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，Kd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)。
| 生物活性 | MYCMI-6 (NSC354961) is a potent and selective endogenousMYC:MAXprotein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with aKdof 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 inducesapoptosis[1]. |
体外研究
(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 ofMYCto one of the immunoglobulin loci - in a dose-dependent manner with an average GI50of 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 IC50for 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 IC50of 3.8 μM. MYCMI-6 efficiently inhibits anchorage-independent growth ofMYCN-amplified neuroblastoma cells with GI50values of<0.4 μM[1].
Cell Viability Assay[1] | Cell Line: | MYCN-amplified neuroblastoma cells (IMR-32, Kelly and SK-N-DZ),MYCN-non-amplified neuroblastoma cells (SK-N-F1, SK-N-AS and SK-N-RA) | | Concentration: | 6.25 μM | | Incubation Time: | 48 hours | | Result: | Reduced growth of theMYCN-amplified cell lines significantly stronger than theMYCN-non-amplified cell lines. |
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体内研究
(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].
| Animal Model: | 6-8 weeks old athymic nude mice (bearing MYCN-amplified SK-N-DZ neuroblastoma cells)[1] | | Dosage: | 20 mg/kg body weight | | Administration: | I.p.; daily for 1-2 weeks | | Result: | A dramatic increase in the extension of apoptotic areas in the tumors and a significant increase in non-proliferative areas as determined by Ki67 staining in tumors. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 2.4 mg/mL(6.43 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6780 mL | 13.3901 mL | 26.7802 mL | | 5 mM | 0.5356 mL | 2.6780 mL | 5.3560 mL | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
