2. IAP ligand 8

IAP ligand 8 是一种 SMAC 模拟物和 IAP (凋亡抑制蛋白) BIR 结构域的结合剂，选择性靶向 cIAP1-BIR3、XIAP-BIR2 和 XIAP-BIR3，SPR 的 pKD 分别为 7.8、7.0、6.7。IAP ligand 8 可作为 IAP 配体模块，与靶向 TEAD1 P 位点的降解剂一起、通过连接子偶联形成 IAP 招募型蛋白水解靶向嵌合体 (PROTACs/IPDs)。该 IPD 可招募 IAP E3 泛素连接酶形成 TEAD1-IPD-IAP 三元复合物，进而介导 TEAD1 的泛素化和蛋白酶体依赖性降解，同时可诱导 cIAP1 的自降解。IAP ligand 8 及系列降解剂可用于 Hippo 通路异常激活相关的恶性胸膜间皮瘤等实体肿瘤的研究。

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IAP ligand 8

IAP ligand 8 Chemical Structure

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IAP ligand 8 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IAP ligand 8 is a SMAC mimetic and a binder of the BIR domain of IAP (inhibitor of apoptosis protein), which selectively targets cIAP1-BIR3, XIAP-BIR2 and XIAP-BIR3, with pKD values of 7.8, 7.0 and 6.7 respectively as determined by SPR. IAP ligand 8 serves as an IAP ligand moiety, which can be conjugated via a linker with degraders targeting the P site of TEAD1 to form IAP-recruiting proteolysis-targeting chimeras (PROTACs/IPDs). This IPD recruits IAP E3 ubiquitin ligase to form a TEAD1-IPD-IAP ternary complex, thereby mediating the ubiquitination and proteasome-dependent degradation of TEAD1, while inducing the autodegradation of cIAP1. IAP ligand 8 and its series of degraders can be used for the research of solid tumors such as malignant pleural mesothelioma associated with abnormal activation of the Hippo pathway[1].
体外研究
(In Vitro)

IAP ligand 8 (EA238) (10 nM-1 μM; 72 h) 以浓度依赖的方式显著降低 H28 细胞的存活率[1]。

IAP ligand 8 (1 μM; 48 h) 可诱导 H28 细胞中 45% 的细胞发生凋亡，显著高于对照组[1]。

IAP ligand 8 (100 nM, 1 μM; 24 h) 可诱导 H28 细胞的细胞周期阻滞于 G2/M 期，G1 期细胞比例降低约 20%[1]。

IAP ligand 8 (1 μM; 24 h) 下调 H28 细胞中 cIAP1 蛋白的表达水平，而上调剪切型半胱天冬酶 3 (cleaved-caspase 3) 的表达[1]。
IAP ligand 8 (100 nM, 1 μM; 24 h) 可下调 H28 细胞中 XIAP 和 TNF-α 的 mRNA 表达水平[1]。
IAP ligand 8 (100 nM, 1 μM; 48 h) 抑制 H28 细胞迁移，其划痕伤口愈合率分别降低了 30%和 65%[1]。
IAP ligand 8 (1 μM; 24 h) 会导致 H28 细胞的细胞质中 cIAP1 荧光信号显著降低，同时 cleaved-PARP 荧光信号升高[1]。

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

IAP ligand 8 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: H28 cell
Concentration: 10 nM, 100 nM, 1 μM
Incubation Time: 72 h
Result: Significantly reduced the cell viability of H28 cells in a concentration-dependent manner, with viability rates of 85%, 60% and 25% at 10 nM, 100 nM and 1 μM respectively, compared with the control group (set as 100%).

Apoptosis Analysis[1]

Cell Line: H28 cell
Concentration: 100 nM, 1 μM
Incubation Time: 72 h
Result: Induced apoptosis of H28 cells, with apoptotic rates of 20% at 100 nM and 45% at 1 μM, while the apoptotic rate of the control group was only 5%.

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: H28 cell
Concentration: 100 nM, 1 μM
Incubation Time: 24 h
Result: Downregulated the protein expression of cIAP1 by 60% at 100 nM and 80% at 1 μM, upregulated the expression of cleaved-caspase 3 by 1.5-fold at 100 nM and 2.5-fold at 1 μM, and had no significant effect on XIAP protein expression.
分子量

424.48

Formula

C21H30F2N4O3
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

IAP ligand 8 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

IAP ligand 8IAP ligand8IAP ligand-8PROTACs/IPDsSMAC mimeticIAP-recruiting proteolysis-targeting chimerasIAP familyTEAD1Inhibitorinhibitorinhibit

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