MYCMI-6

MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a K_d of 1.6?μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC₅₀<0.5?μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis^[1]. In Vitro: MYCMI-6 (NSC354961) (6.25?μM; 48 hours) selectively suppresses MYC-driven tumor cell growth with high efficacy^[1].
MYCMI-6 significantly inhibits growth of Burkitt’s lymphoma cells (Mutu, Daudi and ST486) - another classical example of a MYC-driven tumor, having translocations of MYC to one of the immunoglobulin loci - in a dose-dependent manner with an average GI₅₀ of 0.5?μM. Treatment of MCF7 cells with the MYCMI-6 for 24?hours significantly decreased MYC:MAX isPLA signals to 7%. Titration showed an IC₅₀ for inhibition of MYC:MAX of less than 1.5?μM for MYCMI-6 by isPLA. MYCMI-6 inhibits the MYC:MAX heterodimer formation with an IC₅₀ of 3.8?μM. MYCMI-6 efficiently inhibits anchorage-independent growth of MYCN-amplified neuroblastoma cells with GI₅₀ values of <0.4?μM^[1]. In Vivo: MYCMI-6 (20?mg/kg; i.p.; daily for 1-2 weeks) induces massive apoptosis and reduces tumor cell proliferation, tumor microvasculature density and MYC:MAX interaction in a MYC-dependent xenograft tumor model^[1].