A chemical probe for BRPF1
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PFI-4

Item No. 17663

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,3-dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxy benzamide
CAS Number
900305-37-5
Molecular Formula
C21H24N4O3
Formula Weight
380.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/ml
λmax
240, 325 nm
SMILES
O=C1N(C)C2=CC(N3CCCC3)=C(NC(C4=C(OC)C=CC=C4)=O)C=C2N1C
InChi Code
InChI=1S/C21H24N4O3/c1-23-17-12-15(22-20(26)14-8-4-5-9-19(14)28-3)16(25-10-6-7-11-25)13-18(17)24(2)21(23)27/h4-5,8-9,12-13H,6-7,10-11H2,1-3H3,(H,22,26)
InChi Key
QCIJLRJBZDBVDB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $154

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    10 mg

    $259

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    50 mg

    $1,053

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    Product Description

    PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21).1 It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 µM) and is selective for BRPF1 over BRPF2 and BRPF3.1 PFI-4 is potent in cells, with an IC50 value of 250 nM. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Demont, E.H., Bamborough, P., Chung, C.W., et al. 1,3-Dimethyl benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain. ACS Med. Chem. Lett. 5, 1190-1195 (2014).