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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Epigenetics > (R)-PFI-2 HydrochlorideCAS：1627607-87-7
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 1627607-87-7 |
| Name | (R)-PFI-2 Hydrochloride |
| Molecular Formula | C23H25F4N3O3S·HCl |
| Molecular Weight | 535.98 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28133380 |
| SMILES | O=S(C1=CC2=C(CNCC2)C(F)=C1)(N[C@H](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)=O.[H]Cl |
| Target Point | SETD7 |
| Passage | Epigenetics |
| Background | PFI-2 is a potent, selective and cell-active inhibitor of lysine methyltransferase SETD7. |
| Biological Activity | PFI-2 hydrochloride is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2. IC50 value: 2 nM [1] |
| In Vitro | SETD7(R)-PFI-2 is highly selective(>1，000-fold)for SETD7，over a panel of 18 other human protein methyltransferases and DNMT1，and was shown to be inactive against 134 additional ion channel，GPCR，and enzyme targets(<35% inhibition at 10 μM).(R)-PFI-2 binds to SETD7 only in the presence of SAM. PFI-766，a biotinylated variant of(R)-PFI-2 that retains the ability to bind and inhibit SETD7(IC50 110 ± 26 nM in our in vitro enzymatic assay). [1] |
| Data Literature Source | [1]. Barsyte-Lovejoy D，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. |
| Unit | Bottle |
| Specification | 5mg 10mg |
PFI-2是一种强效的，有选择性和细胞活性的lysine methyltransferase SETD7抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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