MYCMI-6 是一种内源性MYC:MAX蛋白相互作用抑制剂，选择性结合 MYC bHLHZip 域，Kd值为 1.6 μM。它阻断 MYC 驱动的转录，以 MYC 依赖性的方式抑制肿瘤细胞的生长 ，诱导细胞凋亡。

MYCMI-6 is a potent and selective inhibitor of endogenous MYC:MAX protein interactions，reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects.

MYCMI-6 in a cell-based protein interaction screen for small inhibitory molecules.?MYCMI-6 exhibits strong selective inhibition of MYC:MAX interaction in cells and in vitro at single-digit micromolar concentrations, as validated by split Gaussia luciferase, in situ proximity ligation, microscale thermophoresis and surface plasmon resonance (SPR) assays.?Further, MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a KD of 1.6 0.5 μM as demonstrated by SPR.?MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner with IC50 concentrations as low as 0.5 μM, while sparing normal cells.?The response to MYCMI-6 correlates with MYC expression based on data from 60 human tumor cell lines and is abrogated by MYC depletion.?Further, it inhibits MYC:MAX interaction, reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects.

MYCMI-6 ?induces massive apoptosis and reduces tumor cell proliferation, tumor microvasculature density and MYC:MAX interaction in a MYC-dependent xenograft tumor model[1].

681282-09-7

C20H19N7O

373.41

NSC354961

DMSO:2.3 mg/mL (6.16 mM,Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years