A SET7/9 inhibitor
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(R)-PFI-2 (hydrochloride)

Item No. 14678

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)Epigenetic Chemical Probe Guide (PDF)
Technical Information
Formal Name
8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, monohydrochloride
CAS Number
1627607-87-7
Synonyms
  • (-)-PFI-2
Molecular Formula
C23H25F4N3O3S • HCl
Formula Weight
536.0
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 2 mg/mlEthanol: 0.5 mg/ml
SMILES
O=S(C1=CC(CCNC2)=C2C(F)=C1)(N[C@H](CC3=CC(C(F)(F)F)=CC=C3)C(N4CCCC4)=O)=O.Cl
InChi Code
InChI=1S/C23H25F4N3O3S.ClH/c24-20-13-18(12-16-6-7-28-14-19(16)20)34(32,33)29-21(22(31)30-8-1-2-9-30)11-15-4-3-5-17(10-15)23(25,26)27;/h3-5,10,12-13,21,28-29H,1-2,6-9,11,14H2;1H/t21-;/m1./s1
InChi Key
ZADKZNVAJGEFLC-ZMBIFBSDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $83

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    10 mg

    $152

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    25 mg

    $275

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    Product Description

    (R)-PFI-2 is a potent, cell-permeable inhibitor of SET7/9 (IC50 = 2 nM) that demonstrates greater than 1,000-fold selectivity over a panel of 18 other methyltransferases.1 Its enantiomer, (S)-PFI-2 (Item No. 18119), is 500-fold less active (IC50 = 1 µM).1 See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Barsyte-Lovejoy, D., Li, F., Oudhoff, M.J., et al. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc. Natl. Acad. Sci. USA 111(35), 12853-12858 (2014).