Name | PFI-2 hydrochloride |
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. |
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). |
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), Sonication is recommended. Ethanol : 10 mg/mL (18.66 mM), Sonication is recommended.
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Keywords | SETD7 | SET domain containing lysine methyltransferase 7 (SETD7) | renal fibrosis | PFI-2 Hydrochloride | PFI2 Hydrochloride | PFI2 hydrochloride | PFI-2 | PFI2 | PFI 2 hydrochloride | PFI 2 Hydrochloride | PFI 2 | macrophage | Inhibitor | inhibit | inflammation | HistoneMethyltransferase | Histone Methyltransferase | chronic kidney disease |
Inhibitors Related | MAK-683 hydrochloride | BIX-01294 trihydrochloride | ORIC-944 | Tazemetostat | Piribedil | XY1 | MAK683 | EPZ015666 | iso-Azalansta | AMI-1 free acid | MS37452 | MRTX-1719 |
Related Compound Libraries | Highly Selective Inhibitor Library | Methylation Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Chromatin Modification Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-COVID-19 Compound Library |