1. Epigenetics
  2. Histone Methyltransferase

PFI-2 (Synonyms: (R)-PFI-2)

Cat. No.: HY-18627
Handling Instructions

PFI-2 is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.

For research use only. We do not sell to patients.

PFI-2 Chemical Structure

PFI-2 Chemical Structure

CAS No. : 1627676-59-8

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50 mg USD 540 Get quote

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Description

PFI-2 is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2. IC50 value: 2 nM [1] Target: SETD7 (R)-PFI-2 is highly selective (>1,000-fold) for SETD7, over a panel of 18 other human protein methyltransferases and DNMT1, and was shown to be inactive against 134 additional ion channel, GPCR, and enzyme targets (<35% inhibition at 10 μM). (R)-PFI-2 binds to SETD7 only in the presence of SAM. PFI-766, a biotinylated variant of (R)-PFI-2 that retains the ability to bind and inhibit SETD7 (IC50 110 ± 26 nM in our in vitro enzymatic assay). PFI-766 engagement of endogenous SETD7 was also confirmed by mass spectrometry that supported the high specificity of the compound for endogenous SETD7.

References
Molecular Weight

499.52

Formula

C₂₃H₂₅F₄N₃O₃S

CAS No.

1627676-59-8

SMILES

O=S(C1=CC2=C(CNCC2)C(F)=C1)(N[[email protected]](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Cat. No.: HY-18627