OICR 9429

Cat. No. 5267 COA / Product Datasheet SDS

Pricing	Availability	Delivery Time	Qty

Bulk Orders

Cat.No. 5267 - OICR 9429 | C29H32F3N5O3 | CAS No. 1801787-56-3

Description: High affinity and selective WDR5 antagonist

Chemical Name: N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide

Purity: ≥98% (HPLC)

Datasheet

Citations

Reviews

Literature

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

High affinity WDR5 antagonist (K_d = 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
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

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

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 Review

Literature 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.

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

Cancer Metabolism
Epigenetics in Cancer
Receptor Signaling
Cell Cycle and DNA Damage Repair
Angiogenesis
Invasion and Metastasis

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.