SSM3 tetraTFA
SSM3 tetraTFA is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA is able to block furin-dependent cell surface processing of anthrax protective antigen-83 in vitro.
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- CAS. Nr.: 2320930-10-5
- Formel: C30H36F12N12O10
- Molecular Weight:952.66
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
EC50: 54 nM (furin)Ki: 12 nM (furin)[1]
SSM3 tetraTFA is against furin cleavage of the Pyr-RTKR-AMC substrate with an EC50 of 54 nM in vitro cleavage assays and cell-based tests[2].SSM3 tetraTFA (0.1-25 μM) inhibits the furin-dependent conversion of PA83 into PA63 in a dose dependent manner, it inhibits PA83 processing in the cleavage reactions[2].SSM3 tetraTFA shows comparable potency against furin (Ki=0.012 μM) and PC6B (Ki=0.004 μM), these compounds preferentially inhibited furin over PACE4 (Ki=0.041 μM) by 2- to 10-fold and over PC7 (Ki=0.595 μM) by 11- to 76-fold. In addition, it inhibits LF (Ki=1.241 μM) 25- to 167-fold less effectively than in furin and shows no measurable inhibition against trypsin and MT1-MMP[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2320930-10-5
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Molecular Weight 952.66
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Formel C30H36F12N12O10
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SMILES
N=C(N)NC(C=C1)=CC=C1O[C@@H]2[C@H](C[C@@H](NC(N)=N)[C@H](OC3=CC=C(NC(N)=N)C=C3)C2)NC(N)=N.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Albert G Remacle, et al. Selective and Potent Furin Inhibitors Protect Cells From Anthrax Without Significant Toxicity. Int J Biochem Cell Biol [Content Brief]
[2]. Guan-Sheng Jiao, et al. Synthetic Small Molecule Furin Inhibitors Derived From 2,5-dideoxystreptamine. Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19707-12. [Content Brief]
Calculators
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