HXR9 hydrochloride

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HXR9 hydrochloride  纯度: 99.50%

HXR9 hydrochloride 是一种细胞渗透性肽，是 HOX/PBX 相互作用 (HOX/PBX interaction) 的竞争性拮抗剂。HXR9 hydrochloride 拮抗 HOX 与第二转录因子 (PBX) 之间的相互作用，PBX 与旁系同源基因组 1 至 8 中的 HOX 蛋白结合。HXR9 hydrochloride 选择性地减少细胞增殖并促进 HOXA/PBX3 基因高水平表达的细胞，例如 MLL 重排的白血病细胞中的细胞凋亡 (apoptosis)。

HXR9 hydrochloride

HXR9 hydrochloride Chemical Structure

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生物活性

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].

体外研究
(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 IC50 of 20μM[1].

Shanghai Jinpan Biotech Co Ltd 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.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

2754.67

Formula

C119H194ClN53O20S
Sequence Shortening

WYPWMKKHHRRRRRRRRR
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light, stored under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献

  • [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.

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