PFI-2
- CAS No.
- 1627676-59-8
- Chemical Name:
- PFI-2
- Synonyms
- PFI-2;CS-1808;PFI-2 HCl;R-PFI-2 HCl;PFI-2 USP/EP/BP;8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide;6-Isoquinolinesulfonamide, 8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-;(R)-8-fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide (R)-PFI 2 hydrochloride
- CBNumber:
- CB62729655
- Molecular Formula:
- C23H25F4N3O3S
- Molecular Weight:
- 499.52
- MDL Number:
- MFCD28348361
- MOL File:
- 1627676-59-8.mol
- MSDS File:
- SDS
SAFETY
Risk and Safety Statements
| Symbol(GHS) |    GHS05,GHS07,GHS09 |
|---|---|
| Signal word | Danger |
| Hazard statements | H302+H312-H315-H318-H411 |
| Precautionary statements | P264-P270-P273-P280-P301+P312+P330-P302+P352+P312-P305+P351+P338+P310-P332+P313-P391-P501 |
PFI-2 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TRC | P294055 | PFI-2 | 1627676-59-8 | 1mg | $55 | 2021-12-16 | Buy |
| Biorbyt Ltd | orb611667 | PFI-2 | 1627676-59-8 | 1g | $1802 | 2021-12-16 | Buy |
| ApexBio Technology | B4875 | PFI-2 | 1627676-59-8 | 25mg | $250 | 2021-12-16 | Buy |
| Biorbyt Ltd | orb611667 | PFI-2 | 1627676-59-8 | 100mg | $606.9 | 2021-12-16 | Buy |
| Medical Isotopes, Inc. | 61050 | PFI-2 | 1627676-59-8 | 25mg | $875 | 2021-12-16 | Buy |
PFI-2 Chemical Properties,Uses,Production
Uses
PFI-2 is a potent and selective lysine methyltransferase SETD7 inhibitor which is a crucial factor in many disease related pathways.
Biological Activity
pfi-2 is a potent and selective inhibitor of setd7 methyltransferase with ic50 value of 2.0 nm [1].set domain containing (lysine methyltransferase) 7 (setd7) is a protein lysine methyltransferase that acts as monomethyltransferase of lysine 4 on histone h3 (h3k4) and regulates dna methyltransferase 1 (dnmt1) [1].pfi-2 is a potent and selective setd7 methyltransferase inhibitor. (r)-pfi-2 inhibited human setd7 methyltransferase activity with ic50 value of 2.0 nm. however, (s)-pfi-2 was 500-fold less active with ic50 value of only 1.0 μm. (r)-pfi-2 potently inhibited setd7 with morrison kiapp value of 0.33 nm. (r)-pfi-2 occupied the peptide binding groove and effectively inhibited the binding of setd7 substrates. in the presence of 20 μm sam, (r)-pfi-2 bound to setd7 with kd value of 4.2 nm in a sam-dependent way. in hek293 cells, (r)-pfi-2 (10 μm) bound to and stabilized setd7. in setd7+/+ murine embryonic fibroblasts (mefs), (r)-pfi-2 increased nuclear localization of yes-associated protein (yap) and the expression of yap target genes ctgf, gli2 and cdc20 [1].
Enzyme inhibitor
This SETD7 inhibitor (FW = 499.52 g/mol; CAS 1627676-59-8; IUPAC: 8- fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3- (trifluoromethyl)phenyl]methyl]ethyl]-6-isoquinolinesulfonamide, targets the SET domain containing lysine methyltransferase, or SETD7 (Ki = 0.33 nM; IC50 = 2 nM), showing 1000-times selectivity versus other methyltransferases and other non-epigenetic targets. (R)-PFI-2 exhibits an unusual cofactor-dependent and substrate-competitive inhibitory mechanism by occupying the substrate peptide binding groove of SETD7, including the catalytic lysine-binding channel, and by making direct contact with the donor methyl group of the cofactor, S-adenosylmethionine. In murine embryonic fibroblasts, (R)-PFI-2 treatment phenocopies the effects of Setd7 deficiency on Hippo pathway signaling, via modulation of the transcriptional coactivator Yes-associated protein (YAP) and regulation of YAP target genes. In confluent MCF7 cells, (R)-PFI-2 rapidly alters YAP localization, suggesting continuous and dynamic regulation of YAP by the methyltransferase activity of SETD7.
References
[1]. barsyte-lovejoy d, li f, oudhoff mj, et al. (r)-pfi-2 is a potent and selective inhibitor of setd7 methyltransferase activity in cells. proc natl acad sci u s a, 2014, 111(35): 12853-12858.
PFI-2 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Shaanxi Dideu Medichem Co. Ltd | +86-29-87569265 +86-18612256290 | 1056@dideu.com | China | 3581 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29220 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2923 | 55 |
