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  4. I-BET151 dihydrochloride

I-BET151 dihydrochloride  (Synonyms: GSK1210151A dihydrochloride)

Cat. No.: HY-110106
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I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.

For research use only. We do not sell to patients.

CAS No. : 1883545-47-8

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I-BET151 dihydrochloride Related Antibodies

Top Publications Citing Use of Products
Cell Proliferation/Viability Assay
WB
RT-PCR
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    I-BET151 dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079.  [Abstract]

    I-BET151 (5 μM; 3 h or overnight) inhibited LPS- and nigericin-mediated, NLRP3-driven pyroptosis of BMDMs.

    I-BET151 dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079.  [Abstract]

    I-BET151 (5 μM; overnight) reduced ASC oligomerization in macrophages following nigericin treatment and consequently limited caspase-1, GSDMD, and IL-1β processing into their bioactive fragments, including the release of cleaved caspase-1 and IL-1β into the cell supernatant.

    I-BET151 dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079.  [Abstract]

    I-BET151 (5 μM; overnight) prevented LPS-induced NLRP3 transcription and TLR-induced IL-1β transcription in BMDMs.

    I-BET151 dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079.  [Abstract]

    I-BET151 (0.2-5 μM; overnight) limited the LPS– and Pam3CSK4–induced expression of NLRP3 and IL-1β in BMDMs.

    I-BET151 dihydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jul 11;11(28):eadv0079.  [Abstract]

    I-BET151 (5-10 μM; overnight) largely rescued the loss of macrophage viability following nigericin treatment.

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    Description

    I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively[1][2].

    IC50 & Target

    pIC50: 6.1 (BRD4), 6.3 (BRD2), 6.6 (BRD3)[1]
    In Vitro

    I-BET151 dihydrochloride (1 μM; 72 hours) treatment displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation[2].
    I-BET151 dihydrochloride (100 nM; 72 hours) causes a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase[2].

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

    I-BET151 dihydrochloride Related Antibodies

    Cell Viability Assay[2]

    Cell Line: H929 cells
    Concentration: 1 μM
    Incubation Time: 72 hours
    Result: Displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation.

    Cell Proliferation Assay[2]

    Cell Line: H929 cells
    Concentration: 100 nM
    Incubation Time: 72 hours
    Result: Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase.
    In Vivo

    I-BET151 dihydrochloride demonstrates low blood clearance in the rat (~20% liver blood flow) and good oral systemic exposure which resulted in good oral bioavailability. High clearance is observed in the dog (~95% liver blood flow). The systemic exposure in the dog is low, resulting in a poor oral bioavailability of 16%. The high blood clearance in dog correlates well with the high intrinsic clearance observed in dog microsomes and hepatocytes, whereas the low intrinsic clearances seen in rat and mouse (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) correlate with lower in vivo blood clearances in these species. Due to the low systemic exposure observed in the dog, I-BET151 dihydrochloride is investigated in the mini-pig as a potential second species for toxicological evaluation where it showed low clearance (~32% liver blood flow) and good bioavailability (65%)[1].
    I-BET151 dihydrochloride (30 mg/kg; i.p.; daily for 21 days)-treats mice has four- to five fold smaller myeloma tumors and a significantly reduces rate of tumor size doubling than vehicle-treated mice[2].

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

    Animal Model: Mice (model of subcutaneous myeloma)[2]
    Dosage: 50 mg/kg
    Administration: I.p.; daily for 21 days
    Result: Reduced rate of tumor size doubling than vehicle-treated mice.
    Molecular Weight

    488.37

    Formula

    C23H23Cl2N5O3
    CAS No.
    SMILES

    [H]Cl.[H]Cl.C[C@@H](N1C(C(C=C(OC)C(C2=C(C)ON=C2C)=C3)=C3N=C4)=C4NC1=O)C5=CC=CC=N5
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    I-BET151 dihydrochloride Related Classifications

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    Help & FAQs
    • 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.

    Keywords:

    I-BET1511883545-47-8GSK1210151AEpigenetic Reader DomainBETbromodomainBRD4BRD2BRD3Inhibitorinhibitorinhibit

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