(S)-PFI-2 hydrochloride
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2.
For research use only. We do not sell to patients.
- CAS No.: 1627607-88-8
- Formula: C23H26ClF4N3O3S
- Molecular Weight:535.98
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
(S)-PFI-2 hydrochloride (10 μM; 2 h) cannot cause a dose-dependent increase in nuclear YAP in MCF7 cells or enhance the expression of YAP target genes AREG and CYR61; while (R)-PFI-2 can increase the expression of YAP, AREG and CYR61 expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1627607-88-8
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Molecular Weight 535.98
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Formula C23H26ClF4N3O3S
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SMILES
O=S(C1=CC2=C(CNCC2)C(F)=C1)(N[C@@H](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Niu Y, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547. [Content Brief]
[2]. Barsyte-Lovejoy D, et al. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(S)-PFI-2 hydrochloride Related Classifications
HY-110196 Related Classifications
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