hox-1

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

HXR9 is a cell-permeable peptide that acts as a competitive antagonist of the HOX PBX interaction, effectively inhibiting the binding between HOX proteins and the transcription factor PBX in paralogue groups 1 to 8. HXR9 selectively impairs cell proliferation and induces apoptosis in cells with high expression of the HOXA PBX3 genes (e.g., MLL-rearranged leukemic cells).

HXR9 hydrochloride, a cell-permeable peptide and competitive antagonist of the HOX/PBX interaction, selectively reduces cell proliferation and induces apoptosis in cells with elevated HOXA/PBX3 gene expression, notably MLL-rearranged leukemic cells [1] [2] [3]. By inhibiting the interaction between HOX proteins and the transcription factor PBX, which associates with HOX proteins in paralogue groups 1 to 8, it disrupts a critical regulatory mechanism in these cells.