(S)-PFI-2 (hydrochloride)
- CAS No.
- 1627607-88-8
- Chemical Name:
- (S)-PFI-2 (hydrochloride)
- Synonyms
- (S)-PFI-2;(S)-PFI-2 HCl;(S)-PFI-2 (hydrochloride);PFI2;PFI-2;SPFI2;SPFI-2;PFI 2;SPFI 2;S-PFI-2;(1S)-1-[[3-(Trifluoromethyl)phenyl]methyl]-2-oxo-2-(1-pyrrolidinyl)ethyl]1,2,3,4-tetrahydro-6-isoquinolinesulfonamide hydrochloride
- CBNumber:
- CB73152426
- Molecular Formula:
- C23H26ClF4N3O3S
- Molecular Weight:
- 535.98
- MDL Number:
- MFCD29917834
- MOL File:
- 1627607-88-8.mol
(S)-PFI-2 (hydrochloride) price More Price(9)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | PZ0312 | (S)-PFI-2 | 1627607-88-8 | 5MG | $105 | 2023-06-20 | Buy |
Sigma-Aldrich | PZ0312 | (S)-PFI-2 | 1627607-88-8 | 25MG | $339 | 2023-06-20 | Buy |
Cayman Chemical | 18119 | (S)-PFI-2 (hydrochloride) ≥95% | 1627607-88-8 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 18119 | (S)-PFI-2 (hydrochloride) ≥95% | 1627607-88-8 | 5mg | $93 | 2024-03-01 | Buy |
Cayman Chemical | 18119 | (S)-PFI-2 (hydrochloride) ≥95% | 1627607-88-8 | 10mg | $169 | 2024-03-01 | Buy |
(S)-PFI-2 (hydrochloride) Chemical Properties,Uses,Production
Uses
(S)-PFI-2 is n analog of (R)-PFI-2 a potent and selective lysine methyltransferase SETD7 inhibitor which is a crucial factor in many disease related pathways.
General Description
(S)-PFI-2 is a negative control enantiomer and a biotinylated derivative of (R)-PFI-2, which helps to study the biological activity of SETD7 (SET domain containing (lysine methyltransferase) 7).
Biological Activity
(s)-pfi-2 (hydrochloride) is the inactive enantiomer of (r)-pfi-2 and may serve as a negative control. (r)-pfi-2 is a cell-permeable and potent set7/9 inhibitor with ic50 value of 2 nm [1].protein methyltransferases involve in the epigenetic regulation of gene transcription, silencing, chromatin structure establishment, maintenance, dna repair, and replication. set domain containing (lysine methyltransferase) 7 (setd7) (set9; set7/9, kmt7) is a protein lysine methyltransferases and is originally characterized as a monomethyltransferase of lysine 4 on histone h3 (h3k4me1). set7/9 has very broad target specificity that methylates histone h3, tumor suppressor p53 and transcription factor taf10 [1][2][3].(s)-pfi-2 (hydrochloride), the inactive enantiomer of (r)-pfi-2, was 500-fold less potent with ic50 value of 1 μm and used as a negative control in chemical biology experiments. (r)-pfi-2 is a potent and selective inhibitor of setd7 methyltransferase with ic50 value of 2 nm. in high-density mcf7 cells, (r)-pfi-2 dose-dependently increased nuclear yap and enhanced expression of the yap target genes areg and cyr61, whereas (s)-pfi-2 had no effect [1].
Biochem/physiol Actions
(S)-PFI-2 is the negative control probe for (R)-PFI-2 hydrochloride, which is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (SET9). (R)-PFI-2 has 1000-fold selectivity for SETD7 (SET9) over other methyltransferases and other non-epigenetic targets and an IC50 value of 2 nM. (S)-PFI-2 is 500-fold less active. For characterization details of (R)-PFI-2 and (S)-PFI-2, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.(R)-PFI-2, the active SETD7 probe, is available from Sigma. To learn more about and purchase (R)-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 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 sep 2;111(35):12853-8.
[2]. kurash jk, lei h, shen q, et al. methylation of p53 by set7/9 mediates p53 acetylation and activity in vivo. mol cell. 2008 feb 15;29(3):392-400.
[3]. couture jf, collazo e, hauk g, et al. structural basis for the methylation site specificity of set7/9. nat struct mol biol. 2006 feb;13(2):140-6.
(S)-PFI-2 (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
(S)-PFI-2 (hydrochloride) Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 14059 | 65 |
Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51471 | 80 |
DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |
Absin Bioscience Inc. | 021-38015121 15000105423 | chenjw@absin.cn | China | 24734 | 58 |
Energy Chemical | 021-58432009 400-005-6266 | marketing1@energy-chemical.com | China | 44894 | 58 |
MedBioPharmaceutical Technology Inc | 021-69568360 18916172912 | order@med-bio.cn | China | 8141 | 58 |
Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 4030 | 58 |