TNG961
TNG961 is a selective and orally active CRBN-mediated HBS1L molecular glue degrader. TNG961 induces formation of an HBS1L-TNG961-CRBN ternary complex, leading to potent degradation of HBS1L and secondary destabilization of its binding partner PELO. TNG961 can reduce HBS1L protein levels, thereby disrupting the PELO region involved in ribosome rescue. TNG961 can be used for the study of FOCAD-deficient cancers, such as pancreatic cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C28H24F3N3O3S
- 分子量:539.57
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
In vitro, TNG961 leads to a dose-dependent decrease in HBS1L protein levels, which in turn destabilizes the portion of PELO involved in ribosome rescue. TNG961 displays proteome-wide selectivity for HBS1L, with no change in SALL4 protein level as determined by western blot. TNG961-induced HBS1L degradation and PELO destabilization can both be rescued by inactivation of CRBN confirming mechanism[1].
In engineered HiBiT knock-in cells, treatment with TNG961 induces maximal HBS1L degradation within 4 hours, without affecting GSPT1 protein levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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分子量 539.57
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分子式 C28H24F3N3O3S
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SMILES
O=C(NC1=O)CC[C@@H]1C(C=C2)=CC3=C2C(NC(NC(C)(C)C4=CC(C=CC(C(F)(F)F)=C5)=C5S4)=O)=CC=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)