Homo-BacPROTAC7 TFA 

Homo-BacPROTAC7 TFA is a PROTAC protein degrader targeting ClpC1/ClpC2 with a K_d 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^[1].

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.

2436.49

C₁₁₁H₁₅₀F₁₂N₂₂O₂₆

Solid

White to off-white

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Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Hoi DM, et al. Clp-targeting BacPROTACs impair mycobacterial proteostasis and survival. Cell. 2023;186(10):2176-2192.e22.  [Content Brief]