1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Acetyltransferase
  3. PF-CBP1 hydrochloride

PF-CBP1 hydrochloride 

Cat. No.: HY-19999A Purity: 95.95%
Handling Instructions

PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1βIL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.

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

PF-CBP1 hydrochloride Chemical Structure

PF-CBP1 hydrochloride Chemical Structure

CAS No. : 2070014-93-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 69 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 69 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 75 In-stock
Estimated Time of Arrival: December 31
25 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1βIL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al[1].

IC50 & Target[1]

CREBBP

125 nM (IC50)

EP300

363 nM (IC50)

CBP

0.19 μM (Kd)

BRD4

20 μM (Kd)

In Vitro

ITC is the label-free technique for determining KD values, PF-CBP1 is against CBP (Kd=0.19 μM) and >105-fold selective over BRD4 (Kd>20 μM) by ITC[1].
PF-CBP1 displays greater than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins, it against BRD2-1,BRD3-1, BRD3-2,BRD4-1, BRD4-2, BRDT-1, TAF1-2, and TAF1L-2 with IC50 values of 1.24 μM, 1.38 μM, 4.22 μM, 1.54 μM, 9.75 μM, 2.44 μM, 3.39 μM and 7.29 μM, respectively[1].
PF-CBP1 (3-10 μM; pretreatment 30 mins; 4 hours) moderately reduces LPS-induced IL-6 and IFN-b expression in the J774 cell at 10 μM. And it decreases IL-1b expression evidently at 3 μM[1].
PF-CBP1 (100 nM-1000 nM;24 hours) significantly reduced RGS4 mRNA levels(49% reduction) relative to vehicle in cortical neuron cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

525.08

Formula

C₂₉H₃₇ClN₄O₃

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 : 100 mg/mL (190.45 mM; Need ultrasonic)

H2O : 1 mg/mL (1.90 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9045 mL 9.5224 mL 19.0447 mL
5 mM 0.3809 mL 1.9045 mL 3.8089 mL
10 mM 0.1904 mL 0.9522 mL 1.9045 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 (4.76 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PF-CBP1 hydrochloride
Cat. No.:
HY-19999A
Quantity:
MCE Japan Authorized Agent: