A BET bromodomain inhibitor
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PFI-1

Item No. 11155

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide
CAS Number
1403764-72-6
Synonyms
  • PF-06405761
Molecular Formula
C16H17N3O4S
Formula Weight
347.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12 mg/mlDMSO: 12 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
λmax
262 nm
SMILES
O=S(C1=C(OC)C=CC=C1)(NC2=CC=C(NC(N(C)C3)=O)C3=C2)=O
InChi Code
InChI=1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20)
InChi Key
TXZPMHLMPKIUGK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

    $115

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    10 mg

    $183

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    25 mg

    $402

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    Product Description

    Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease.1,2,3 PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. In an AlphaScreen assay it has been shown to inhibit BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 μM, respectively. 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. Filippakopoulos, P., Qi, J., Picaud, S., et al. Selective inhibition of BET bromodomains. Nature 468(7327), 1067-1073 (2010).

    2. Hewings, D.S., Wang, M., Philpott, M., et al. 3,5-Dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. J. Med. Chem. 54(19), 6761-6770 (2011).

    3. Chung, C.W., Coste, H., White, J.H., et al. Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J. Med. Chem. 54(11), 3827-3838 (2011).