WDR5-C47 --- WDR5-MLL (SET1) Antagonist

Catalog No. size PriceQuantity
M60118-2S 2mg solid $129
M60118-10S 10mg solid $529


WDR5-C47 is a highly potent and selective antagonist of WDR5-MLL interaction with an IC50 ~0.3 µM. WDR5-C47 was designed based on the structure of the WDR5-MLL complex. The WD40-repeat protein WDR5 plays a critical role in maintaining the integrity of the MLL complex and fully activating its methyltransferase function. The MLL complex, the trithorax-like family of SET1 methyltransferase, catalyzes trimethylation of lysine 4 on histone 3, and they have been widely implicated in various cancers. WDR5-C47 could serve as a tool compound to study functions of SET1-family of human histone methyltransferases and further develop therapeutic drug molecules targeting the WDR5−MLL interaction.

Product information

CAS Number: 1422389-91-0

Molecular Weight: 406.84

Formula: C19H20ClFN4O3

Chemical Name: 2-chloro-4-fluoro-3-methyl-N-(2-(4-methylpiperazin-1-yl)-5-nitrophenyl)benzamide

Smiles: CN1CCN(CC1)C1=CC=C(C=C1NC(=O)C1=CC=C(F)C(C)=C1Cl)[N+]([O-])=O


InChi: InChI=1S/C19H20ClFN4O3/c1-12-15(21)5-4-14(18(12)20)19(26)22-16-11-13(25(27)28)3-6-17(16)24-9-7-23(2)8-10-24/h3-6,11H,7-10H2,1-2H3,(H,22,26)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

WDR5-C47 was suggested to be used at 10 µM final concentration in vitro and in cellular assays.


  1. Bolshan Y, et al. Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction. (2013) ACS Med. Chem. Lett., 4 (3), 353–357.

Products are for research use only. Not for human use.


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