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Products Details
Product Description
– PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC50  value of 1.0  μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis[1][2].
Web ID
– HY-18627
Shipping
– Room temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C23H25F4N3O3S
Citations
– Acta Pharmacol Sin. 2021 Apr 13.|Biochem Pharmacol. 2023 Dec 2:115964.|Med Oncol. 2023 Apr 12;40(5):146.|Patent. US20180263995A1.|Sci Adv. 2023 May 26;9(21):eade4186.|Sci Total Environ. 2022 Dec 5;861:160682.|Int J Mol Med. 2021 Dec;48(6):210.|Mol Carcinog. 2023 May 5.|Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. |Research Square Print. September 20th, 2022.
References
– [1]Yuzhen Niu, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547.|[2]Benquan Liu, et al. Pharmacological inhibition of SETD7 by PFI-2 attenuates renal fibrosis following folic acid and obstruction injury. Eur J Pharmacol. 2021 Jun 15;901:174097.
CAS Number
– 1627676-59-8
Molecular Weight
– 499.52
SMILES
– O=S(C1=CC2=C(CNCC2)C(F)=C1)(N[C@H](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)=O
Clinical Information
– No Development Reported
Research Area
– Cancer; Infection; Inflammation/Immunology
Solubility
– 10 mM in DMSO
Target
– Histone Methyltransferase
Isoform
– SETD7/KMT7
Pathway
– Epigenetics
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
