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
- MOL File:
- 1627676-59-8.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/5/21 10:59:17
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 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.
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.
PFI-2 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32760 | 60 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | United States | 19892 | 58 | Inquiry |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 26216 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
| Aladdin Scientific | +1-+1(833)-552-7181 | United States | 52927 | 58 | Inquiry |
| Amadis Chemical Company Limited | 571-89925085 | China | 131980 | 58 | Inquiry |
| Taizhou Crene Biotechnology Co. Ltd. | 0576-88813233 13396860566 | China | 1998 | 58 | Inquiry |
| Twochem Co.Ltd. | 021-58111628 15800915896 | China | 1790 | 58 | Inquiry |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4197 | 55 | Inquiry |
| Selleck Chemicals | 021-68591985 | China | 2543 | 65 | Inquiry |
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