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PFI-2 hydrochloride ((R)-PFI-2 hydrochloride) is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-PFI-2.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
2 mg | $47 | In Stock | |
5 mg | $77 | In Stock | |
10 mg | $119 | In Stock | |
25 mg | $223 | In Stock | |
50 mg | $397 | In Stock | |
100 mg | $582 | In Stock | |
500 mg | $1,230 | In Stock | |
1 mL x 10 mM (in DMSO) | $130 | In Stock |
Description | PFI-2 hydrochloride ((R)-PFI-2 hydrochloride) is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-PFI-2. |
Targets&IC50 | SETD7:2 nM |
In vitro | (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). |
Alias | PFI-2 HCl, (R)-PFI-2 hydrochloride |
Molecular Weight | 535.98 |
Formula | C23H26ClF4N3O3S |
Cas No. | 1627607-87-7 |
Smiles | Cl.Fc1cc(cc2CCNCc12)S(=O)(=O)N[C@H](Cc1cccc(c1)C(F)(F)F)C(=O)N1CCCC1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (102.62 mM) Ethanol: 10 mg/mL | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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