WDR5 Inhibitors
WD repeat domain 5 (WDR5) is a core component of the SET1 family of histone methyltransferases, specifically involved in the catalysis of histone H3 lysine 4 (H3K4) methylation, a key epigenetic mark associated with gene activation. WDR5 plays a critical role in various biological processes, including cell cycle regulation, development, and differentiation, by facilitating the assembly of the methyltransferase complex and mediating its interaction with histone substrates. Its interaction with other proteins is not limited to histone modifiers; WDR5 is also involved in the regulation of non-histone protein functions, thereby influencing numerous cellular pathways. The multifaceted roles of WDR5 underscore its importance in maintaining genomic stability and regulating gene expression, positioning it as a central player in epigenetic modulation and cellular function. The precise regulation of H3K4 methylation by WDR5 is crucial for the transcriptional activation of genes necessary for cellular growth and response to environmental stimuli, highlighting its significance in both normal physiology and disease states.
The inhibition of WDR5 involves disrupting its interaction with the SET1 family of methyltransferases or blocking its binding to histone or non-histone proteins. This can be achieved through small molecules or peptides that specifically target the WDR5 interaction domain, disrupting the formation of functional methyltransferase complexes and thereby reducing H3K4 methylation levels. Such inhibition directly impacts gene expression, leading to alterations in cellular pathways regulated by WDR5-mediated methylation. Inhibition strategies focus on the precise mechanisms by which WDR5 contributes to the assembly and function of methyltransferase complexes, aiming to modulate its activity without disrupting essential cellular functions.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
N2-[4-(Aminomethyl)phenyl]-5-fluoro-N4-phenylpyrimidine-2,4-diamine | 916603-07-1 | sc-212341 | 2.5 mg | $250.00 | ||
Also called CZC-8004, this compound is a small molecule inhibitor that directly targets WDR5, impeding its interaction with MLL complexes. By disrupting the WDR5-MLL interaction, CZC-8004 interferes with the assembly of active histone methyltransferase complexes, leading to altered histone methylation patterns and gene expression. | ||||||
PF-3758309 | 898044-15-0 | sc-478493 | 10 mg | $260.00 | ||
PF-3758309 is a small molecule inhibitor that indirectly modulates WDR5 expression by targeting the PI3K/AKT/mTOR pathway. Inhibition of this pathway affects downstream targets, including WDR5. The indirect inhibition of WDR5 by PF-3758309 underscores the crosstalk between the PI3K/AKT/mTOR pathway and WDR5-mediated epigenetic regulation, offering a targeted approach to modulate WDR5 expression within the context of PI3K/AKT/mTOR pathway dysregulation. | ||||||
XAV939 | 284028-89-3 | sc-296704 sc-296704A sc-296704B | 1 mg 5 mg 50 mg | $35.00 $115.00 $515.00 | 26 | |
XAV-939 is a small molecule inhibitor that indirectly modulates WDR5 expression by inhibiting the Wnt/β-catenin pathway. Inhibition of this pathway influences downstream targets, including WDR5. The indirect inhibition of WDR5 by XAV-939 underscores the intricate interplay between the Wnt/β-catenin pathway and WDR5-mediated epigenetic regulation, offering a targeted approach to modulate WDR5 expression within the context of Wnt/β-catenin pathway dysregulation. | ||||||
C646 | 328968-36-1 | sc-364452 sc-364452A | 10 mg 50 mg | $260.00 $925.00 | 5 | |
C646 is a small molecule inhibitor that indirectly modulates WDR5 expression by inhibiting the histone acetyltransferase p300. Inhibition of p300 affects downstream targets, including WDR5. The indirect inhibition of WDR5 by C646 underscores the crosstalk between histone acetylation and WDR5-mediated epigenetic regulation, offering a targeted approach to modulate WDR5 expression within the context of p300 inhibition. | ||||||
3-[(3-Methoxybenzoyl)amino]-4-(4-methyl-1-piperazinyl)benzoic acid methyl ester-d3 | 890190-22-4 (unlabeled) | sc-484812 | 1 mg | $380.00 | ||
This compound, also called WDR5-0103, is a small molecule inhibitor that directly targets WDR5, disrupting its interaction with MLL complexes. By inhibiting the WDR5-MLL interaction, WDR5-0103 interferes with the formation of active histone methyltransferase complexes, leading to altered histone methylation patterns and gene expression. | ||||||