HXR9 hydrochloride |
| Catalog No.GC64485 |
HXR9 염산염은 세포 투과성 펩타이드이며 HOX/PBX 상호작용의 경쟁적 길항제입니다. HXR9 염산염은 HOX와 두 번째 전사 인자(PBX) 사이의 상호 작용을 길항하며, 이는 파라로그 그룹 1~8의 HOX 단백질에 결합합니다. HXR9 염산염은 HOXA/ MLL 재배열 백혈병 세포와 같은 PBX3 유전자.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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.
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