WDR5-IN-4

WDR5-IN-4 (Compound C6) is a WIN site inhibitor of chromatin-associated WD repeat domain 5 protein (WDR5), Kd The value is 0.1 nM. WDR5-IN-4 is able to displace WDR5 from chromatin and reduce the expression of related genes, causing translation inhibition and nucleolar stress. Has anti-cancer effects [1][1].

Product Specifications

CAS Number

[2407457-36-5]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Apoptosis; WDR5

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/WIN_site_inhibitor_1.html

Purity

98.13

Solubility

10 mM in DMSO

Smiles

ClC1=CC=C(CNC(C2=CC(CN3C(N(C)C=C3)=N)=CC(C4=C(C)N=C(F)C=C4)=C2)=O)C=C1Cl

Molecular Formula

C25H22Cl2FN5O

Molecular Weight

498.38

Precautions

H315, H319, H335

References & Citations

[1]Aho ER, et al. Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep. 2019 Mar 12;26 (11) :2916-2928.e13.|[2]Wang H, et al. The E3 ubiquitin ligase RNF220 maintains hindbrain Hox expression patterns through regulation of WDR5 stability[J]. Elife, 2024, 13: RP94657.