824960-50-1
Chemical Structure
WDR5-0102
- CAS No.: 824960-50-1
- Formula:C18H19ClN4O3
- Molecular Weight:374.82
IUPAC Name: (S)-1-(4,4-dimethylcyclohexyl)ethan-1-amine hydrochloride
InChIKey: WOGZFCMBPXJNFI-UHFFFAOYSA-N
SMILES: O=C(C1=C(Cl)C=CC=C1)NC2=CC([N+]([O-])=O)=CC=C2N3CCN(CC3)C
Biological Activity: WDR5-0102 is an inhibitor of WDR5. WDR5-0102 specifically targets the WIN site of WDR5, disrupts the WDR5-MLL1 interaction, and reduces the histone methyltransferase activity of MLL1. WDR5-0102 exerts dose-dependent toxicity on MDSC-like cells and reduces their osteopontin levels, while showing extremely low cytotoxicity to pancreatic cancer cells. WDR5-0102 can be used in the research of related diseases such as acute myeloid leukemia, lymphoid leukemia, biphenotypic leukemia and pancreatic cancer[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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WDR5-0102 | 97.07% | WDR5-0102 is an inhibitor of WDR5. WDR5-0102 specifically targets the WIN site of WDR5, disrupts the WDR5-MLL1 interaction, and reduces the histone methyltransferase activity of MLL1. WDR5-0102 exerts dose-dependent toxicity on MDSC-like cells and reduces their osteopontin levels, while showing extremely low cytotoxicity to pancreatic cancer cells. WDR5-0102 can be used in the research of related diseases such as acute myeloid leukemia, lymphoid leukemia, biphenotypic leukemia and pancreatic cancer. | ||||||||||||||||||||
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- [1]. Chen X, Xu J, Wang X, et al. Targeting WD repeat-containing protein 5 (WDR5): a medicinal chemistry perspective[J]. Journal of medicinal chemistry, 2021, 64(15): 10537-10556.
- [2]. Lu C, et al. WDR5-H3K4me3 epigenetic axis regulates OPN expression to compensate PD-L1 function to promote pancreatic cancer immune escape. J Immunother Cancer. 2021;9(7):e002624. [Content Brief]
- [3]. 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;29(4):638-645. [Content Brief]
Keywords
