WDR5-IN-4 TFA

• CAT Number: I045970
• CAS Number: 2749300-35-2
• Molecular Formula: C27H23Cl2F4N5O3
• Molecular Weight: 612.40
• Purity: ≥95%
• Synonyms: N-[(3,4-dichlorophenyl)methyl]-3-(6-fluoro-2-methylpyridin-3-yl)-5-[(2-imino-3-methylimidazol-1-yl)methyl]benzamide;2,2,2-trifluoroacetic acid
• InChI: InChI=1S/C25H22Cl2FN5O.C2HF3O2/c1-15-20(4-6-23(28)31-15)18-9-17(14-33-8-7-32(2)25(33)29)10-19(12-18)24(34)30-13-16-3-5-21(26)22(27)11-16;3-2(4,5)1(6)7/h3-12,29H,13-14H2,1-2H3,(H,30,34);(H,6,7)
• InChIKey: SRNPJMNSZVVBDZ-UHFFFAOYSA-N
• SMILES: CC1=C(C=CC(=N1)F)C2=CC(=CC(=C2)CN3C=CN(C3=N)C)C(=O)NCC4=CC(=C(C=C4)Cl)Cl.C(=O)(C(F)(F)F)O

WDR5-IN-4 TFA 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].

Reference

[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.
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