For research use only. Not for therapeutic Use.
WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (Kdis=7 μM, Kd=4 μM). WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 methyltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5[1][2].
| Catalog Number | I041765 |
| CAS Number | 824960-50-1 |
| Synonyms | 2-chloro-N-[2-(4-methylpiperazin-1-yl)-5-nitrophenyl]benzamide |
| Molecular Formula | C18H19ClN4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C18H19ClN4O3/c1-21-8-10-22(11-9-21)17-7-6-13(23(25)26)12-16(17)20-18(24)14-4-2-3-5-15(14)19/h2-7,12H,8-11H2,1H3,(H,20,24) |
| InChIKey | WOGZFCMBPXJNFI-UHFFFAOYSA-N |
| SMILES | CN1CCN(CC1)C2=C(C=C(C=C2)[N+](=O)[O-])NC(=O)C3=CC=CC=C3Cl |
| Reference | [1]. Ye X, et al. The identification of novel small-molecule inhibitors targeting WDR5-MLL1 interaction through fluorescence polarization based high-throughput screening. Bioorg Med Chem Lett. 2019 Feb 15;29(4):638-645. [2]. Chen X, et al. Targeting WD Repeat-Containing Protein 5 (WDR5): A Medicinal Chemistry Perspective. J Med Chem. 2021 Aug 12;64(15):10537-10556. |
