MYCMI-6

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Chemical Structure| 681282-09-7 同义名 : NSC354961
CAS号 : 681282-09-7
货号 : A1329217
分子式 : C20H19N7O
纯度 : 98%
分子量 : 373.41
MDL号 : MFCD32701920
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(5.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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 KD 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.68mL

0.54mL

0.27mL

13.39mL

2.68mL

1.34mL

26.78mL

5.36mL

2.68mL
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