Inflammation/Immunology

Isothipendyl hydrochloride (), an azaphenothiazine derivative, is a potent histamine 1 (H1) receptor antagonist.othipendyl is a primary metabolite.

CI 972 anhydrous is a potent, orally active, and competitive inhibitor of purine nucleoside phosphorylase (PNP) (K_i=0.83 μM) under development as a T cell-selective immunosuppressive agent.

LRRK2/NUAK1/TYK2-IN-1 (conpound 226) shows inhibitory activity toward LRRK2 (Wt), LRRK2 (G2019), TYK2 and NUAK1, with IC₅₀ values lower than 10 nM. LRRK2/NUAK1/TYK2-IN-1 can be used for autoimmune disease research.

CP-944629 (Compound 20) is an inhibitor of p38 alpha kinase with an IC₅₀ of 3.2. CP-944629 can be studied in research for chronic inflammation diseases.

dTAG-TRIMTAC is a PROTAC-like degrader targeting TRIM21. dTAG-TRIMTAC forms a ternary complex with TRIM21 and target proteins to drive degradation of oligomeric/assembled substrates via TRIM21 clustering-based activation, with degradation dependent on endogenous TRIM21. dTAG-TRIMTAC can be used for the research of neurodegenerative disease and inflammatory disease.

Catalposide, an iridoid glycoside that could be isolated from Catalpa ovate G. Don (Bignoniaceae), inhibits TNF-α, IL-1β, and IL-6 productions and NF-κB (p65) activation in lipopolysaccharide-activated RAW 264.7 macrophages.

16α-Hydroxyprednisolone-d₅ (OH-PRED-d₅) is the deuterium labeled 16α-Hydroxyprednisolone (HY-117580). 16α-Hydroxyprednisolone (OH-PRED) is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid Budesonide (HY-13580). 16α-Hydroxyprednisolone formation is catalyzed by isoenzymes within the cytochrome P450 3A (CYP3A) subfamily. 16α-Hydroxyprednisolone formation can be inhibited by antibodies targeting the CYP3A subfamily.

Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor of carbonic anhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), and has anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 67 has IC₅₀s of 10.4 μM and 50 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 67 binding to different isoforms of carbonic anhydrase are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII).

AVSEHQLLHDKGKSIQDLRRRFFLHHLI-{Aib}-EIHTAYRFGG promotes bone-ossification. AVSEHQLLHDKGKSIQDLRRRFFLHHLI-{Aib}-EIHTAYRFGG can be used in the research of diseases or disorders related to osteogenic defects or bone mineral density (BMD) decreasing, such as osteoporosis.

Belamcandae rhizoma extract (Belamcanda extract) is an extract of Belamcanda chinensis (L.) DC., which has antioxidant, anti-inflammatory and anti-tumor activities.

Anti-inflammatory agent 114 is an anti-inflammatory agent. Anti-inflammatory agent 114 binds to the allosteric inhibitory pocket in the NLRP3 NACHT domain. Anti-inflammatory agent 114 inhibits the expression of iNOS, COX-2 and NLRP3. Anti-inflammatory agent 114 can be used for the research of inflammatory diseases.

Nepetoidin B, an anti-inflammatory agent, inhibits inflammation by modulating the NF-κB and Nrf2/HO-1 signaling pathways. Nepetoidin B also has antifungal and antibacterial activity. Nepetoidin B is a natural product that can be obtained from Salvia plebeia R. Br. Nepetoidin B can be used in anti-inflammatory and anti-infectious research.

ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC₅₀ = 0.68 μM) and TLR9 (IC₅₀ = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research.

TLR7 agonist 20 is a selective Toll-like receptor 7 (TLR7) agonist with an EC₅₀ of 0.22 μM. TLR7 agonist 20, as an immunostimulant and vaccine adjuvant, enhances the production of anti-spike protein antibodies, increases IgG2b and IgG2c levels, and thereby drives Th1-type immune responses in mice. TLR7 agonist 20 can be used in studies related to non-inflammatory potent vaccine adjuvants.

Brombuterol-d₉ (hydrochloride) is a deuterium labeled Brombuterol hydrochloride. Brombuterol hydrochloride is a β-adrenergic receptor agonist.

MMP-13 Substrate TFA is a substrate of MMP-13. MMP-13 Substrate TFA can be used for the research of osteoarthritis (OA).

Urolignoside is an antioxidant with free radical scavenging activity. Urolignoside potently scavenges DPPH radical, and exhibits antioxidant to β-carotene-lineoleate model. 3'-Azido-3'-deoxyguanosine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

Gusacitinib-d₄ (ASN-002-d₄) is the deuterium labeled Gusacitinib (HY-103018). Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC₅₀ values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma.

PROTAC HDAC6 degrader 10 is a highly efficient, safe and selective HDAC6 PROTAC degrader with a pIC₅₀ of 8.75 and a pDC₅₀ of 9.2 in BEAS-2B cells. PROTAC HDAC6 degrader 10 recruits cereblon to form a ternary complex with HDAC6, thereby achieving the degradation of HDAC6. PROTAC HDAC6 degrader 10 significantly induces hyperacetylation of α-tubulin without affecting the acetylation of H3, and achieves sustained HDAC6 knockdown in mouse lung tissues. PROTAC HDAC6 degrader 10 exhibits high bioavailability after subcutaneous administration in mice. PROTAC HDAC6 degrader 10 enables the study of HDAC6 pharmacology via chemical knockdown of HDAC6 in vitro and in vivo, and can be used for research on pulmonary diseases.

Nemonoxacin-d₃-1 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia.