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

PROTAC TEAD1/IAP degrader-3 是一种 TEAD1/IAP PROTAC 降解剂。PROTAC TEAD1/IAP degrader-3 招募 cIAP1 和 XIAP E3 连接酶形成三元复合物，驱动 TEAD1 的蛋白酶体降解，并触发 cIAP1 的自泛素化和蛋白酶体降解。PROTAC TEAD1/IAP degrader-3 可抑制细胞增殖。PROTAC TEAD1/IAP degrader-3 可通过依赖 TEAD 的方式下调 CTGF 基因表达来调控 Hippo 通路活性。PROTAC TEAD1/IAP degrader-3 可用于间皮瘤的研究。

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PROTAC TEAD1/IAP degrader-3

PROTAC TEAD1/IAP degrader-3 Chemical Structure

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PROTAC TEAD1/IAP degrader-3 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 YAP 亚型特异性产品:

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC TEAD1/IAP degrader-3 is a TEAD1/IAP PROTAC degrader. PROTAC TEAD1/IAP degrader-3 recruits the cIAP1 and XIAP E3 ligases to form a ternary complex, drives proteasomal degradation of TEAD1, and triggers autoubiquitination and proteasomal degradation of cIAP1. PROTAC TEAD1/IAP degrader-3 inhibits cell proliferation. PROTAC TEAD1/IAP degrader-3 regulates Hippo pathway activity by downregulating CTGF gene expression in a TEAD-dependent manner. PROTAC TEAD1/IAP degrader-3 is applicable to the research of mesothelioma[1].

IC50 & Target[1]

cIAP1

 

TEAD1

 

体外研究
(In Vitro)

PROTAC TEAD1/IAP degrader-3 (A538) (0.0001-10 μM; 20 h) 可在 NCI-H2052 细胞中诱导 TEAD1 发生蛋白酶体依赖性降解，其 DC50 为 44 nM，最大降解率为 42%，降解依赖于 cIAP1 和 XIAP，其中 XIAP 有助于实现最大降解效力，cIAP1 则有助于提升降解剂的活性[1]。
PROTAC TEAD1/IAP degrader-3 (0.001-10 μM; 20 h) 可在 NCI-H226 细胞中诱导 TEAD1 发生部分降解，其 DC50 为 76 nM，最大降解率为 38%[1]。
PROTAC TEAD1/IAP degrader-3 (0.0001-30 μM; 4 h) 可在 NCI-H2052 细胞中与 cIAP1、XIAP 及 TEAD1 共同形成稳定的三元复合物[1]。
PROTAC TEAD1/IAP degrader-3 (0.5 μM; 16 h) 可在 NCI-H2052 细胞中特异性下调蛋白质组水平的 TEAD1，而对其他 TEAD 旁系同源物无显著影响[1]。
PROTAC TEAD1/IAP degrader-3 (1 nM-10 μM; 144 h) 可抑制 ZL55、NCI-H2052、 NCI-H226 细胞系的增殖[1]。
PROTAC TEAD1/IAP degrader-3 (0.001-10 μM; 48 h) 在 ZL55、NCI-H2052、 NCI-H226 细胞中可通过依赖 TEAD 的方式下调 CTGF 基因表达来调控 Hippo 通路活性[1] 。

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

PROTAC TEAD1/IAP degrader-3 相关抗体:

Western Blot Analysis[1]

Cell Line: NCI-H2052 cells (stably expressing HiBiT-TEAD1; wildtype)
Concentration: 0, 0.0001,0.001, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 M
Incubation Time: 20 h
Result: Achieved 48% degradation of endogenous TEAD1 at 3 μM treatment.
Induced HiBiT-TEAD1 degradation with a Dmax of 49% and a DC50 of 293 nM.
Degraded endogenous TEAD1 with a Dmax of 42% and a DC50 of 44 nM.

Western Blot Analysis[1]

Cell Line: NCI-H226 cells
Concentration: 0.001-10 μM
Incubation Time: 20 h
Result: Degraded endogenous TEAD1 with a Dmax of 38% and a DC50 of 76 nM.

Western Blot Analysis[1]

Cell Line: NCI-H2052 cells
Concentration: 3 μM; 5 μM (MG132)
Incubation Time: 16 h
Result: Completely abolished TEAD1 degradation induced by 3 μM PROTAC TEAD1/IAP degrader-3 (A538), with near 100% recovery of TEAD1 levels, in the presence of MG132.

Western Blot Analysis[1]

Cell Line: NCI-H2052 wildtype, cIAP1 KO, XIAP KO, and cIAP1/XIAP DKO cell lines
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 20 h
Result: Induced TEAD1 degradation in wildtype cells with a Dmax of 48% and a DC50 of 64 nM.
Reduced Dmax to 27% with a DC50 of 61 nM in XIAP KO cells.
Right-shifted DC50 to 340 nM with a Dmax of 44% in cIAP1 KO cells.
Achieved a Dmax of 28% with a DC50 of 220 nM in cIAP1/XIAP DKO cells.

Western Blot Analysis[1]

Cell Line: NCI-H2052 cells; NCI-H226 transgenic cell lines (stably expressing HiBiT-TEAD1-4)
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM (endogenous assay); 0.3 nM-10 μM (HiBiT assay)
Incubation Time: 20 h (endogenous assay); 18 h (HiBiT assay)
Result: Degraded TEAD4 with a Dmax of 9% and a DC50 of 510 nM in NCI-H2052 cells, compared to TEAD1 Dmax of 42% and DC50 of 44 nM.
Induced degradation of TEAD1 with a Dmax of ~40%, TEAD2 with a Dmax of <5%, TEAD3 with a Dmax of 13%, and TEAD4 with a Dmax of <5% in NCI-H226 HiBiT assays.

Cell Proliferation Assay[1]

Cell Line: ZL55, NCI-H226, NCI-H2052 (mesothelioma cell lines); NCI-H520 (Hippo pathway-independent cell line)
Concentration: 1 nM-10 μM
Incubation Time: 144 h
Result: Inhibited proliferation in ZL55 cells with an IC50 of 925 nM and an Emax of 100%.
Inhibited proliferation in NCI-H226 cells with an IC50 of 733 nM and an Emax of 100%.
Inhibited proliferation in NCI-H2052 cells with an IC50 of 1267 nM and an Emax of 99%.
Inhibited proliferation in NCI-H520 cells with an IC50 of 443 nM and an Emax of 96%.

Real Time qPCR[1]

Cell Line: ZL55, NCI-H226, NCI-H2052 (mesothelioma cell lines)
Concentration: 0.001-10 μM
Incubation Time: 48 h
Result: Inhibited CTGF expression in ZL55 cells with an IC50 >1000 nM.
Inhibited CTGF expression in NCI-H226 cells with an IC50 of 826 nM and an Emax of 99%.
Inhibited CTGF expression in NCI-H2052 cells with an IC50 of 875 nM and an Emax of 89%.
分子量

870.93

Formula

C47H50F4N6O6
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-3 相关分类

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  • 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-3PROTACsYAPYes-associated proteinTEAD1/IAP PROTAC degraderNCI-H2052 cellsNCI-H226 cellsZL55 cells
Inhibitorinhibitorinhibit

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