1. Epigenetics
  2. Epigenetic Reader Domain
  3. PFI-4

PFI-4 

Cat. No.: HY-18664 Purity: 98.24%
Handling Instructions

PFI-4 is a potent and selective and cell permeable BRPF1 bromodomain inhibitor (IC50 = 80 nM).

For research use only. We do not sell to patients.

PFI-4 Chemical Structure

PFI-4 Chemical Structure

CAS No. : 900305-37-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 380 In-stock
Estimated Time of Arrival: December 31
100 mg USD 680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

PFI-4 is a potent and selective and cell permeable BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. IC50 value: 80 nM Target: BRPF1 in vitro: Disrupts BRPF1 binding to histone H3.3. PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 with a Kd =13 nM as determined by ITC. It reduces recovery time in triple BRD cell construct in FRAP, inhibiting binding to tri-acetylated histone 4 (residues 1-21). It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 μM) and is selective for BRPF1 over BRPF2 and BRPF3. PFI-4 is potent in cells, with an IC50 value of 250 nM.

Molecular Weight

380.44

Formula

C₂₁H₂₄N₄O₃

CAS No.
SMILES

O=C(NC1=C(N2CCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC

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 : 26 mg/mL (68.34 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6285 mL 13.1427 mL 26.2854 mL
5 mM 0.5257 mL 2.6285 mL 5.2571 mL
10 mM 0.2629 mL 1.3143 mL 2.6285 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: ≥ 1 mg/mL (2.63 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1 mg/mL (2.63 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1 mg/mL (2.63 mM); Clear solution

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

PFI-4PFI4PFI 4Epigenetic Reader DomainInhibitorinhibitorinhibit

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PFI-4
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HY-18664
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