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I-BET762

CAS No. 1260907-17-2

I-BET762 ( GSK525762A;GSK-525762A;I-BET-762;Molibresib )

Catalog No. M11080 CAS No. 1260907-17-2

I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    I-BET762
  • Note
    Research use only, not for human use.
  • Brief Description
    I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins.
  • Description
    I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins BRD2, BRD3 and BRD4 with IC50 of 32.5-42.5 nM, does not interact with other bromodomain-containing proteins (BAZ2B, ATAD2, CREBBP and PCAF); inhibits binding of BET proteins to acetylated histones, disrupts chromatin complexes responsible for the expression of key inflammatory genes in activated macrophages, suppresses TNF-inducible key proinflammatory cytokine (il1b, il1a) and chemokine genes (ccl5, cxcl10, cxcl2/3) in BMDMs; inhibits the ability of Th1-differentiated 2D2 T cells to induce neuroinflammation in vivo in mouse model of EAE; inhibits myeloma cell proliferation both in vitro and myeloma xenograft models.Blood Cancer Phase 2 Clinical
  • Synonyms
    GSK525762A;GSK-525762A;I-BET-762;Molibresib
  • Pathway
    Chromatin/Epigenetic
  • Target
    Bromodomain
  • Recptor
    BETproteins
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1260907-17-2
  • Formula Weight
    423.90
  • Molecular Formula
    C22H22ClN5O2
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C(NCC)C[C@H]1C2=NN=C(C)N2C3=CC=C(OC)C=C3C(C4=CC=C(Cl)C=C4)=N1
  • Chemical Name
    4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Nicodeme E, et al. Nature. 2010 Dec 23;468(7327):1119-23.
2. Bandukwala HS, et al. Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14532-7.
3. Mirguet O, et al. J Med Chem. 2013 Oct 10;56(19):7501-15.
4. Chaidos A, et al. Blood. 2014 Jan 30;123(5):697-705.
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