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TED-347
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TED-347图片
CAS NO:2378626-29-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
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 TEAD4oYap1 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。
生物活性

TED-347 is a potent, irreversible, covalent and allosteric inhibitor atYAP-TEAD protein-protein interactionwith anEC50of 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 aKiof 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 uPARouPA or Cav2.2 αoβ protein-protein interactions. Non-covalent binding of TED-347 to TEAD4 exhibits little change to the TEAD4oYap1 binding affinity[1].
TED-347 has the maximum rate of inactivation of 0.038 hours, corresponding to a t1/2of 18.2 hours[1].

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

性状

Solid

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM3.1878 mL15.9388 mL31.8776 mL
5 mM0.6376 mL3.1878 mL6.3755 mL
10 mM0.3188 mL1.5939 mL3.1878 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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本网站选购。