917953-08-3
Chemical Structure
HXR9
- CAS No.: 917953-08-3
- Formula:C119H193N53O20S
- Molecular Weight:2718.21
SMILES: O=C([C@H]1N(CCC1)C([C@@H](NC([C@@H](N)CC2=CNC3=CC=CC=C23)=O)CC4=CC=C(C=C4)O)=O)N[C@H](C(N[C@@H](CCSC)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@H](C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(O)=O)CCCNC(N)=N)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC5=CN=CN5)=O)CC6=CN=CN6)=O)=O)=O)=O)CC7=CNC8=CC=CC=C78
Biological Activity: HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells[1][2][3].
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HXR9 | HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells. | |||||||||||||||||||||
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References
- [1]. Morgan R, et al. Antagonism of HOX/PBX dimer formation blocks the in vivo proliferation of melanoma. Cancer Res. 2007;67(12):5806-5813. [Content Brief]
- [2]. Li Z, et al. PBX3 is an important cofactor of HOXA9 in leukemogenesis. Blood. 2013;121(8):1422-1431. [Content Brief]
- [3]. Plowright L, et al. HOX transcription factors are potential therapeutic targets in non-small-cell lung cancer (targeting HOX genes in lung cancer). Br J Cancer. 2009;100(3):470-475. [Content Brief]
