MYCMI-6 (NSC354961) 是一种有效的选择性内源性 MYC:MAX 蛋白相互作用抑制剂。 MYCMI-6 阻断 MYC 驱动的转录。MYCMI-6 选择性结合 MYC bHLHZip 域，K_d 值为 1.6 μM。MYCMI-6 以 MYC 依赖性的方式抑制肿瘤细胞的生长 (IC₅₀<0.5 μM)。MYCMI-6 对正常人细胞无细胞毒性。MYCMI-6 诱导细胞凋亡 (apoptosis)。

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 (IC 50 <0.5?μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis.

Solid

MYCMI-6 (NSC354961) (6.25?μM; 48 hours) selectively suppresses MYC-driven tumor cell growth with high efficacy.
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.

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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Powder -20°C 3 years；4°C 2 years

[1]. Castell A, et al. A selective high affinity MYC-binding compound inhibits MYC:MAX interaction and MYC-dependent tumor cell proliferation. Sci Rep. 2018 Jul 3;8(1):10064.

In Vitro: DMSO : 2.4 mg/mL (6.43 mM; Need ultrasonic)配制储备液