Homo-BacPROTAC7 TFA
Homo-BacPROTAC7 TFA is a PROTAC protein degrader targeting ClpC1/ClpC2 with a Kd of 0.5-2.5 nM for both targets. Homo-BacPROTAC7 (TFA) acts as a bactericidal agent, induces killing of pathogenic mycobacteria, retains activity against dormant-like mycobacterial cells with reduced intracellular ATP levels, and shows elevated antibiotic potency relative to its parent monomer. Homo-BacPROTAC7 (TFA) can be used for the research of tuberculosis.
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: C111H150F12N22O26
- 分子量:2436.49
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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生物活性
製品説明
体外実験
Homo-BacPROTAC7 TFA (100 μM; 2 h) induces degradation of ~80% of purified M. tuberculosis ClpC1_NTD substrate via the ClpC1P1P2 protease in vitro[1].
Homo-BacPROTAC7 TFA (12.5 μM; 24 h) reduces ClpC1 levels to 34% and ClpC2 levels to 51% (relative to dCym7 treatment) in M. smegmatis ATCC 607 cells[1].
Homo-BacPROTAC7 TFA (100-0.048 μM; 5 days) exhibits potent antibacterial activity against M. tuberculosis H37Rv wild-type cells with an MIC50 of 0.26 μM (150-fold more potent than dCymM) and against ΔclpC2 mutant cells with an MIC50 of 0.18 μM after 5 days of treatment[1].
Homo-BacPROTAC7 TFA(7.8 μM; 48 h) induces a 5-fold reduction in ClpC1 levels and significant reduction in ClpC2 levels in M. tuberculosis H37Rv wild-type cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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性状 Solid
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分子量 2436.49
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分子式 C111H150F12N22O26
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Color White to off-white
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SMILES
O=C(N[C@H](C(N(C)[C@H](C(N[C@@H](CC1=CN(CCCCCN2N=NC(C[C@H](NC([C@@H](N(C)C([C@H](C(C)C)NC([C@H]([C@@H](C3=CC=CC=C3)OC)NC([C@H](C)NC([C@@H](N4C)C[C@@H](C)CO)=O)=O)=O)=O)CC(C)C)=O)C(N[C@@H](CC5=CN(C)C6=C5C=CC=C6)C4=O)=O)=C2)N=N1)C(N[C@@H](CC7=CN(C)C8=C7C=CC=C8)C9=O)=O)=O)CC(C)C)=O)C(C)C)[C@@H](NC([C@H](C)NC([C@H](C[C@H](CO)C)N9C)=O)=O)[C@H](OC)C%10=CC=CC=C%10.FC(F)(F)C(O)=O.FC(F)(F)C(O)=O.FC(F)(F)C(O)=O.FC(F)(F)C(O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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)