( R )-PFI 2 hydrochloride

• Supplier: Tocris Bioscience
• Catalog: 4445
• Prices: $299.00
• Sizes: 10 mg
• Function Type: Inhibitor
• Cas Number: 1627607-87-7
• Chemical Name: (1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamidehydrochloride
• Formula: C23H25F4N3O3S.HCl
• Molecular Weight: 535.98
• Purity: >97 %
• Description: Potent and selective SETD7 histone lysine methyltransferase inhibitor (IC 50 = 2 nM). Exhibits >1000-fold selectivity over DNMT1 and a panel of 18 other methyltransferases. Inhibits YAP nuclear translocation and function following activation of the Hippo signaling pathway in MCF7 cells. Negative control ( S )-PFI 2 hydrochloride (Cat. No. 5400) available.

Product References

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity - (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity

Barsyte-Lovejoy D, Li F, Oudhoff MJ, Tatlock JH, Dong A, Zeng H, Wu H, Freeman SA, Schapira M, Senisterra GA, Kuznetsova E, Marcellus R, Allali-Hassani A, Kennedy S, Lambert JP, Couzens AL, Aman A, Gingras AC, Al-Awar R, Fish PV, Gerstenberger BS, Roberts L, Benn CL, Grimley RL, Braam MJ, Rossi FM, Sudol M, Brown PJ, Bunnage ME, Owen DR, Zaph C, Vedadi M, Arrowsmith CH. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8. doi: