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Purity: ≥98%
PF-CBP1 HCl (also known as PF-06670910 HCl) is a novel, potent and highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). Bromodomains are involved in transcriptional regulation through the recognition of acetyl lysine modifications on diverse proteins. Selective pharmacological modulators of bromodomains are lacking, although the largely hydrophobic nature of the pocket makes these modules attractive targets for small-molecule inhibitors. PF-CBP1 downregulated a number of inflammatory genes in macrophages that were not affected by a selective BET bromodomain inhibitor. In addition, the CBP bromodomain inhibitor modulated the mRNA level of the regulator of G-protein signaling 4 (RGS4) gene in neurons, suggesting a potential therapeutic opportunity for CBP inhibitors in the treatment of neurological disorders.
| ln Vitro |
ITC is a label-free method for calculating KD values; it is more than 105 times more selective than BRD4 (Kd>20 μM) and PF-CBP1 targets CBP (Kd=0.19 μM) [1]. In comparison to BRD4 and a panel of other proteins (for BRD2-1, BRD3-1, BRD3-2, BRD4-1, BRD4-2, BRDT-), PF-CBP1 is 100 times more selective for the CBP bromodomain [1]. The IC50 values for the aforementioned proteins, TAF1-2 and TAF1L-2, are 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. LPS-induced IL-6 and IFN-b production in J774 cells was moderately inhibited by PF-CBP1 at 10 μM (3-10 μM; 30 min pretreatment; 4 Hours). Significant reduction in IL-1b expression occurs when the concentration reaches 3 μM [1]. PF-CBP1 (100 nM-1000 nM; 24 hours) dramatically lowers (by 49%) the levels of RGS4 mRNA in cortical neuronal cells in comparison to vehicle [1].
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| References |
[1]. Chekler EL, et al. Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities. Chem Biol. 2015 Dec 17;22(12):1588-96.
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| Molecular Formula |
C29H37CLN4O3
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|---|---|
| Molecular Weight |
525.082086324692
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| CAS # |
2070014-93-4
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| Related CAS # |
PF-CBP1;1962928-21-7
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| SMILES |
CCCOC1=CC=C(C=C1)CCC2=NC3=CC(C4=C(C)ON=C4C)=CC=C3N2CCN5CCOCC5.[H]Cl
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| InChi Key |
HFOZCHHWLMTUTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H36N4O3.ClH/c1-4-17-35-25-9-5-23(6-10-25)7-12-28-30-26-20-24(29-21(2)31-36-22(29)3)8-11-27(26)33(28)14-13-32-15-18-34-19-16-32;/h5-6,8-11,20H,4,7,12-19H2,1-3H3;1H
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| Chemical Name |
4-(2-(5-(3,5-Dimethylisoxazol-4-yl)-2-(4-propoxyphenethyl)-1H-benzo[d]imidazol-1-yl)ethyl)morpholine hydrochloride
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| Synonyms |
PF-06670910; PF 06670910; PF06670910; PF-CBP1 HCl; PF-CBP1; hydrochloride; PF-CBP1; PF-CBP-1; PF-CBP 1;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~190.45 mM)
H2O : ~1 mg/mL (~1.90 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (190.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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