A potent and selective SETD7 histone lysine methyltransferase inhibitor. K i = 0.33 nM and IC 50 = 2 nM against SETD7. It displays > 1000-fold selectivity against DNMT1 and many other\xa0methyltransferases.
Storage Temp
Protected from light,Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of SET domain containing 7; histone lysine methyltransferase
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Shipped at 4°C. Store at -20°C. Store In the Dark.
1.Barsyte-Lovejoy D, Li F, Oudhoff MJ, Tatlock JH, Dong A, Zeng H, Wu H, Freeman SA, Schapira M, Senisterra GA et al.. (2014) (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.. Proc Natl Acad Sci USA, 111 (35):(12853-8). [PMID:25136132]
2.Guitot K et al.. (2017) A direct label-free MALDI-TOF mass spectrometry based assay for the characterization of inhibitors of protein lysine methyltransferases.. Anal Bioanal Chem, 409 (15):(3767-3777). [PMID:28389916]
3.Niu Y et al.. (2017) Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis.. Sci Rep, 7 (46547). [PMID:28417976]
4.Kaniskan HÜ et al.. (2015) Selective inhibitors of protein methyltransferases.. J Med Chem, 58 (4):(1596-629). [PMID:25406853]
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