2412923-11-4
Chemical Structure
TFMU-ADPr
- CAS No.: 2412923-11-4
- Formula:C25H26F3N5O16P2
- Molecular Weight:771.44
IUPAC Name: 1-(2-methoxyphenyl)adamantane
InChIKey: JNMHMJORTGCLAH-IPSZZCKZSA-N
SMILES: O[C@H]1[C@](O[C@@H]([C@H]1O)COP(OP(OC[C@H]2O[C@@H]([C@@H]([C@@H]2O)O)OC3=CC=C(C(C(F)(F)F)=CC(O4)=O)C4=C3)(O)=O)(O)=O)([H])N5C6=NC=NC(N)=C6N=C5
Biological Activity: TFMU-ADPr is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr is also applicable to COVID-19-related research[1][2][3].
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TFMU-ADPr | TFMU-ADPr is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr is also applicable to COVID-19-related research. | |||||||||||||||||||||
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References
- [1]. Rack JGM, et al. (ADP-ribosyl)hydrolases: Structural Basis for Differential Substrate Recognition and Inhibition. Cell Chem Biol. 2018 Dec 20;25(12):1533-1546.e12. [Content Brief]
- [2]. Drown BS, et al. Monitoring Poly(ADP-ribosyl)glycohydrolase Activity with a Continuous Fluorescent Substrate. Cell Chem Biol. 2018;25(12):1562-1570.e19. [Content Brief]
- [3]. Anmangandla A, et al. A Fluorescence Polarization Assay for Macrodomains Facilitates the Identification of Potent Inhibitors of the SARS-CoV-2 Macrodomain. ACS Chem Biol. 2023;18(5):1200-1207. [Content Brief]
