targets IFN.Anifrolumab inhibits the activity of type I interferon and is used for the prevention and treatment of systemic lupus erythematosus (SLE).

Prezalumab (AMG 557) is a human IgG2 monoclonal antibody against ICOSL and BAFF. Prezalumab can be used to study sjogren's syndrome cutaneous lupus erythematosus, psoriasis, systemic lupus erythematosus arthritis and systemic lupus erythematosus (SLE).