2. PROTAC Stem Cell/Wnt Apoptosis
  3. PROTACs YAP IAP
  4. PROTAC TEAD1/IAP degrader-1

PROTAC TEAD1/IAP degrader-1 (Compound A232) 是一种选择性的 TEAD1 和 cIAP1 PROTAC 类降解剂，DC50 分别为 14 nM 和 270 nM。PROTAC TEAD1/IAP degrader-1 能促进 TEAD1 和 cIAP1 的泛素化和降解。PROTAC TEAD1/IAP degrader-1 下调 TEAD 依赖性基因 CTGF 的表达。PROTAC TEAD1/IAP degrader-1 对间皮瘤具有抗癌活性。
(粉色: TEAD1 配体 (HY-181536)；蓝色: YAP 配体 (HY-181530)；黑色: 连接子 (HY-141371))。

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PROTAC TEAD1/IAP degrader-1

PROTAC TEAD1/IAP degrader-1 Chemical Structure

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PROTAC TEAD1/IAP degrader-1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 YAP 亚型特异性产品:

查看所有亚型
YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

查看 IAP 亚型特异性产品:

查看所有亚型
cIAP cIAP-1 cIAP-2 XIAP

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma[1]. (Pink: TEAD1 ligand (HY-181536); Blue: YAP ligand (HY-181530); Black: linker (HY-141371)).

IC50 & Target[1]

cIAP1

270 nM (DC50)

TEAD1

14 nM (DC50)

体外研究
(In Vitro)

PROTAC TEAD1/IAP degrader-1 (20 h) 处理 NCI-H2052 细胞 20 h 后，可诱导 HiBiT-TEAD1 发生最大 55% 的降解，其 DC50 为 196 nM[1]。
PROTAC TEAD1/IAP degrader-1 (0.01-10 μM; 20 h) 处理 20 h 后，可在 NCI-H2052 细胞中诱导内源性 TEAD1 发生最高 32% 的降解，其 DC50 为 14 nM；同时可诱导内源性 cIAP1 发生最高 88% 的降解，其 DC50 为 270 nM[1]。
PROTAC TEAD1/IAP degrader-1 (0.001-10 μM; 144 h) 可抑制 ZL55、NCI-H226、NCI-H2052 和 NCI-H520 细胞的增殖，其 IC50 值分别为 2194 nM、798 nM、1375 nM 和 2491 nM，且在处理 144 h 后可实现近乎完全的最大抑制效果[1]。
PROTAC TEAD1/IAP degrader-1 (0.001-10 μM; 48 h) 可降低 ZL55、NCI-H226 和 NCI-H2052 细胞中 CTGF 的转录水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC TEAD1/IAP degrader-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: ZL55, NCI-H226, NCI-H2052, NCI-H520
Concentration: 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 144 h
Result: Inhibited cell proliferation with an IC50 of 2194 nM (ZL55), 798 nM (NCI-H226), 1375 nM (NCI-H2052), and 2491 nM (NCI-H520), with a maximum inhibition (Emax) of 99% (ZL55), 100% (NCI-H226), 99% (NCI-H2052), and 98% (NCI-H520).

Real Time qPCR[1]

Cell Line: ZL55, NCI-H226, NCI-H2052
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 48 h
Result: Reduced CTGF transcript levels with an IC50 of 866 nM (ZL55), 497 nM (NCI-H226), and 125 nM (NCI-H2052), with an Emax of 72% (ZL55), 100% (NCI-H226), and 73% (NCI-H2052).
分子量

910.96

Formula

C46H45F3N8O7S
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.
纯度 & 产品资料
参考文献

PROTAC TEAD1/IAP degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC TEAD1/IAP degrader-1PROTACsYAPIAPYes-associated proteinpalmitoylation pocketproteasomal degradationcIAP1mesotheliomaTEAD1TEAD4ubiquitinationTEAD2CTGFTEAD3Inhibitorinhibitorinhibit

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产品名称：
PROTAC TEAD1/IAP degrader-1
目录号：
HY-181534
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