(Rac)-TNG961
(Rac)-TNG961 is the rac isomer of TNG961 (HY-183115). 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.
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- CAS 番号: 3127008-95-8
- 分子式: C28H24F3N3O3S
- 分子量:539.57
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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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CAS 番号 3127008-95-8
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性状 Solid
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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)CCC1C(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
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 100 mg/mL (185.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8533 mL | 9.2666 mL | 18.5333 mL | 46.3332 mL |
| 5 mM | 0.3707 mL | 1.8533 mL | 3.7067 mL | 9.2666 mL | |
| 10 mM | 0.1853 mL | 0.9267 mL | 1.8533 mL | 4.6333 mL | |
| 15 mM | 0.1236 mL | 0.6178 mL | 1.2356 mL | 3.0889 mL | |
| 20 mM | 0.0927 mL | 0.4633 mL | 0.9267 mL | 2.3167 mL | |
| 25 mM | 0.0741 mL | 0.3707 mL | 0.7413 mL | 1.8533 mL | |
| 30 mM | 0.0618 mL | 0.3089 mL | 0.6178 mL | 1.5444 mL | |
| 40 mM | 0.0463 mL | 0.2317 mL | 0.4633 mL | 1.1583 mL | |
| 50 mM | 0.0371 mL | 0.1853 mL | 0.3707 mL | 0.9267 mL | |
| 60 mM | 0.0309 mL | 0.1544 mL | 0.3089 mL | 0.7722 mL | |
| 80 mM | 0.0232 mL | 0.1158 mL | 0.2317 mL | 0.5792 mL | |
| 100 mM | 0.0185 mL | 0.0927 mL | 0.1853 mL | 0.4633 mL |
(Rac)-TNG961 関連分類
HY-183115A 関連分類
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