- PFI-2 hydrochloride
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- $15.00 / 1KG
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2021-07-13
- CAS:1627607-87-7
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
- PFI-2 hydrochloride
-
- $15.00 / 1KG
-
2021-07-09
- CAS:1627607-87-7
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
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| | PFI-2 (hydrochloride) Basic information |
| Product Name: | PFI-2 (hydrochloride) | | Synonyms: | 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 | | CAS: | 1627607-87-7 | | MF: | C23H26ClF4N3O3S | | MW: | 535.98 | | EINECS: | | | Product Categories: | API | | Mol File: | 1627607-87-7.mol |  |
| | PFI-2 (hydrochloride) Chemical Properties |
| 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. |
| | PFI-2 (hydrochloride) Usage And Synthesis |
| 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 | | storage | Store at -20°C | | References | 1)?Barsyte-Lovejoy?et al.?(2014),?(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells;?Proc. Natl. Acad. Sci. USA?111?12853 |
| | PFI-2 (hydrochloride) Preparation Products And Raw materials |
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