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    I-BET151 (GSK1210151A)
    I-BET151 (GSK1210151A)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0412
    CAS #: 1300031-49-5Purity ≥98%

    Description: I-BET151 (also known as GSK-1210151A) is a novel, potent and selective BET (Bromodomain and extra terminal domain) inhibitor with anticancer activity. It inhibits BRD2, BRD3 and BRD4 with IC50s of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively. I-BET151 has the similar inhibition function as TMZ. When tested with 6 myeloma cell lines, I-BET151 treatment decreased cells percent in S/G2 phase and increased cell apoptosis in a time- and dose- dependent manner. In globlastoma cell line U87MG, administration of I-BET151 arrested cells in the G1 phase and reduced cell proliferation ability.

    References: Nature. 2011 Oct 2;478(7370):529-33.

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    Molecular Weight (MW)415.44
    CAS No.1300031-49-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 27 mg/mL (65.0 mM)
    Water: <1 mg/mL
    Ethanol:  <1 mg/mL
    SMILESO=C(N1[[email protected]@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3
    Synonyms7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-oneGSK-1210151A; GSK 1210151A; GSK1210151A; IBET-151; IBET 151; IBET151; 

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    In Vitro

    In vitro activity: I-BET151 exhibits potent selectivity over an extensive range of diverse protein types such as COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, and transporters. Similar to I-BET762 (GSK525762A), I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with KD of 0.02-0.1 μM, and significantly inhibits lipopolysaccharide-stimulated IL-6 cytokine production in human peripheral blood mononuclear cells (PBMC) and whole blood (WB) as well as rat WB with IC50 of 0.16 μM, 1.26 μM, and 1.26 μM, respectively. I-BET151 (0.5 or 5 μM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins in HL60 nuclear extract to acetylated histone peptides. I-BET151 has potent efficacy against cell lines harboring different MLL-fusions such as MV4;11, RS4;11, MOLM13, and NOMO1 cells with IC50 of 15-192 nM. Consistently, I-BET151 completely ablates the colony-forming potential of MLL-fusion-driven leukaemias (MOLM13) but not leukaemias driven by tyrosine kinase activation (K562). I-BET151 also displays potent efficacy in both liquid culture and clonogenic assays using primary murine progenitors transformed with either MLL-ENL or MLL-AF9. I-BET151 treatment significantly induces apoptosis and prominent G0/G1 arrest in MLL-fusion cell lines driven by distinct MLL fusions (MOLM13 and MV4;11 containing MLL-AF9 and MLL-AF4, respectively) but not the K562 cells, probably due to the inhibition of transcription of BCL2, C-MYC and CDK6 by blocking the recruitment of BRD3/4, PAFc and SEC components into transcriptional start site (TSS).

    Kinase Assay: All components are dissolved in buffer of composition 50 mM HEPES pH 7.4, 150 mM NaCl and 0.5 mM CHAPS with final concentrations of BRD 2/3/4 75 nM, fluorescent ligand 5 nM. 10 μL of this reaction mixture is added using a micro multidrop to wells containing 100 nL of various concentrations of I-BET151 or DMSO vehicle (1% final) in Greiner 384 well Black low volume microtitre plate and equilibrated in the dark for 60 minutes at room temperature. Fluorescence anisotropy is read in Envision (lex = 485 nm, lEM = 530 nm; Dichroic = 505 nM). 

    Cell Assay: Cells are exposed to various concentrations of I-BET151 for 24 or 72 hours in 384-well or 96-well plates. For cell growth inhibition assays, plates are added with CellTiter-Glo reagent using a volume equivalent to the cell culture volume in the wells, shaken for approximately 2 minutes and chemiluminescent signal is read on the Analyst GT or EnVision Plate Reader. For cell proliferation assays, CellTiter-Aqueous One is added to each well and plates are incubated for 4 hours at 37 °C. Absorbance is read at 490 nm on a SpectraMax Gemini reader.

    In VivoAdministration of I-BET151 at 30 mg/kg/day significantly inhibits tumor growth of murine MLL-AF9 and human MLL-AF4 leukaemia in mice, and provides marked survival benefit.
    Animal model NOD-SCID mice injected intravenously with MV4;11 cells, and C57BL/6 mice injected intravenously with MLL-AF9 cells
    Formulation & DosageDissolved in normal saline containing 5% (v/v) DMSO and 10% (w/v) Kleptose HPB; 30 mg/kg;  i.p. injection

    Nature. 2011 Oct 2;478(7370):529-33.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    I-BET151 (GSK1210151A)

    I-BET151 is efficacious in in vivo murine models and primary patients samples of MLL-fusion leukaemia. Nature. 2011 Oct 2; 478(7370): 529–533.


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