OICR 9429
Biological Activity
High affinity WDR5 antagonist (Kd = 93 nM); disrupts WDR5-MLL interaction. Exhibits selectivity for WDR5 over 22 methyltransferases and a panel of kinases, GPCRs, ion channels, and transporters. Reduces viability of acute myeloid leukemia cells in vitro. Also disrupts MLL1-RbBP5 interaction.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the OICR-9429 probe summary on the SGC website.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of OICR 9429 is reviewed on the chemical probes website.
Compound Libraries
OICR 9429 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 555.59 |
Formula | C29H32F3N5O3 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1801787-56-3 |
PubChem ID | 91623360 |
InChI Key | DJOVLOYCGXNVPI-UHFFFAOYSA-N |
Smiles | CN(CC4)CCN4C1=C(NC(C5=CNC(C=C5C(F)(F)F)=O)=O)C=C(C2=CC(CN3CCOCC3)=CC=C2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 27.78 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 555.59. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 1.8 mL | 9 mL | 18 mL |
5 mM | 0.36 mL | 1.8 mL | 3.6 mL |
10 mM | 0.18 mL | 0.9 mL | 1.8 mL |
50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Grebien et al (2015) Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat.Chem.Biol. 11 571 PMID: 26167872
Getlik et al (2016) Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1). J.Med.Chem. 59 2478 PMID: 26958703
If you know of a relevant reference for OICR 9429, please let us know.
View Related Products by Target
Keywords: OICR 9429, supplier, OICR9429, High, affinity, selective, WDR5, antagonists, WD, repeat-containing, proteins, 5, antagonism, sgc, Lysine, Methyltransferases, WDR5, WDR5, Tocris Bioscience
Citations for OICR 9429
Citations are publications that use Tocris products.
Currently there are no citations for OICR 9429. Do you know of a great paper that uses OICR 9429 from Tocris? If so please let us know.
Reviews for OICR 9429
There are currently no reviews for this product. Be the first to review OICR 9429 and earn rewards!
Have you used OICR 9429?
Submit a review and receive an Amazon gift card.
$10US/$10CAN/€7/£6 gift card for a review without an image
$25US/$25CAN/€18/£15 gift card for a review with an image
*Offer only valid in the USA / Canada, UK and Europe
Submit a ReviewLiterature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
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.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- Bromodomains
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, 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.