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CAS No.: 681282-09-7

MYCMI-6 Catalog No. CSN27224

Synonyms: NSC354961;BXI-61

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 Kd 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 .

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生物活性

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技术信息

生物活性

描述The MYC family of oncogenes, which encodes basic helix-loop-helix leucine zipper (bHLHZip) transcription factors, is considered as one of the most important drivers of tumor development and has been highlighted as a key therapeutic target for cancer therapy for a number of tumor types. MYCMI-6 is a potent and selective inhibitor of MYC:MAX interaction with an IC₅₀ less than 1.5 μM and binds to the MYC bHLHZip domain with a K_D of 1.6 ± 0.5 μM. MYCMI-6 significantly reduced growth of the MYCN-amplified cell lines and the MYCN-non-amplified cell lines with average growth inhibition of 50% (GI₅₀) values of 2.5-6 μM and 20 μM, respectively. Further, MYCMI-6 efficiently inhibited anchorage-independent growth of MYCN-amplified neuroblastoma cells with a GI₅₀ value less than 0.4 μM. In vivo, MYCMI-6 (20 mg/kg; i.p.; daily for 1-2 weeks) induced massive apoptosis and reduces tumor cell proliferation, tumor microvasculature density and MYC:MAX interaction in a MYC-dependent xenograft tumor model^[2].
作用机制MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain^[2].
参考文献

[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.
[2] 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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6780 mL
- 13.3901 mL
- 26.7801 mL
- 5 mM
- 0.5356 mL
- 2.6780 mL
- 5.3560 mL
- 10 mM
- 0.2678 mL
- 1.3390 mL
- 2.6780 mL

技术信息

CAS号	681282-09-7	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C20H19N7O	运输	蓝冰
分子量	373.41	别名	NSC354961;BXI-61

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MYCMI-6 Catalog No. CSN27224

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