HXR9 hydrochloride
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 2754.67 |
| Molecular Formula | C119H194ClN53O20S |
| SMILES | - |
Summary
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 [1] [2] [3] .
In Vitro
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 IC
50
of 20μM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis
| Cell Line: | murine B16melanoma cells |
| Concentration: | 60 μM |
| Incubation Time: | 4 hours |
| Result: | Blocked the binding of HOXD9 to PBX. |
Apoptosis Analysis
| Cell Line: | B16 cells |
| Concentration: | 60 μM |
| Incubation Time: | 2 hours |
| Result: | A significant proportion of cells were in late phases of apoptosis. |
RT-PCR
| Cell Line: | B16F10cells |
| Concentration: | 60 μM |
| Incubation Time: | 2 hours |
| Result: | Fos , Jun , Dusp1 , and Atf1 ，were allsignificantly up-regulate. |
In Vivo
HXR9 hydrochloride (10 mg/kg; i.v. via the tail vein; twice weekly) blocks tumor growth
[1]
.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57black/6 mice (bearing B16 cells) |
| Dosage: | 10 mg/kg |
| Administration: | I.v. via the tail vein; twice weekly (~30 days) |
| Result: | Tumors showed a significant degree of growth retardation. |
| Animal Model: | Athymic nude mice (bearing A549 cells) |
| Dosage: | Initial dose of 100 mg/kg (subsequent dosing of 10 mg/kg twice weekly) |
| Administration: | Intraperitoneal; twice weekly for 18 days |
| Result: | The tumours of HXR9-treated mice were considerably smaller than those of the control groups. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
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
H 2 O : 50 mg/mL ( 18.15 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.3630 mL | 1.8151 mL | 3.6302 mL |
| 5 mM | 0.0726 mL | 0.3630 mL | 0.7260 mL |
| 10 mM | 0.0363 mL | 0.1815 mL | 0.3630 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (36.30 mM); Clear solution; Need ultrasonic
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.
- [2] Li Z, et al. PBX3 is an important cofactor of HOXA9 in leukemogenesis. Blood. 2013;121(8):1422-1431.
- [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.