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WDR5-IN-4 (TFA)

CAT: 0804-HY-111753A-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-111753A-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, stored under nitrogen, away from moisture)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Citation 01
BioRxiv. 2023 Dec 16.|bioRxiv. 2023 Jun 5.|Cell Rep. 2023 Apr 21;42 (5) :112423.

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