keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HXR9 is a cell-permeable peptide that acts as a competitive antagonist of the HOX/PBX interaction. It effectively inhibits the binding between HOX proteins and the transcription factor PBX, specifically in paralogue groups 1 to 8. HXR9 selectively impairs cell proliferation and induces apoptosis in cells with a high expression of the HOXA/PBX3 genes, for instance, MLL-rearranged leukemic cells.
产品描述 | HXR9 is a cell-permeable peptide that acts as a competitive antagonist of the HOX/PBX interaction. It effectively inhibits the binding between HOX proteins and the transcription factor PBX, specifically in paralogue groups 1 to 8. HXR9 selectively impairs cell proliferation and induces apoptosis in cells with a high expression of the HOXA/PBX3 genes, for instance, MLL-rearranged leukemic cells. |
体外活性 | 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 IC 50 of 20μM[1]. 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. |
体内活性 |
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]. 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 | 2718.26 |
分子式 | C119H193N53O20S |
CAS No. | 917953-08-3 |
keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
HXR9 917953-08-3 HXR-9 HXR 9 Inhibitor inhibitor inhibit