1. Epigenetics
  2. Histone Methyltransferase
  3. PFI-2 hydrochloride

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

Cat. No.: HY-18627A Purity: 99.80%
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

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Solution
10 mM * 1 mL in DMSO USD 185 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Estimated Time of Arrival: December 31
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10 mg USD 168 In-stock
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50 mg USD 540 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of PFI-2 hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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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.

Molecular Weight

535.98

Formula

C₂₃H₂₆ClF₄N₃O₃S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (59.70 mM)

H2O : 5.56 mg/mL (10.37 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

  • 4.

    Add each solvent one by one:  PBS

    Solubility: 1 mg/mL (1.87 mM); Clear solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References

Purity: 99.80%

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