A CBP and p300 inhibitor
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GNE-781

Item No. 36450

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1,4,6,7-tetrahydro-N-methyl-1-(tetrahydro-2H-pyran-4-yl)-5H-pyrazolo[4,3-c ]pyridine-5-carboxamide
CAS Number
1936422-33-1
Molecular Formula
C27H33F2N7O2
Formula Weight
525.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
O=C(N1CC2=C(CC1)N(C3CCOCC3)N=C2N4C5=C(CCC4)C=C(C6=CN(C)N=C6)C(C(F)F)=C5)NC
InChi Code
InChI=1S/C27H33F2N7O2/c1-30-27(37)34-9-5-23-22(16-34)26(32-36(23)19-6-10-38-11-7-19)35-8-3-4-17-12-20(18-14-31-33(2)15-18)21(25(28)29)13-24(17)35/h12-15,19,25H,3-11,16H2,1-2H3,(H,30,37)
InChi Key
CQCWHSDMJBAGDC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $406

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    10 mg

    $731

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    25 mg

    $1,319

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    50 mg

    $2,436

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    Product Description

    GNE-781 is an inhibitor of CREB-binding protein (CBP) and histone acetyltransferase p300 (IC50s = 0.94 and 1.2 nM, respectively).1 It is selective for CBP and p300 over bromodomain-containing protein 4 (BRD4) bromodomain 1, BRD4 bromodomain 2, and bromodomain and PHD finger-containing 1 (BRPF1; IC50s = 5.1, 12, and 4.6 µM, respectively), as well as nine other bromodomain-containing proteins (IC50s = >18 µM for all). GNE-781 inhibits the expression of Myc in MV4-11 leukemia cells (EC50 = 6.6 nM). It reduces the differentiation of isolated human naïve CD4+ T cells into FOXP3+ inducible regulatory T cells (Tregs) in a concentration-dependent manner without affecting cell viability. Oral administration of GNE-781 (3-30 mg/kg) decreases tumor volume in a MOLM-16 acute myeloid leukemia (AML) mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Romero, F.A., Murray, J., Lai, K.W., et al. GNE-781, a highly advanced potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein, binding protein (CBP). J. Med. Chem. 60(22), 9162-9183 (2017).