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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- CAS No.: 917953-08-3
- Formule: C119H193N53O20S
- Masse moléculaire:2718.21
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
HXR9 (60μM; 4 hours) blocks the interaction between PBX and HOX[1].
HXR9 (60μM; 2 hours) triggers apoptosis in B16 and primary melanoma cells[1].
HXR9 (60μM; 2 hours) causes specific transcriptional changes[1].
HXR9 (B16 cells) shows antiproliferative activity with an IC50 of 20μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine B16melanoma cells
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Concentration:60 μM
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Incubation Time:4 hours
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Result:Blocked the binding of HOXD9 to PBX.
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Cell Line:B16 cells
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Concentration:60 μM
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Incubation Time:2 hours
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Result:A significant proportion of cells were in late phases of apoptosis.
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Cell Line:B16F10cells
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Concentration:60 μM
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Incubation Time:2 hours
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Result:Fos, Jun, Dusp1, and Atf1，were allsignificantly up-regulate.
HXR9 (Initial dose of 100 mg/kg (subsequent dosing of 10 mg/kg twice weekly); Intraperitoneal; twice weekly for 18 days) blocks A549 tumour growth in vivo[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57black/6 mice (bearing B16 cells)
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Dosage:10 mg/kg
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Administration:I.v. via the tail vein; twice weekly (~30 days)
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Result:Tumors showed a significant degree of growth retardation.
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Animal Model:Athymic nude mice (bearing A549 cells)
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Dosage:Initial dose of 100 mg/kg (subsequent dosing of 10 mg/kg twice weekly)
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Administration:Intraperitoneal; twice weekly for 18 days
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Result:The tumours of HXR9-treated mice were considerably smaller than those of the control groups.
Chemical Information
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CAS No. 917953-08-3
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Masse moléculaire 2718.21
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Formule C119H193N53O20S
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Sequence
Trp-Tyr-Pro-Trp-Met-Lys-Lys-His-His-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg
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Sequence Shortening
WYPWMKKHHRRRRRRRRR
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HXR9 Related Classifications
HY-P3245 Related Classifications
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