WDR5-IN-4 (TFA)

WDR5-IN-4 TFA (Compound C6) is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity[1].

Product Specifications

CAS Number

[2749300-35-2]

UNSPSC

12352005

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-tfa.html

Purity

98.04

Solubility

DMSO : 100 mg/mL (ultrasonic)

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.O=C(O)C(F)(F)F

Molecular Formula

C27H23Cl2F4N5O3

Molecular Weight

612.40

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]Pan M, et al., UTP18-mediated p21 mRNA instability drives adenoma-carcinoma progression in colorectal cancer. Cell Rep. 2023 May 30;42 (5) :112423.|[3]Wang H, et al. The E3 ubiquitin ligase RNF220 maintains hindbrain Hox expression patterns through regulation of WDR5 stability[J]. Elife, 2024, 13: RP94657.