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WDR5-0103

Item № 13945
CAS № 890190-22-4
Purity ≥95%
product image
                (CAS 890190-22-4)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $49.00 0.00
     5 mg $221.00 0.00
     10 mg $392.00 0.00
     25 mg $858.00 0.00

Pricing updated 2019-07-17. Prices are subject to change without notice.

Description
Synonyms
  • WD-Repeat Protein 5-0103

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.3,1 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

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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
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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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, 933-937 (2007).

3. Guelman, S., Kozuka, K., Mao, Y., et al. The double-histone-acetyltransferase complex ATAC is essential for mammalian development Molecular and Cellular Biology 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 Biochemistry Journal 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 Current Opinion in Chemical Biology 17(3), 369-378 (2013).

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