1. Immunology/Inflammation
  2. STING
  3. diABZI STING agonist-1 (tautomerism)

diABZI STING agonist-1 (tautomerism) 

Art. -Nr.: HY-112921 Reinheit: 99.91%
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diABZI STING agonist-1 tautomerism is a tautomerism of diABZI STING agonist-1 (HY-112921A). diABZI STING agonist-1 tautomerism is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

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CAS. Nr. : 2138498-18-5

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Based on 2 publication(s) in Google Scholar

Other Forms of diABZI STING agonist-1 (tautomerism):

Top Publications Citing Use of Products

2 Publications Citing Use of MCE diABZI STING agonist-1 (tautomerism)

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    diABZI STING agonist-1 (tautomerism) purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Dec;32(12):1086-1104.  [Abstract]

    Western blot analysis of EVPs isolated from HeLa, HCT116, and B16F10 cells treated with or without 10 µM STING agonist-1 (diABZI), 1 µM cGAMP, or 50 µg/mL DMXAA for 48 h.

    diABZI STING agonist-1 (tautomerism) purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Dec;32(12):1086-1104.  [Abstract]

    Immunofluorescence analysis of STING (green) and Flag-RAB22AQ64L (red) in stable Flag-RAB22AQ64L NCI-H1975 cells treated with or without 1 µM STING agonist-1 (diABZI) for 1 h.

    diABZI STING agonist-1 (tautomerism) purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Dec;32(12):1086-1104.  [Abstract]

    Western blot analysis of the WCL of the indicated stable 4T1 cells at the indicated time points after treatment with 10 µM STING agonist-1 (diABZI).
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    Beschreibung

    diABZI STING agonist-1 tautomerism is a tautomerism of diABZI STING agonist-1 (HY-112921A). diABZI STING agonist-1 tautomerism is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively[1].

    IC50 & Target

    EC50: 130 nM (human STNG in PBMCs) [1].

    Cellular Effect
    Cell Line Type Value Description References
    H69AR EC50
    0.035 μM
    Compound: 5; GSK
    Agonist activity at STING in human THP1 Dual cells assessed as IRF reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay
    Agonist activity at STING in human THP1 Dual cells assessed as IRF reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay
    [PMID: 35108011]
    H69AR EC50
    0.055 μM
    Compound: 5; GSK
    Agonist activity at STING in human THP1-Dual cells assessed as NF-kappaB reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay
    Agonist activity at STING in human THP1-Dual cells assessed as NF-kappaB reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay
    [PMID: 35108011]
    In Vitro

    diABZI STING agonist-1 tautomerism is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    diABZI STING agonist-1 (subcutaneous injection; 2.5 mg/kg) tautomerism induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo[1].
    diABZI STING agonist-1 (intravenous injection; 3 mg/kg) tautomerism exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (200 ng/mL)[1].
    diABZI STING agonist-1 (intravenous injection; 1.5 mg/kg; 43 days) tautomerism results in significant tumour growth inhibition and significantly improves survival with 8 out of 10 mice remaining tumor free at the end of the study on day 43[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molekulargewicht

    849.94

    Formel

    C42H51N13O7

    CAS. Nr.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(N)C1=CC(N/C(N2C/C=C/CN3/C(NC4=C3C(OCCCN5CCOCC5)=CC(C(N)=O)=C4)=N/C(C6=CC(C)=NN6CC)=O)=N\C(C7=CC(C)=NN7CC)=O)=C2C(OC)=C1

    Versand

    Room temperature in continental US; may vary elsewhere.

    Speicherung

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Produktname:
    diABZI STING agonist-1 (tautomerism)
    Art. -Nr.:
    HY-112921
    Menge:
    MCE Japan Authorized Agent: