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    Molibresib (I-BET762; GSK-525762A)
    Molibresib (I-BET762; GSK-525762A)

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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 #: V0414
    CAS #: 1260907-17-2Purity ≥98%

    Description: Molibresib (also known as GSK525762A, I-BET-762, GSK-525762) is a novel and potent inhibitor for BET (Bromodomain and Extra-Terminal) family of proteins with potential anti-inflammatory and anticancer activity. It inhibits BET with IC50 of ~35 nM in a cell-free assay. It suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, and is highly selective over other bromodomain-containing proteins. GSK525762 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides.

    References: Nature. 2010 Dec 23;468(7327):1119-23; Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14532-7.

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    I-BET-762

    Name: Molibresib
    CAS#: 1260907-17-2
    Chemical Formula: C22H22ClN5O2
    Exact Mass: 423.1462
    Molecular Weight: 423.9
    Elemental Analysis: C, 62.34; H, 5.23; Cl, 8.36; N, 16.52; O, 7.55
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: GSK-525762; GSK525762;IBET762; IBET 762; IBET-762; GSK 525762;  GSK-525762A; GSK 525762A; GSK525762A; 
    Chemical Name: (S)-2-(6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
    InChi Key: AAAQFGUYHFJNHI-SFHVURJKSA-N
    InChi Code: InChI=1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1
    SMILES Code: O=C(NCC)C[[email protected]]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1


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    In Vitro

    In vitro activity: I-BET-762 is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4, binds to the tandem bromodomains of BET with Kd of 50.5–61.3 nM, displaces a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5–42.5 nM in FRET analysis. I-BET-762 occupies the acetyl-lysine binding pocket of BET proteins and inhibits binding of BET proteins to acetylated histones, thus disrupts the formation of the chromatin complexes essential for expression of inflammatory genes. I-BET-762 treatment during the first 2 d of differentiation alters CD4+ T-cell cytokine production, up-regulated expression of several antiinflammatory gene products and down-regulated expression of several proinflammatory cytokines.


    Kinase Assay: Fluorescence resonance energy transfer (FRET) titrations. I-BET is titrated against BRD2 (200 nM), BRD3 (100 nM) and BRD4 (50 nM) in 50 mM HEPES pH7.5, 50 mM NaCl, 0.5 mM CHAPS in the presence of tetra-acetylated Histone H4 peptide (200 nM). After equilibrating for 1 hour, the bromodomain protein : peptide interaction is detected using FRET following the addition of 2nM Europium cryptate labelled streptavidin and 10 nM XL-665-labelled anti-6His antibody in assay buffer containing 0.05% (v/v) BSA and 400 mM KF. Plates are read using an Envision Plate reader (excitation 320 nm, emission 615 nm and 665 nm).


    Cell Assay: CD4+ T cells are isolated from lymph nodes and spleens of 10- to 12-wk old mice and activated with plate bound anti-CD3 and anti-CD28 antibodies in the presence of indicated cytokines. I-BET-762 compounds is included during the 60–72 h of initial activation. Over the course of 5 d of T-cell culture and expansion, the compounds is diluted 12-fold relative to the starting concentrations.

    In VivoI-BET-762 confers protection against lipopolysaccharide-induced endotoxic shock and bacteria induced sepsisa. Single dose of I-BET applied at 1.5 h after LPS injection cures the mice. Twice-daily injections of I-BET for 2 days protects mice against death caused by sepsis. Limited treatment with I-BET-762 exclusively during early priming inhibited the ability of Th1-differentiated 2D2 T cells to induce neuroinflammation in a mouse model of experimental autoimmune encephalomyelitis (EAE).
    Animal modelMouse model
    Formulation & DosageDissolved in 20% beta-cyclodextrin, 2% DMSO in 0.9% saline; 30mg/kg;  i.v. injection
    References

    Nature. 2010 Dec 23;468(7327):1119-23; Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14532-7.


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

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