(R)-PFI 2 hydrochloride
Modify Date: 2024-01-02 19:27:59
(R)-PFI 2 hydrochloride structure
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Common Name | (R)-PFI 2 hydrochloride | ||
|---|---|---|---|---|
| CAS Number | 1627607-87-7 | Molecular Weight | 535.982 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H26ClF4N3O3S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of (R)-PFI 2 hydrochloridePFI-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]Target: 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). PFI-766 engagement of endogenous SETD7 was also confirmed by mass spectrometry that supported the high specificity of the compound for endogenous SETD7. |
| Name | PFI-2 |
|---|---|
| Synonym | More Synonyms |
| Description | 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]Target: 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). PFI-766 engagement of endogenous SETD7 was also confirmed by mass spectrometry that supported the high specificity of the compound for endogenous SETD7. |
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| Related Catalog | |
| References |
| Molecular Formula | C23H26ClF4N3O3S |
|---|---|
| Molecular Weight | 535.982 |
| Exact Mass | 535.131958 |
| Storage condition | -20℃ |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302 |
| Precautionary Statements | P301 + P312 + P330 |
| RIDADR | NONH for all modes of transport |
| 6-Isoquinolinesulfonamide, 8-fluoro-1,2,3,4-tetrahydro-N-[(1R)-2-oxo-2-(1-pyrrolidinyl)-1-[[3-(trifluoromethyl)phenyl]methyl]ethyl]-, hydrochloride (1:1) |
| MFCD28133380 |
| 8-Fluoro-N-{(2R)-1-oxo-1-(1-pyrrolidinyl)-3-[3-(trifluoromethyl)phenyl]-2-propanyl}-1,2,3,4-tetrahydro-6-isoquinolinesulfonamide hydrochloride (1:1) |
| (R)PFI-2 HCl |
| PFI-2 (hydrochloride) |