An inhibitor of WDR5 peptide binding
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WDR5-0103

Item No. 13945

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(3-methoxybenzoyl)amino]-4-(4-methyl-1-piperazinyl)-benzoic acid, methyl ester
CAS Number
890190-22-4
Synonyms
  • WD-Repeat Protein 5-0103
Molecular Formula
C21H25N3O4
Formula Weight
383.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33.3 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 16.6 mg/mlEthanol: 12.5 mg/ml
λmax
212, 264 nm
SMILES
O=C(OC)C1=CC(NC(C2=CC=CC(OC)=C2)=O)=C(N3CCN(C)CC3)C=C1
InChi Code
InChI=1S/C21H25N3O4/c1-23-9-11-24(12-10-23)19-8-7-16(21(26)28-3)14-18(19)22-20(25)15-5-4-6-17(13-15)27-2/h4-8,13-14H,9-12H2,1-3H3,(H,22,25)
InChi Key
ZPLBXOVTSNRBFB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $90

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    10 mg

    $165

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    25 mg

    $345

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    Product Description

    WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.1 For example, WDR5 is a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3.2 WDR5 can also be a component of histone acetyltransferase complexes and can directly bind methylated as well as unmodified histones.1,3 WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM).4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Migliori, V., Mapelli, M., and Guccione, E. On WD40 proteins: Propelling our knowledge of transcriptional control? Epigenetics 7(8), 815-822 (2012).

    2. Guccione, E., Bassi, C., Casadio, F., et al. Methylation of histone H3R2 by PRMT6 and H3K4 by an MLL complex are mutually exclusive. Nature 449(7164), 933-937 (2007).

    3. Guelman, S., Kozuka, K., Mao, Y., et al. The double-histone-acetyltransferase complex ATAC is essential for mammalian development. Mol. Cell. Biol. 29(5), 1176-1188 (2009).

    4. Senisterra, G., Wu, H., Allali-Hassani, A., et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem. J. 449(1), 151-159 (2013).

    5. Wigle, T.J., and Copeland, R.A. Drugging the human methylome: An emerging modality for reversible control of aberrant gene transcription. Curr. Opin. Chem. Biol. 17(3), 369-378 (2013).