I-BRD9

CAS No. 1714146-59-4

I-BRD9( I-BRD9 | I-BRD-9 | I-BRD 9 )

Catalog No. M12612 CAS No. 1714146-59-4

The first selective cellular chemical probe for BRD9 with pIC50 of 7.3.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    I-BRD9
  • Note
    Research use only, not for human use.
  • Brief Description
    The first selective cellular chemical probe for BRD9 with pIC50 of 7.3.
  • Description
    The first selective cellular chemical probe for BRD9 with pIC50 of 7.3; displays 700-fold selectivity over the BET family and 200-fold over the highly homologous BRD7; decreases cell proliferation, G1-arrest and apoptosis in rhabdoid tumor cells; shows synergistic inhibitory effects on cell proliferation combined with doxorubicin or carboplatin.
  • In Vitro
    I-BRD9 (10 μM, 6 h) has a regulation role in cancer and immunology pathways.I-BRD9 (10 μM) has high BRD9 affinity and excellent broader bromodomain selectivity.I-BRD9 (10 μM) has affinity for BRD9 (TR-FRET), BRD4 BD1 (TR-FRET) and BRD9 NanoBRET with pIC50 values of 7.3 μM, 5.3 μM and 6.8 μM.I-BRD9 (10 μM) has high aqueous solubility (CLND) with 359 μM.I-BRD9 (10 μM) displays >625 fold selectivity in binding with endogenous BRD9 against BET family member BRD3 in HUT-78 cell lysate. RT-PCR Cell Line:Kasumi-1 cells Concentration:10 μM Incubation Time:6 h Result:Showed 4 genes (CLEC1, 62 DUSP6, 63 FES64 and SAMSN165) that were strongly down-regulated and not by I-BET151.
  • In Vivo
    ——
  • Synonyms
    I-BRD9 | I-BRD-9 | I-BRD 9
  • Pathway
    Chromatin/Epigenetic
  • Target
    Bromodomain
  • Recptor
    BRD4|BRD9
  • Research Area
    Other Indications
  • Indication
    ——

Chemical Information

  • CAS Number
    1714146-59-4
  • Formula Weight
    497.5536
  • Molecular Formula
    C22H22F3N3O3S2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 15.5 mg/mL
  • SMILES
    N=C(C(S1)=CC2=C1C(C3=CC=CC(C(F)(F)F)=C3)=CN(CC)C2=O)NC(CC4)CCS4(=O)=O
  • Chemical Name
    Thieno[3,2-c]pyridine-2-carboximidamide, 5-ethyl-4,5-dihydro-4-oxo-N-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-7-[3-(trifluoromethyl)phenyl]-

Shipping & Storage Information

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

Reference

1. Theodoulou NH, et al. J Med Chem. 2016 Feb 25;59(4):1425-39. 2. Kr?mer KF, et al. Int J Mol Sci. 2017 Jul 16;18(7). pii: E1537.
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