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Submit ReviewWDR5 0103 is a WD repeat-containing protein 5 (WDR5) antagonist (Kd = 450 nM). Disrupts WDR5 interaction with MLL and inhibits MLL core complex methyltransferase activity in vitro. Has no effect on a panel of seven other methyltransferases, including SETD7.
WDR5 0103 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
M. Wt | 383.44 |
Formula | C21H25N3O4 |
Storage | Store at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 890190-22-4 |
PubChem ID | 6457069 |
InChI Key | ZPLBXOVTSNRBFB-UHFFFAOYSA-N |
Smiles | O=C(OC)C1=CC(NC(C3=CC=CC(OC)=C3)=O)=C(N2CCN(C)CC2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 38.34 | 100 | |
ethanol | 19.17 | 50 |
The following data is based on the product molecular weight 383.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.61 mL | 13.04 mL | 26.08 mL |
5 mM | 0.52 mL | 2.61 mL | 5.22 mL |
10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
References are publications that support the biological activity of the product.
Senisterra et al (2013) Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem.J. 449 151 PMID: 22989411
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Keywords: WDR5 0103, WDR5 0103 supplier, WDR50103, WDR5, antagonists, MLL, methyltransferases, epigenetics, WD, repeat-containing, WD40, Lysine, Methyltransferases, 5323, Tocris Bioscience
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Reaction mixtures with various concentrations of WDR5-0103 (1 μM–1 mM) were incubated for 1 h at room temperature and then quenched by adding 20 μL of 7.5 M guanidinium chloride.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.