10074-A4 is a c-Myc inhibitor. 10074-A4 could bind to c-Myc_370-409 at different sites along the peptide chain. 10074-A4 has anticancer effects^[1][2].

10074-A4 shows inhibitory activity of HL-60 cells with an IC₅₀ of 15.1 μM^[1].
10074-A4 (25-50 μM; 24 hours) arrests the cell cycle at the S-phase in a dose-dependent manner in HL-60 cells. 10074-A4 inhibits the mRNA level of the c-Myc target genes, CCND2 and CDK4^[1].
10074-A4 could bind to c-Myc_370-409 at different sites along the peptide chain and its binding behavior could be described as a ‘ligand cloud’. Even in the bound state, the structure of the c-Myc_370-409 peptide remained a dynamic ensemble. The 10074-A4 ligand bound at different sites throughout the c-Myc_370-409 chain with different strength^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

409.29

C₁₈H₁₄Cl₂N₂O₃S

312631-87-1

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

In Vitro: 

DMSO : 125 mg/mL (305.41 mM; Need ultrasonic)

*

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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.08 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Chen Yu, et al. Structure-based Inhibitor Design for the Intrinsically Disordered Protein c-Myc. Sci Rep. 2016 Mar 2;6:22298.

  [2]. Fan Jin, et al. Ligand clouds around protein clouds: a scenario of ligand binding with intrinsically disordered proteins. PLoS Comput Biol. 2013;9(10):e1003249.