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)。
货号:ajcx37708
CAS:N/A
分子式:C119H194ClN53O20S
分子量：2754.67
溶解度:H2O : 50 mg/mL (18.15 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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].

[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.