标签归档：tead

YAP-TEAD-IN-1 TFA

发表于由

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。

YAP-TEAD-IN-1 TFA  纯度: 99.88%

YAP-TEAD-IN-1 TFA 是 YAP-TEAD 相互作用的有效的竞争性肽类抑制剂 (IC50=25 nM)。YAP-TEAD-IN-1 TFA 是一种 17mer 的多肽，与 YAP (50-171) (Kd=40 nM) 相比，其与 TEAD1 的结合亲和力更高 (Kd= 15 nM)。

YAP-TEAD-IN-1 TFA

YAP-TEAD-IN-1 TFA Chemical Structure

CAS No. : 1659305-79-9

规格 价格 是否有货 数量
1 mg ￥1800 In-stock
5 mg ￥4200 In-stock
10 mg ￥7000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

YAP-TEAD-IN-1 TFA 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library
  • Peptide Library

生物活性

YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM)[1].

IC50 & Target

IC50: 25 nM (YAP-TEAD interaction)[1]
体外研究
(In Vitro)

YAP-TEAD-IN-1 (peptide 17)(2 μM) is against endogenous YAP binding to GST-TEAD(1209-426) in a GST pull-down assay, the Kd of His-YAP(1209-426) is determined to be 40 nM[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.
Formula

C93H144ClN23O21S2.xC2HF3O2
CAS 号

1659305-79-9
Sequence

Ac-Val-Pro-{Phe(3-Cl)}-{Hcy}-Leu-Arg-Lys-{Nle}-Pro-Ala-Ser-Phe-Cys-Lys-Pro-Pro-Glu-NH2 (Disulfide bridge:Hcy4-Cys13)
Sequence Shortening

Ac-VP-{Phe(3-Cl)}-{Hcy}-LRK-{Nle}-PASFCKPPE-NH2 (Disulfide bridge:Hcy4-Cys13)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : ≥ 50 mg/mL

* “≥” means soluble, but saturation unknown.
参考文献

  • [1]. Zhang Z, et al. Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction.ACS Med Chem Lett. 2014 Jul 14;5(9):993-8.

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K-975

发表于由

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。

K-975  纯度: 98.55%

K-975 是一种有效的，具有选择性和口服活性的 TEAD 抑制剂，可强烈抑制 YAP1/TAZ 和 TEAD 之间的蛋白质-蛋白质相互作用。K-975 通过丙烯酰胺结构与位于 TEAD 棕榈酸酯结合口袋中的 Cys359 共价结合。 K-975 具有抗恶性胸膜间皮瘤的活性。

K-975

K-975 Chemical Structure

CAS No. : 2563855-03-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥2000 In-stock
10 mg ￥3200 In-stock
25 mg ￥6400 In-stock
50 mg ￥9000 In-stock
100 mg ￥12500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

K-975 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Orally Active Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma[1].

IC50 & Target

TEAD[1]
体外研究
(In Vitro)

K-975 (0.1-10000 nM; 144 h) inhibits the cell proliferation of NF2-non-expressing malignant pleural mesothelioma (MPM) cell lines[1].
K-975 (10-10000 nM; 24 h) inhibits protein-protein interaction (PPI) between Halo-YAP and endogenous TEAD1/4 and Halo-TAZ and TEAD1/4 in NCI-H226 cells[1].
K-975 (0.1-10000 nM; 24 h) strongly inhibits the reporter activity in NCI-H661/CTGF-Luc cells, with the maximum inhibition of ~70%, and does not inhibit the reporter activity in NCI-H661/NRF2-Luc cells[1].
K-975 (1-10000 nM; 24 h) decreases the expressions of CTGF, IGFBP3, and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCI-H226 cells[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 Proliferation Assay[1]

Cell Line: NF2-non-expressing MPM and NF2-expressing malignant MPM cells
Concentration: 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time: 144 hours
Result: Had a stronger inhibitory effect against NF2-non-expressing cell lines than NF2-expressing cell lines.
Inhibited the proliferation of MSTO-211H cells, an NF2-expressing cell line.

Western Blot Analysis[1]

Cell Line: NCI-H226 cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 24 hours
Result: Inhibited TEAD1-YAP1 PPI and TEAD4-YAP1 PPI.
Inhibited TEAD1-TAZ PPI and TEAD4-TAZ PPI.

体内研究
(In Vivo)

K-975 (10-300 mg/kg; p.o. twice a day for 14 days) inhibits the tumor growth by inhibiting YAP1/TAZ-TEAD signaling in MPM xenograft mouse models[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.

Animal Model: Male SCID mice (5 weeks) injected with NCI-H226 or MSTO-211H cells[1]
Dosage: 10, 30, 100, 300 mg/kg
Administration: P.o. twice a day for 14 days
Result: Exhibited strong anti-tumor effect in MPM s.c. xenograft mouse models. Decreased the expressions of CTGF, IGFBP3, and NPPB, and increased the expression of FBXO32 in the NCI-H226 xenograft model.

分子量

287.74

Formula

C16H14ClNO2
CAS 号

2563855-03-6
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 : 220 mg/mL (764.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4754 mL 17.3768 mL 34.7536 mL
5 mM 0.6951 mL 3.4754 mL 6.9507 mL
10 mM 0.3475 mL 1.7377 mL 3.4754 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    40% PEG300    5% Tween-80    45% saline

    Solubility: 5.5 mg/mL (19.11 mM); Suspended solution; Need ultrasonic

    此方案可获得 5.5 mg/mL (19.11 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 55.0 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 5.5 mg/mL (19.11 mM); Clear solution

    此方案可获得 ≥ 5.5 mg/mL (19.11 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 5.5 mg/mL (19.11 mM); Clear solution

    此方案可获得 ≥ 5.5 mg/mL (19.11 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 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*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]. Kaneda A, et, al. The novel potent TEAD inhibitor, K-975, inhibits YAP1/TAZ-TEAD protein-protein interactions and exerts an anti-tumor effect on malignant pleural mesothelioma. Am J Cancer Res. 2020 Dec 1;10(12):4399-4415.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

YAP-TEAD-IN-1

发表于由

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。

YAP-TEAD-IN-1 

YAP-TEAD-IN-1 是 YAP–TEAD 相互作用的有效的竞争性肽类抑制剂 (IC50=25 nM)。YAP-TEAD-IN-1 是一种 17mer 的多肽，与 YAP (50-171) (Kd=40 nM) 相比，其与 TEAD1 的结合亲和力更高 (Kd=15 nM)。

YAP-TEAD-IN-1

YAP-TEAD-IN-1 Chemical Structure

CAS No. : 1659305-78-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

YAP-TEAD-IN-1 的其他形式现货产品:

YAP-TEAD-IN-1 TFA

生物活性

YAP-TEAD-IN-1 is a potent and competitive inhibitor of YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM)[1].

IC50 & Target

IC50: 25 nM (YAP–TEAD interaction)[1]
体外研究
(In Vitro)

YAP-TEAD-IN-1 (peptide 17)(2 μM) is against endogenous YAP binding to GST-TEAD (1209-426) in a GST pull-down assay, the Kd of His-YAP1209-426 is determined to be 40 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

2019.86

Formula

C93H144ClN23O21S2
CAS 号

1659305-78-8
Sequence Shortening

Ac-VP-{Phe(3-Cl)}-{Hcy}-LRK-{Nle}-PASFCKPPE-NH2 (Disulfide bridge:Hcy4-Cys13)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zhang Z, et al. Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction.ACS Med Chem Lett. 2014 Jul 14;5(9):993-8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

VT103

发表于由

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。

VT103 

VT103 是 VT101 的类似物，是一种具有口服活性和选择性的 TEAD1 蛋白棕榈酰化抑制剂。 VT103 抑制 YAP/TAZ-TEAD 促进的基因转录，阻断 TEAD auto-palmitoylation，阻断 YAP/TAZ和TEAD 之间的相互作用。VT103 可用于癌症研究。

VT103

VT103 Chemical Structure

CAS No. : 2290608-13-6

规格 价格 是否有货
5 mg ￥4000 询问价格 & 货期
10 mg ￥6800 询问价格 & 货期
25 mg ￥13500 询问价格 & 货期

* Please select Quantity before adding items.

VT103 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Orally Active Compound Library
  • Chemical Probe Library
  • Transcription Factor Targeted Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer[1].

IC50 & Target

TEAD1 Palmitoylation[1]
体外研究
(In Vitro)

VT103 (HEK293T cells; 3 μM) appeares to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4. VT103 (NF2-deficient NCI-H226 cells; 3 mmol/L; 4 or 24 hours) selectively disrupts YAP–TEAD1 interaction[1].
VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1[1].
VT103 shows an IC50 of 1.02 nM in YAP reporter assay[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.
体内研究
(In Vivo)

VT103 (0.3~10 mg/kg; p.o. once per day) blocks tumor growth even at 0.3 mg/kg[1].
Pharmacokinetics of VT103 in mice[1]

Dose IV PO
7 mg/kg T1/2 (hours) Vdss (L/kg) CI(mL/min/kg) AUC 0-24 hours (μg*h/mL) AUC 0-24 hours (μg*h/mL) Oral availability (%) Cmax (ng/mL) C24 hours (ng/mL)
13.2 4.5 4.7 20.0 14.9 75 896 (1 hour) 340

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.

Animal Model: NCI-H226-tumor bearing mice[1]
Dosage: 0.3~10 mg/kg
Administration: P.o. once per day
Result: Blocked tumor growth even at 0.3 mg/kg.

分子量

410.41

Formula

C18H17F3N4O2S
CAS 号

2290608-13-6
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 : 50 mg/mL (121.83 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4366 mL 12.1829 mL 24.3659 mL
5 mM 0.4873 mL 2.4366 mL 4.8732 mL
10 mM 0.2437 mL 1.2183 mL 2.4366 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。
参考文献

  • [1]. Tang TT, et al. Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. Mol Cancer Ther. 2021;20(6):986-998.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务