Multiple Sclerosis

RIPK1-IN-43 is a triazolopyridine compound and also a RIPK1 inhibitor. RIPK1-IN-43 can be used in the research of diseases associated with abnormal RIPK1, such as multiple sclerosis, Parkinson's disease, non-alcoholic steatohepatitis, etc.

2ccPA (2ccPA18:1) sodium is a chemically stable cyclic phosphatidic acid derivative and antifibrotic inhibitor-inducer. 2ccPA sodium increases intracellular cAMP levels in skin fibroblasts, downregulates the expression of extracellular matrix (ECM) components, and promotes the production of antifibrotic factors HGF and PGE₂. 2ccPA sodium ameliorates Bleomycin hydrochloride (HY-17565A)-induced skin fibrosis in mice and can be used for research on systemic sclerosis (SSc) and other fibrotic disorders.

HDAC degrader-2 is a HDAC degrader, and its DC₅₀ for HDAC1 in MM.1S cells is 2.55 μM. HDAC degrader-2 recruits and covalently binds to DDB1, thereby inducing proteasomal degradation of HDAC1 and HDAC2. HDAC degrader-2 inhibits HDAC6 activity and increases the acetylation levels of α-tubulin and histone H3. HDAC degrader-2 induces early and late apoptosis and reduces the proliferative capacity of cancer cells. HDAC degrader-2 can be used for research on multiple myeloma and breast cancer.

CN045 is a blood-brain barrier-permeable, selective M1 muscarinic receptor ligand with an IC₅₀ value of 1 μM. CN045 enhances remyelination in mouse brain regions. CN045 can be used in studies related to multiple sclerosis.

FGFR3-IN-10 is a FGFR3 inhibitor with an IC₅₀ of <350 nM. FGFR3-IN-10 is applicable to research related to cancer, systemic sclerosis, fibrosis, achondroplasia, thanatophoric dysplasia, and Muenke syndrome.

A-3190 is an orally active, blood-brain barrier permeable CD38 inhibitor, with an IC₅₀ of 7.25 nM against human CD38 and 1.24 nM against mouse CD38. A-3190 is a derivative of A-8531 (HY-184021), and it forms covalent adducts with NAD⁺ in the presence of CD38. A-3190 acts as an inducer of NAD⁺ levels and an inhibitor of NAM and ADPR levels. A-3190 increases NAD⁺ levels in the skin, lung, liver and brain of rodents, while reducing NAM and ADPR levels in brain tissues. A-3190 can be used in research related to multiple sclerosis, Parkinson's disease and Alzheimer's disease.

Rolipram GMP is Rolipram (HY-16900) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.

IC 100 is a humanized IgG4κ monoclonal antibody targeting apoptosis-associated speck-like protein (ASC) with blood-brain barrier permeability. IC 100 specifically inhibits ASC after being endocytosed via its Fc segment, blocks ASC polymerization and inflammasome activation, suppresses IL-1β release, forms complexes with ASC and TRIM21, and evades TRIM21-mediated proteasomal degradation. IC 100 alleviates symptoms associated with autoimmune encephalomyelitis, reduces immune cell infiltration and microglial activation in the mouse EAE model. IC 100 is suitable for research on neuroinflammatory and inflammasome-related diseases such as multiple sclerosis. Isotype comparison: HY-P99003.

RO-7303509 (MTBT1466A; RG-6315) is a human monoclonal antibody and TGFβ3 neutralizer. RO-7303509 targets the profibrotic mediator TGFβ3 to alleviate fibrosis. RO-7303509 can be administered via subcutaneous or intravenous routes and is used in research on systemic sclerosis. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).

C26-Dihydro ceramide is a dihydroceramide containing a C26 very-long-chain fatty acid. C26-Dihydro ceramide can be used for research on various neurological disorders including Alzheimer's disease, Parkinson's disease, multiple sclerosis, depression, and anxiety disorders.

Buloxibutid (AT2 receptor agonist C21) hydrochloride is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a K_i value of 0.4 nM for porcine AT2R. Buloxibutid hydrochloride exerts vasodilatory, anti-inflammatory, antifibrotic (promoting the expression of collagenase MMP-13) and tissue repair effects mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway and inflammatory NF-κB pathway. Buloxibutid hydrochloride can be used in research related to idiopathic pulmonary fibrosis, hypertension, systemic sclerosis and other conditions.

CS1P1 is a brain-penetrant and selective S1PR1 antagonist and PET radiotracer, with human S1PR1 IC₅₀ values of 2.1 nM. CS1P1 binds specifically to S1PR1 to enable in vivo receptor expression quantification. CS1P1 can be used as PET radiotracer when labelled with 11C. CS1P1 can be used for the research of multiple sclerosis, neointimal hyperplasia, vascular inflammation.

BTK-IN-49 is a selective, orally active and brain-penetrant BTK inhibitor with an IC₅₀ of 0.14 nM. BTK-IN-49 binds to BTK and blocks B-cell receptor and Fcγ receptor signaling. BTK-IN-49 inhibits the proliferation of CNS-compartmentalized B-cells and FcγR-induced microglial proliferation in a BTK-dependent manner. BTK-IN-49 can be used for the study of multiple sclerosis.

KLK6-IN-1 is a reversible small‑molecule inhibitor of KLK6, KLK1, and plasmin. KLK6-IN-1 shows IC₅₀ values of 1.57 μM (KLK6), 5.1 μM (KLK1), 7.4 μM (plasmin), and K_i values of 0.8 μM (KLK6), 2.4 μM (KLK1), 1.3 μM (plasmin). KLK6-IN-1 is highly selective for KLK6 and its proteolytic network. KLK6-IN-1 induces oligodendrocyte differentiation by promoting oligodendrocyte precursor cell maturation. KLK6-IN-1 can be used for the research of multiple sclerosis.

(R)-HM5023507 (Compound 470) is a potential PI3K inhibitor. (R)-HM5023507 can be used for the research of cancer, inflammatory, allergic and autoimmune diseases and leukemia etc.

EED-IN-5 is an orally active, EZH2-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC₅₀ value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis.

EED-IN-4 is an orally active, EZH2-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC₅₀=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis.

ERβ agonist-2 (Page 72) is a selective ERβ agonist with an EC₅₀ of 800 nM or lower. ERβ agonist-2 selectively inhibits T cell activation and/or proliferation, thereby reducing circulating T cell levels in subjects, without exerting significant effects on circulating neutrophil, monocyte or B cell levels. ERβ agonist-2 is applicable to studies of chronic heart failure after myocardial infarction, as well as graft-versus-host disease, multiple sclerosis and experimental autoimmune encephalomyelitis.

BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with K_i values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis.

Vitedoamine A is a Phenylnaphthalene-type lignan alkaloid. Vitedoamine A can be isolated from Vitex negundo. Vitedoamine A inhibits the activity of IKKβ with an IC₅₀ value of 39 μM. Vitedoamine A could inhibit the transcriptional activity of NF-κB, and suppress the production of NO and reduce the expressions of inflammatory cytokines (IL-1β, IL-6, and TNF-α). Vitedoamine A inhibits the phosphorylation of IKKα/β and p65, and prevents the degradation of IκBα. Vitedoamine A possesses anti-rheumatoid arthritis capacity.