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CIAS

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30

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3

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2

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-162011

    EBI2/GPR183 Inflammation/Immunology
    GPR183 antagonist-2 (compound 32) is a selective GPR183 antagonist with good water solubility and excellent pharmacokinetic properties. GPR183 antagonist-2 significantly reduces paw and joint swelling and gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a collagen-induced arthritis (CIA) mouse model in a dose-dependent manner. GPR183 antagonist-2 can be used in the study of autoimmune diseases .
    GPR183 antagonist-2
  • HY-110177

    NF-κB Inflammation/Immunology
    SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA) .
    SP-100030
  • HY-123133

    Kallikrein Inflammation/Immunology
    PKSI-527 is a new, highly selective plasma kallikrein inhibitor. PKSI-527 can suppress collagen-induced arthritis (CIA) by modifying the kallikrein-kinin system .
    PKSI-527
  • HY-153321

    BTK-IN-24

    Btk PROTACs Inflammation/Immunology Cancer
    NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
    NX-5948
  • HY-131903

    IRAK Inflammation/Immunology
    HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties .
    HS271
  • HY-125997

    Btk Inflammation/Immunology
    BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment .
    BTK inhibitor 10
  • HY-P5003

    MMP Inflammation/Immunology
    Collagen Type II Fragment is an anti-inflammatory peptide that potently inhibits collagen-induced arthritis (CIA) in mice. Collagen Type II Fragment can be used for research on inflammation and immunity .
    Collagen Type II Fragment
  • HY-112863

    ROR Inflammation/Immunology
    RORγt inhibitor 3 is an orally active and potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor. RORγt inhibitor 3 shows high binding affinity and inhibitory activity of Th17 cell differentiation. RORγt inhibitor 3 also shows efficacy in both mouse experimental autoimmune encephalomyelitis (EAE) and collagen induced arthritis (CIA) models .
    RORγt inhibitor 3
  • HY-155031

    Reactive Oxygen Species COX Inflammation/Immunology Cancer
    MCI alleviates inflammation by macrophage reprogramming via targeting ROS scavenging and COX-2 downregulation. MCI inhibits COX-2 with an IC50 value of 1.23 μM. MCI has significant anti-inflammatory effects in collagen-induced arthritis (CIA) models. MCI can be used in research for rheumatoid arthritis (RA) .
    MCI
  • HY-119245

    BMS-986166

    LPL Receptor Inflammation/Immunology
    Udifitimod (BMS-986166) is a potent, selective and orally active S1P1R modulator. Udifitimod has the potential for the research of autoimmune diseases .
    Udifitimod
  • HY-168625

    Molecular Glues Inflammation/Immunology
    VAV1 degrader-3 (Example 185) is an orally active VAV1 molecular glue degrader (DC50: 7 nM). VAV1 degrader-3 reduces immune cell activation, immune cell proliferation and the production of various cytokines. VAV1 degrader-3 can be used for research of inflammatory or autoimmune disorder. VAV1 degrader-3 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc. .
    VAV1 degrader-3
  • HY-156190

    Others Cancer
    NR2F6 modulator-2 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F6 modulator-2 substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F6 modulator-2 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
    NR2F2-IN-1
  • HY-13207A
    ONX-0914 TFA
    10+ Cited Publications

    PR-957 TFA

    Proteasome Bacterial HIV Infection Inflammation/Immunology
    ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .
    ONX-0914 TFA
  • HY-161354

    JAK Apoptosis Inflammation/Immunology
    JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability .
    JAK3 covalent inhibitor-2
  • HY-10999
    Trametinib
    Maximum Cited Publications
    184 Publications Verification

    GSK1120212; JTP-74057

    MEK Autophagy Apoptosis Cancer
    Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
    Trametinib
  • HY-10999A
    Trametinib (DMSO solvate)
    Maximum Cited Publications
    184 Publications Verification

    GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)

    MEK Apoptosis Cancer
    Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis .
    Trametinib (DMSO solvate)
  • HY-B0524A

    Histamine Receptor Neurological Disease Inflammation/Immunology Endocrinology
    Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .
    Betahistine dihydrochloride
  • HY-18054
    BVT 2733
    3 Publications Verification

    11β-HSD Inflammation/Immunology
    BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease .
    BVT 2733
  • HY-B0524

    Histamine Receptor Inflammation/Immunology Cancer
    Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine is used for the study of rheumatoid arthritis (RA) .
    Betahistine
  • HY-139780

    ROR Inflammation/Immunology
    JNJ-61803534 is a potent and orally active RORγt inverse agonist with an IC50 of 9.6  nM. JNJ-61803534 has anti-inflammatory activity. JNJ-61803534 inhibits IL-17A production in human CD4+ T cells under Th17 differentiation conditions .
    JNJ-61803534
  • HY-10999R

    MEK Autophagy Apoptosis Cancer
    Trametinib (Standard) is the analytical standard of Trametinib. This product is intended for research and analytical applications. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
    Trametinib (Standard)
  • HY-B0524AR

    Histamine Receptor Neurological Disease Inflammation/Immunology Endocrinology
    Betahistine (dihydrochloride) (Standard) is the analytical standard of Betahistine (dihydrochloride). This product is intended for research and analytical applications. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .
    Betahistine dihydrochloride (Standard)
  • HY-163651

    (R)-CR6086

    Prostaglandin Receptor Inflammation/Immunology
    (R)-Vorbipiprant ((R)-CR6086) is an orally active antagonist for prostaglandin E2 receptor 4 (EP4) with Ki of 16.6 nM for human EP4. (R)-Vorbipiprant inhibits PGE2 (HY-101952)-induced cAMP production with an IC50 of 22 nM. (R)-Vorbipiprant exhibits immunomodulatory and anti-angiogenic activities, and ameliorates the collagen-induced arthritis in mice .
    (R)-Vorbipiprant
  • HY-163673

    Glucocorticoid Receptor Drug-Linker Conjugates for ADC Inflammation/Immunology
    Glucocorticoid receptor modulator 4 (Compound DL5) is a conjugate of a linker and a glucocorticoid receptor modulator. Glucocorticoid receptor modulator 4 exhibits GRE Reporter activity in mTNF expressing K562 cell with an EC50 of 40 μM. Glucocorticoid receptor modulator 4 binds with an anti-tumor necrosis factor (TNF) antibody, and exhibits anti-inflammtory activity against arthritis in mouse models .
    Glucocorticoid receptor modulator 4
  • HY-N0976

    11b-Hydroxy-11b,1-dihydromedicarpin

    Interleukin Related Inflammation/Immunology
    1,11b-Dihydro-11b-hydroxymedicarpin (11b-Hydroxy-11b,1-dihydromedicarpin) is a pterocarpan from Ononis viscosa subsp. breviflora is a Medicarpin derivative . Medicarpin, a natural pterocarpan, heals cortical bone defect by activation of Notch and Wnt canonical signaling pathways . Medicarpin prevents arthritis in post-menopausal conditions by arresting the expansion of TH17 cells and pro-inflammatory cytokines. Medicarpin down-regulates pro-inflammatory cytokines like TNF-α, IL-6 and IL-17A, while up-regulates anti-inflammatory cytokine IL-10 in arthritis (CIA) model of mice .
    1,11b-Dihydro-11b-hydroxymedicarpin
  • HY-135844
    LS-102
    2 Publications Verification

    E1/E2/E3 Enzyme Inflammation/Immunology
    LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment .
    LS-102
  • HY-153808B

    Toll-like Receptor (TLR) Inflammation/Immunology
    Complete Freund's adjuvant (CFA, 1 mg/ml) is an immunoadjuvant emulsified with antigen that can enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA, 1 mg/ml) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA, 1 mg/ml) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA, 1 mg/ml) stimulates a strong and durable immune response and can be used to induce rheumatoid arthritis in rats, and more .
    Complete Freund's adjuvant (CFA, 1 mg/ml)
  • HY-164102

    TNF Receptor NF-κB Inflammation/Immunology
    TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
    TNF-α-IN-18
  • HY-101490

    Phosphodiesterase (PDE) Neurological Disease
    PDE1-IN-2 is a PDE1 inhibitor extracted from patent WO2016/55618 A1, example 31. PDE1-IN-2 has IC50 values of 6 nM, 140 nM and 164 nM for PDE1C, PDE1B and PDE1A, respectvely. PDE1-IN-2 is developed for the research of neurodegenerative disorders and psychiatric disorders .
    PDE1-IN-2
  • HY-153808
    Complete Freund's adjuvant (CFA)
    4 Publications Verification

    Toll-like Receptor (TLR) Inflammation/Immunology
    Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response .
    Complete Freund's adjuvant (CFA)

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