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(R)-PFI-2 (hydrochloride)

Item № 14678
CAS № 1627607-87-7
Purity ≥95%
product image
                (CAS 1627607-87-7)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $39.00 0.00
     5 mg $127.00 0.00
     10 mg $234.00 0.00
     25 mg $536.00 0.00

Pricing updated 2019-05-26. Prices are subject to change without notice.

Description
Synonyms
  • (-)-PFI-2

SET domain-containing protein 7/9 (SET7/9) is a histone methyltransferase that monomethylates lysine 4 of histone H3, which generates a specific tag for epigenetic transcriptional activation. It plays a role in the transcriptional activation of tumor suppressor p53 in response to DNA damage as well as the transcription factor TAF10.1,2 (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.3 Its enantiomer, (S)-PFI-2 (Item No. 18119), is 500-fold less active (IC50 = 1 µM).3 See the Structural Genomics Consortium (SGC) website for more information.

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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
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
Downloads & Resources
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Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

Download SGC Epigenetic Chemical Probe Guide

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References & Product Citations
Product Description References

1. Couture, J.F., Collazo, E., Hauk, G., et al. Structural basis for the methylation site specificity of SET7/9 Nature Structural & Molecular Biology 13(2), 140-146 (2006).

2. Kurash, J.K., Lei, H., Shen, Q., et al. Methylation of p53 by Set7/9 mediates p53 acetylation and activity in vivo Molecular Cell 29, 392-400 (2008).

3. 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 Proceedings of the National Academy of Sciences of the United States of America 111(35), 12853-12858 (2014).

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