HXR9 hydrochloride
Based on 1 Customer Validation
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride 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.
For research use only. We do not sell to patients.
- Purity: 99.48%
- Formula: C119H194ClN53O20S
- Molecular Weight:2754.67
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Storage:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
HXR9 hydrochloride (60μM; 4 hours) blocks the interaction between PBX and HOX[1].
HXR9 hydrochloride (60μM; 2 hours) triggers apoptosis in B16 and primary melanoma cells[1].
HXR9 hydrochloride (60μM; 2 hours) causes specific transcriptional changes[1].
HXR9 hydrochloride (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 hydrochloride (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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Appearance Solid
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Molecular Weight 2754.67
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Formula C119H194ClN53O20S
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Color White to off-white
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Sequence Shortening
WYPWMKKHHRRRRRRRRR
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Solvent & Solubility
H2O : 50 mg/mL (18.15 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (36.30 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.3630 mL | 1.8151 mL | 3.6302 mL | 9.0755 mL |
| 5 mM | 0.0726 mL | 0.3630 mL | 0.7260 mL | 1.8151 mL | |
| 10 mM | 0.0363 mL | 0.1815 mL | 0.3630 mL | 0.9075 mL | |
| 15 mM | 0.0242 mL | 0.1210 mL | 0.2420 mL | 0.6050 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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