HXR9

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

HXR9 

HXR9 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 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 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

HXR9 Chemical Structure

CAS No. : 917953-08-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

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].

体外研究
(In Vitro)

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].

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 (10 mg/kg; i.v. via the tail vein; twice weekly) blocks tumor growth[1].
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].

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

2718.21

Formula

C119H193N53O20S
CAS 号

917953-08-3
Sequence

Trp-Tyr-Pro-Trp-Met-Lys-Lys-His-His-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg
Sequence Shortening

WYPWMKKHHRRRRRRRRR
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务