systemic lupus erythematosus

TLR7 8 9 antagonist 2 is an orally active and highly bioavailable vTLR7 8 9 antagonist. It 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.

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.

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.

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

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

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.

Prednisolone hemisuccinate is a soluble glucocorticoid and cortisol, a prodrug of the glucocorticoid (GR) agonist Prednisone, which exerts anti-inflammatory, immunosuppressive, and antiallergic effects by binding to GR receptor, and is commonly used in systemic lupus erythematosus, acute dermatologic conditions, and arthritis.

(S)-Dexfadrostat ((S)-Fadrozole), an aromatase inhibitor, exhibits an IC 50 of 4.6 nM in in vitro assays using human placental microsomes. It is applicable for research on estrogen-dependent breast cancer, gynecomastia, and systemic lupus erythematosus.

(S)-Hydroxychloroquine ((S)-HCQ) sulfate is an isomer of Hydroxychloroquine. At concentrations of 2.5-20 mg mL, (S)-Hydroxychloroquine sulfate can reduce the rate of insulin degradation in liver homogenates isolated from both non-diabetic and diabetic rats. Preparations containing Hydroxychloroquine have been used in studies of malaria, rheumatoid arthritis, and systemic lupus erythematosus.

KV1.3-IN-2 (Compound I) selectively inhibits the kv1.3 potassium channel without affecting the hERG channel. It is applicable in research related to immune-associated diseases such as psoriasis, rheumatoid arthritis, and systemic lupus erythematosus.

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

PAD-IN-2, a potent inhibitor of PAD4 with an IC50 value <1 μM, can be utilized to study autoimmune diseases and cancers, including rheumatoid arthritis, vasculitis, systemic lupus erythematosus, cutaneous lupus erythematosus, cystic fibrosis, ulcerative colitis, asthma, multiple sclerosis, and psoriasis.

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

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].

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].

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].

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].

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].

Avizakimab (BOS161721) is a humanized lgG1 monoclonal antibody that targets and inhibits the biological activity of IL-21, with potential for the treatment of systemic lupus erythematosus (SLE).

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.

Dapirolizumab is an anti-CD40 monoclonal antibody used in research on systemic lupus erythematosus (SLE) and other autoimmune diseases.

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 targeting ICOSL and BAFF, used for studying Sjogren's syndrome, cutaneous lupus erythematosus, psoriasis, systemic lupus erythematosus arthritis, and systemic lupus erythematosus (SLE).