INH1 specifically disrupts the Hec1/Nek2 interaction via direct Hec1 binding. INH1 shows promising cancer inhibition activity both in vitro and in vivo^[1].

INH1 (25 μM, 24 h) treatment resulted in reduced association of Hec1 with kinetochore and decrease of global Nek2 protein level^[1].
INH1 exhibits GI₅₀ values of 10.5 μM (in MDA-MB-468 cells), 15 μM (in SKBR3 cells), 10.5 μM (in T47D cells), 20.5 μM (in MDA-MB-361 cells), 15 μM (in ZR-75-1 cells), 15 μM (in HBL 100 cells), 15.5 μM (in MDA-MB-435 cells), 11 μM (in HS578T cells) and 41 μM (in MCF10A cells), respectively^[1].
INH1 (5k) has an IC₅₀ value of 176 nM in the dose-dependent transwell migration assays in MDA-MB-231 cells. INH1 (5k) substantially reduces cellular f-actin and prevented localization of fascin to actin-rich membrane protrusions^[2].
INH1 induces abnormal mitotic processes, as well as cell apoptosis^[3].

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.

INH1 (50 or 100 mg/kg, i.p., every other day/25 cycles) inhibits tumor outgrowth in a xenografted breast cancer model in nude mice^[1].

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.

308.40

C₁₈H₁₆N₂OS

313553-47-8

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL (324.25 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。-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。

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: ≥ 2.5 mg/mL (8.11 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.11 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (8.11 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.11 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Wu G, et al. Small molecule targeting the Hec1/Nek2 mitotic pathway suppresses tumor cell growth in culture and in animal. Cancer Res. 2008 Oct 15;68(20):8393-9.

  [2]. Shilong Zheng, et al. Discovery of a Series of Thiazole Derivatives as Novel Inhibitors of Metastatic Cancer Cell Migration and Invasion. ACS Med Chem Lett. 2013 Feb 14; 4(2): 191–196.

  [3]. Yongxia Zhu, et al. Small Molecule TH-39 Potentially Targets Hec1/Nek2 Interaction and Exhibits Antitumor Efficacy in K562 Cells via G0/G1 Cell Cycle Arrest and Apoptosis Induction. Cell Physiol Biochem. 2016;40(1-2):297-308.