Inflammation/Immunology

Dyclonine (Dyclocaine) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.

HuGAL-F2 is a human-derived antibody expressed in CHO cells, targeting FGF2. HuGAL-F2 contains a huIgG2 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for HuGAL-F2 can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

Experimental allergic encephalitogenic peptide (human) is a EAE peptide. Experimental allergic encephalitogenic peptide (human) induces encephalomyelitis in guinea pigs.

MRS7925 (Compound 43) is a 5-HT_2BR antagonist (K_i: 17 nM). MRS7925 can be used for research of fibrosis.

Menaquinone-9-d7 is the deuterated-labeled Menaquinone 9 (HY-131501). Menaquinone 9 is a naphthoquinone-type vitamin K and electron transport component produced by bacteria. Menaquinone 9 is an orally active analog of Vitamin K2 (HY-109569). Menaquinone 9 acts as an ultraviolet-sensitive, photooxidizable substrate that generates more polar photodegradation products under oxygen and ultraviolet irradiation. Menaquinone 9 binds to the αβ dimer of Escherichia coli nitrate reductase, supporting electron transport within the αβ subunit structure of the enzyme. Menaquinone 9 serves as a precursor for bone Menaquinone-4 (HY-B2156). Menaquinone 9 can be used in studies related to metabolic diseases.

Clobetasol propionate-d₅ is a deuterium substitute of Clobetasol propionate. Clobetasol propionate is a potent, selective CYP3A5 inhibitor with a IC₅₀ of 0.206 μM and has potential for use in the study of psoriasis and other skin diseases.

Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury.

JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC₅₀ value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases.

15(R)-Prostaglandin F2α is the isomer of 9α,11β-Prostaglandin F2α (HY-129953). 9α,11β-Prostaglandin F2α is an endogenous metabolite present in Urine that can be used for the research of Asthma.

24-O-Acetyllycoclavanol (compound 1) is a triterpenoid anti-inflammatory agent that selectively targets the NF-κB and ERK1/2 signaling pathways. It exerts its anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) and COX-2 expression, reducing the production of inflammatory mediators such as nitric oxide (NO), IL-1β, and IL-8. 24-O-Acetyllycoclavanol can be used in research related to inflammatory bowel disease (IBD). 24-O-Acetyllycoclavanol can be biologically isolated from the ethyl acetate extract of Lycopodium clavatum.

(Z)-Onjisaponin B ((Z)-Senegin III) is a derivative of Onjisaponin B (HY-N2099). Onjisaponin B is an orally active natural product derived from Polygala tenuifolia. Onjisaponin B inhibits NF-κB p65. Onjisaponin B enhances autophagy and accelerates the degradation of mutant α-synuclein and huntingtin. Onjisaponin B reduces β-amyloid (Aβ) production. Onjisaponin B reduces radiation-induced cell apoptosis. Onjisaponin B has anti-oxidant and anti-inflammatory activities. Onjisaponin B can be used for neurological disease and radiation injury study, and its metabolite tenuifolin (TF) can enter the brain through the BBB.

COX-2/5-LOX-IN-8 is an orally active dual COX-2/5-LOX inhibitor, with an IC₅₀ of 6.30 μM against sheep-derived COX-2 and an IC₅₀ of 8.09 μM against 5-LOX. COX-2/5-LOX-IN-8 acts as a membrane stabilizer that stabilizes erythrocyte membranes against hypotonicity-induced hemolysis. COX-2/5-LOX-IN-8 functions as a protein stabilizer that inhibits heat-induced denaturation of bovine serum albumin. COX-2/5-LOX-IN-8 reduces paw swelling, improves hind limb weight-bearing function, decreases serum levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, CRP), and lowers serum levels of cartilage degradation biomarkers (COMP, MMP-3, CTX-II). COX-2/5-LOX-IN-8 can be used in the research of osteoarthritis.

VUF10132 is a non-peptide CXCR3 receptor antagonist with anti-inflammatory activity, inhibiting diseases such as rheumatoid arthritis, multiple sclerosis, and psoriasis. VUF10132 has high affinity for the human CXCR3 receptor but slightly lower affinity for the murine CXCR3 receptor. Additionally, VUF10132 exhibits inverse agonist properties at the CXCR3 receptor.

IOR-T3 is a monoclonal antibody targeting CD3, with biological activities related to T cell activation regulation. IOR-T3 uses its variable region to competitively engage surface CD3 on lymphocytes and trigger robust T cell proliferation and activation. IOR-T3 and its derivatives can be used in studies related to acute transplant rejection.

O-Methyl Atorvastatin (hemicalcium) is an impurity of Atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, has the ability to effectively decrease blood lipids.

COX-2/CA II-1 is an orally active dual selective inhibitor targeting COX-2 and hCA II. COX-2/CA II-1 inhibits COX-2 with an IC₅₀ value of 0.13 μM (SI = 9.25 vs COX-1) and hCA II with a K_i value of 39.1 nM (SI = 933.8 vs hCA I). COX-2/CA II-1 demonstrates significant analgesic and anti-inflammatory effects in animal models, shows improved gastric safety with reduced ulcerogenic liability, and exhibits intraocular pressure (IOP)-lowering effects in rabbit glaucoma models. COX-2/CA II-1 can be used for anti-inflammatory, analgesic and antiglaucoma research.

Pyrazinobutazone (Phenylbutazone piperazium) is an antipyrene derivative that possesses anti-inflammatory properties and has been associated with hypersensitivity reactions leading to agranulocytosis and liver injury.

Rosemary extract is an extract of rosemary (Salvia rosmarinus) with biological activities such as liver protection, antifungal, insecticidal, antioxidant and antibacterial properties.

REGN6490 is a humanized monoclonal anti-IL1RL2/IL-36R antibody. REGN6490 can be used in research related to pustular psoriasis.

STING agonist-10 (Compound 91) is a potent small molecule cyclic urea activator of STING with the EC₅₀ of 2600 nM. Activation of STING is a highly promising approach in immunotherapy.