1. Epigenetics
  2. Histone Methyltransferase

PFI-2 hydrochloride (Synonyms: (R)-PFI-2 hydrochloride)

Cat. No.: HY-18627A Purity: 98.60%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
PFI-2 hydrochloride Chemical Structure

PFI-2 hydrochloride Chemical Structure

CAS No. : 1627607-87-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO $154 In-stock
10 mg $140 In-stock
50 mg $450 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Other Forms of PFI-2 hydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.8657 mL 9.3287 mL 18.6574 mL
5 mM 0.3731 mL 1.8657 mL 3.7315 mL
10 mM 0.1866 mL 0.9329 mL 1.8657 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

535.98

Formula

C₂₃H₂₆ClF₄N₃O₃S

CAS No.

1627607-87-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 32 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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PFI-2 hydrochloride
Cat. No.:
HY-18627A
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