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製品番号: HY-184179

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TEAD degrader-1

TEAD degrader-1 is a potent FBXO22-mediated molecular glue degrader of TEAD, with a 24 h DC₅₀ of 1.0 nM. TEAD degrader-1 binds reversibly and covalently to FBXO22 C326, assembles a functional ternary complex, and mediates proteasomal degradation of TEAD. TEAD degrader-1 exhibits high selectivity for the Hippo pathway and specifically downregulates only TEAD and its downstream target proteins. TEAD degrader-1 is applicable to research related to malignant pleural mesothelioma and non-small cell lung cancer.

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CAS 番号: 3103984-17-1
分子式: C₃₆H₃₈ClF₂N₃O₆
分子量:682.15

保管条件:

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

TEAD degrader-1 構造式

CAS 番号: 3103984-17-1

価格（税別）

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

IC₅₀ & Target

^[1]

TEAD

3.1 nM (IC₅₀)

YAP アイソフォーム固有の製品をすべて表示 :

体外実験

TEAD degrader-1 (compound 15) potently inhibits the TEAD1-YAP1 protein-protein interaction with an IC₅₀ of 3.1 nM in a cell-free biochemical assay^[1].
TEAD degrader-1 potently and rapidly degrades TEAD in NCI-H226 mesothelioma cells, with a DC₅₀ of 1.9 nM (6 h, 97% D_max) and 1.0 nM (24 h, 98% D_max), and sustained deep degradation for up to 72 hours^[1].
TEAD degrader-1 (24 h) potently degrades TEAD in MSTO-211H mesothelioma cells, achieving > 72% maximal degradation with a DC₅₀ < 80 nM after 24 hours^[1].
TEAD degrader-1 (24 h) potently inhibits TEAD target gene (CCN1, CCN2) expression in MSTO-211H mesothelioma cells, with > 90% maximal inhibition and an IC₅₀ < 2 nM after 24 hours^[1].
TEAD degrader-1 (120 h) potently inhibits the viability of Hippo pathway-dysregulated MSTO-211H mesothelioma cells, achieving >95% maximal growth inhibition after 120 hours^[1].

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

化学情報

CAS 番号 3103984-17-1
分子量 682.15
分子式 C₃₆H₃₈ClF₂N₃O₆
SMILES

O=C(N)C1=[C@]([C@]2=C(Cl)C(F)=CC3=C2[C@H](C)[C@](C4=CC=CC=C4)(CN[C@@H]5CC[C@@H](C(N6CC(C=O)OCC6)=O)CC5)O3)C(F)=C(OC)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Fisher M, et al. Identification and SAR optimization of FBXO22-mediated TEAD Targeted Glue™ degraders. bioRxiv. 2026.

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
化学情報
純度とドキュメンテーション
参考文献

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TEAD degrader-1

YAP アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC50 & Target

体外実験

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

TEAD degrader-1 関連分類

HY-184179 関連分類

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