ChemicalBook > CAS DataBase List > PFI-2 (hydrochloride)

PFI-2 (hydrochloride)

Product Name: PFI-2 (hydrochloride)
CAS No.: 1627607-87-7
Chemical Name: PFI-2 (hydrochloride)
Synonyms: (R)-PFI-2;PFI-2 HCl salt;PFI-2 HCl ，S7294;PFI-2 (hydrochloride);(R)-PFI-2 (hydrochloride);PFI-2; PFI2;PFI 2;R PFI-2;R-PFI2;PFI-2 hydrochloride, 10 mM in DMSO;(1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide hydrochloride;(R)-8-Fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide hydrochloride;macrophage,chronic kidney disease,inhibit,Histone Methyltransferase,PFI-2,Inhibitor,SET domain containing lysine methyltransferase 7 (SETD7),PFI2 hydrochloride,renal fibrosis,inflammation,PFI 2,PFI2,PFI 2 hydrochloride
CBNumber: CB83041444
Molecular Formula: C23H26ClF4N3O3S
Formula Weight: 535.98
MOL File: 1627607-87-7.mol

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PFI-2 (hydrochloride) Property

Melting point:: >209°C (dec.)
storage temp.: 2-8°C
solubility: Soluble in DMSO (up to at least 25 mg/ml)
form: powder
color: white to beige
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
InChIKey: ZADKZNVAJGEFLC-GKNLIIIVNA-N
SMILES: FC1C=C(S(=O)(=O)N[C@@H](C(N2CCCC2)=O)CC2C=CC=C(C(F)(F)F)C=2)C=C2CCNCC=12.Cl |&1:8,r|

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Warning
Hazard statements: H302Harmful if swallowed

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1408
Product name: (R)-PFI-2
Purity: ≥97% (HPLC)
Packaging: 5mg
Price: $202
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML1408
Product name: (R)-PFI-2
Purity: ≥97% (HPLC)
Packaging: 25mg
Price: $791
Updated: 2025/07/31

Cayman Chemical

Product number: 14678
Product name: (R)-PFI-2 (hydrochloride)
Purity: ≥95%
Packaging: 1mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 14678
Product name: (R)-PFI-2 (hydrochloride)
Purity: ≥95%
Packaging: 5mg
Price: $179
Updated: 2024/03/01

Cayman Chemical

Product number: 14678
Product name: (R)-PFI-2 (hydrochloride)
Purity: ≥95%
Packaging: 10mg
Price: $330
Updated: 2024/03/01

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PFI-2 (hydrochloride) Chemical Properties,Usage,Production

Description

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. (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. Its enantiomer, (S)-PFI-2 , is 500-fold less active (IC₅₀ = 1 μM). See the Structural Genomics Consortium (SGC) website for more information.

Uses

(1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide Hydrochloride known as (-)-PFI-2 HCl is a cell permeable inhibitor of SET Domain-Containing protein 7/9 (SET 7/9) which plays a role in tumorigenesis in cell cancer lines.

Biochem/physiol Actions

(R)-PFI-2 is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (also known as SET9). (R)-PFI-2 has an IC50 value of 2 nM and 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. For full characterization details, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.(S)-PFI-2, an enantiomer of (R)-PFI-2, is used as a negative control. (S)-PFI-2 is available from Sigma. To learn more about and purchase (S)-PFI-2, click here.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

in vivo

PFI-2 hydrochloride (i.p., 200 μM, twice a week) attenuates the progression of renal fibrosis and preserves renal function in FA nephropathy^[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced ECM accumulation and fibroblasts activation after FA injury^[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) impeded Th2 cytokine signaling activation and M2 macrophage polarization^[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed M2 macrophages-myofibroblasts transition and myeloid myofibroblasts accumulation in the FA-treated kidneys^[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) attenuated macrophages M2 polarization and M2 macrophages-to-myofibroblasts transition in obstructed kidneys^[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed myeloid myofibroblast accumulation and renal fibrosis after UUO injury^[2].
PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced the infiltration of inflammatory cells, the production of inflammatory molecules, and NF-κB activation in FA nephropathy^[2].

Animal Model:	Male C57BL/6 mice (8-10-week old, 20-25 g)^[2]
Dosage:	200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL)
Administration:	intraperitoneal injection, twice a week
Result:	Presented less bone marrow-derived myofibroblasts, fewer CD206+/α-smooth muscle actin + cells and developed less renal fibrosis (P<0.01). Reduced the infiltration of inflammatory cells and decreased the production of pro-inflammatory cytokines and chemokines in the kidneys after folic acid treatment (P<0.01). Suppressed the accumulation of NF-κB p65+ cells in folic acid nephropathy (P<0.01).

IC 50

SETD7/KMT7

storage

Store at -20°C

References

[1] DALIA BARSYTE-LOVEJOY. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2014, 111 35: 12853-12858. DOI:10.1073/pnas.1407358111

PFI-2 (hydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from PFI-2 (hydrochloride) manufacturers

Zhuozhou Wenxi import and Export Co., Ltd

Product: PFI-2 hydrochloride 1627607-87-7
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-10

Zhuozhou Wenxi import and Export Co., Ltd

Product: PFI-2 hydrochloride 1627607-87-7
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-08

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PFI-2 (hydrochloride)

PFI-2 HCl salt

(R)-PFI-2 (hydrochloride)

(R)-PFI-2

PFI-2; PFI2;PFI 2;R PFI-2;R-PFI2

(1R)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide hydrochloride

(R)-8-Fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide hydrochloride

macrophage,chronic kidney disease,inhibit,Histone Methyltransferase,PFI-2,Inhibitor,SET domain containing lysine methyltransferase 7 (SETD7),PFI2 hydrochloride,renal fibrosis,inflammation,PFI 2,PFI2,PFI 2 hydrochloride

PFI-2 hydrochloride, 10 mM in DMSO

PFI-2 HCl ，S7294

1627607-87-7

C23H25F4N3O3SHCl

C23H26ClF4N3O3S

API