[CAS NO. 2070014-93-4] PF-CBP1hydrochloride
PRODUCTS SPECIFICATIONS [2070014-93-4]
DESCRIPTION [2070014-93-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 525.08 |
| Molecular Formula | C29H37ClN4O3 |
| SMILES | CCCOC1=CC=C(CCC2=NC3=CC(C4=C(C)ON=C4C)=CC=C3N2CCN5CCOCC5)C=C1.Cl[H] |
1 Publications Citing Use of MCE
Summary
PF-CBP1 hydrochloride is a highly selective inhibitor of the
CREB binding protein bromodomain (CBP BRD)
. PF-CBP1 inhibits
CREBBP
and
EP300 bromodomains
with
IC
50
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
|
CREBBP 125 nM (IC 50 ) |
EP300 363 nM (IC 50 ) |
CBP .19 μM (Kd) |
BRD4 20 μM (Kd) |
In Vitro
ITC is the label-free technique for determining K
D
values, PF-CBP1 is against CBP (K
d
=0.19 μM) and >105-fold selective over BRD4 (K
d
>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 IC
50
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.
Appearance
Solid
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
DMSO : 100 mg/mL ( 190.45 mM ; Need ultrasonic)
H 2 O : 1 mg/mL ( 1.90 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (190.45 mM); Clear solution; Need ultrasonic
-
2.
-
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