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 K_i of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity^[1].

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

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 t_1/2^∞ 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.

313.70

C₁₅H₁₁ClF₃NO

2378626-29-8

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL (318.78 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    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

• [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.