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

PF-CBP1 hydrochloride 

Cat. No.: HY-19999A Purity: 99.99%
COA 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-1β, IL-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

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Based on 1 publication(s) in Google Scholar

Other Forms of PF-CBP1 hydrochloride:

PF-CBP1 hydrochloride Related Antibodies

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1 Publications Citing Use of MCE PF-CBP1 hydrochloride

  • 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-1β, IL-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

.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].

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

PF-CBP1 hydrochloride Related Antibodies
Molecular Weight

525.08

Appearance

Solid

Formula

C29H37ClN4O3
CAS No.
SMILES

CCCOC1=CC=C(CCC2=NC3=CC(C4=C(C)ON=C4C)=CC=C3N2CCN5CCOCC5)C=C1.Cl[H]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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:  PBS

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

  • 2.

    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

  • 3.

    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

  • 4.

    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 available by MedChemExpress (MCE).
Purity & Documentation
References
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PF-CBP1 hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

PF-CBP12070014-93-4Epigenetic Reader DomainHistone AcetyltransferaseHATsHATRGS4neurological disorderparkinson's diseaseepilepsycorticalneuroninflammatoryInhibitorinhibitorinhibit

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