TED-347

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

TED-347  纯度: 98.78%

TED-347 是一种有效,不可逆且共价的 YAP-TEAD 蛋白质-蛋白质相互作用变构抑制剂,对 TEAD4•Yap1 蛋白质-蛋白质相互作用的 EC50 为 5.9 μM。TED-347 与 TEAD4 中央口袋内的 Cys-367 特异性共价结合,Ki 为 10.3 μM。TED-347 可以阻断 TEAD 的转录活性,并且具有抗肿瘤活性。

TED-347

TED-347 Chemical Structure

CAS No. : 2378626-29-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1100 In-stock
1 mg ¥1000 In-stock
5 mg ¥1300 In-stock
10 mg ¥2200 In-stock
25 mg ¥4500 In-stock
50 mg ¥7600 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity[1].

IC50 & Target

IC50: 5.9 μM (TEAD4⋅Yap1 protein-protein interaction)[1]

体外研究
(In Vitro)

TED-347 (0.5-100 μM; 48 hours) inhibits GBM43 cancer cell viability[1].
TED-347 (5 μM; 48 hours) inhibits co-immunoprecipitation of Myc-tagged TEAD4 with FLAG-tagged Yap1[1].
TED-347 (10 μM; 48 hours) shows a significant reduction in CTGF transcript levels[1].
TED-347 (0.5-100 μM; 24 hours) reduces reporter activity in cells transfected with a TEAD reporter. TED-347 (0.5-100 μM) also inhibits TEAD4 transcriptional activity in GBM43 cells[1].
TED-347 is selective for TEADs and inhibits TEAD2 with the same efficacy. TED-347 (0.1-100 μM; 24-48 hours) inhibits TEAD4 binding to full-length Yap1 in dose- and time-dependent manner. TED-347 (1-100 μM) shows no inhibition of uPAR•uPA or Cav2.2 α•β protein-protein interactions. Non-covalent binding of TED-347 to TEAD4 exhibits little change to the TEAD4•Yap1 binding affinity[1].
TED-347 has the maximum rate of inactivation of 0.038 hours, corresponding to a t1/2 of 18.2 hours[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.

Cell Viability Assay[1]

Cell Line: GBM43 glioblastoma cell lines
Concentration: 0.5, 1, 10, 100 μM
Incubation Time: 48 hours
Result: Inhibited GBM43 cancer cell viability and inhibited GBM43 cell viability by 30% at 10 μM.

Western Blot Analysis[1]

Cell Line: HEK-293 cells
Concentration: 5 μM
Incubation Time: 48 hours
Result: Showed a significant loss of co-immunoprecipitation of Myc-tagged TEAD4 with FLAG-tagged Yap1.

RT-PCR[1]

Cell Line: HEK-293 cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: Showed a significant reduction in CTGF transcript levels versus control cells and had no inhibition on TEAD mutant transcriptional activity and protein-protein interactions in cell culture.

分子量

313.70

Formula

C15H11ClF3NO

CAS 号

2378626-29-8

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
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (318.78 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1878 mL 15.9388 mL 31.8776 mL
5 mM 0.6376 mL 3.1878 mL 6.3755 mL
10 mM 0.3188 mL 1.5939 mL 3.1878 mL

*

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。

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    90% corn oil

    Solubility: ≥ 6.25 mg/mL (19.92 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (19.92 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 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 2.

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

    Solubility: 2.5 mg/mL (7.97 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.97 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Khuchtumur Bum-Erdene, et al. Small-Molecule Covalent Modification of Conserved Cysteine Leads to Allosteric Inhibition of the TEAD⋅Yap Protein-Protein Interaction. Cell Chem Biol. 2019 Mar 21;26(3):378-389.e13.

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