| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
PF‑CBP1 targets the bromodomain of CBP (CREBBP) and p300, inhibiting their recognition of acetyl‑lysine on histones; it has 139‑fold biochemical selectivity over BRD4 and >105‑fold by ITC. This inhibition disrupts transcriptional regulation of genes involved in inflammation and neuronal function.
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| ln Vitro |
Key inflammatory genes in primary macrophages are modulated by PF-CBP1. Parkinson's disease-related RGS4 in neurons is downregulated by PF-CBP1. In the biochemical tests, PF-CBP1 is 139-fold selective over BRD4, and by ITC, it is more than 105-fold selective. As has been shown for other CBP inhibitors, F-CBP1 is likewise a strong inhibitor of EP300[1].
In vitro, PF‑CBP1 modulates key inflammatory genes in primary macrophages and downregulates RGS4 in neurons. It is a strong inhibitor of EP300 and shows high selectivity for CBP/p300 over BET bromodomains, confirming its mechanism as a selective epigenetic modulator without affecting BRD4‑dependent transcription. |
| ln Vivo |
In vivo data are limited; however, its ability to modulate inflammatory gene expression and neuronal RGS4 suggests potential in inflammatory and neurological disease models. Further in vivo pharmacokinetic and efficacy studies are needed to confirm its therapeutic utility.
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| Enzyme Assay |
Cell‑free binding is measured by HTRF or AlphaScreen assays using recombinant CBP bromodomain and labelled acetyl‑lysine peptide; displacement by PF‑CBP1 is quantified to determine IC50. Selectivity is confirmed by similar assays against p300 and BRD4, and by isothermal titration calorimetry (ITC) for thermodynamic binding parameters.
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| Cell Assay |
Cell‑based assays use primary macrophages treated with PF‑CBP1 and stimulated with LPS; inflammatory gene mRNA levels are measured by qPCR. In neuronal cell lines, RGS4 expression is assessed. These assays confirm the compound’s ability to modulate target genes through bromodomain inhibition in a cellular context.
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| Animal Protocol |
In vivo animal studies are not extensively reported; however, given its in vitro effects, potential models include LPS‑induced inflammation and Parkinson’s disease models to evaluate RGS4 modulation. Dosing routes and PK/PD relationships require further investigation.
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| ADME/Pharmacokinetics |
PF‑CBP1 is a small molecule (MW 488.6, C₂₉H₃₆N₄O₃) with properties suitable for oral bioavailability. Detailed PK data (half‑life, clearance, bioavailability) are not publicly available. It is typically handled as a solid and soluble in DMSO for in vitro studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported; as a selective bromodomain inhibitor, potential off‑target effects on CBP/p300‑dependent cellular processes may occur. Safety profiling would be required before clinical development, including genotoxicity and organ toxicity assessments.
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| References |
Chem Biol.2015 Dec 17;22(12):1588-96.
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| Additional Infomation |
PF‑CBP1 is a research tool for studying CBP/p300 bromodomain function; it is not approved for clinical use. Its high selectivity makes it valuable for dissecting the role of CBP/p300 in inflammation and neurodegeneration, and it may serve as a lead for therapeutic development.
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| Exact Mass |
488.279
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|---|---|
| CAS # |
962928-21-7
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| Related CAS # |
PF-CBP1 hydrochloride;2070014-93-4
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| PubChem CID |
119081417
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
0
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
36
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| Complexity |
654
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCOC1=CC=C(C=C1)CCC2=NC3=C(N2CCN4CCOCC4)C=CC(=C3)C5=C(ON=C5C)C
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| InChi Key |
CGWBJJZOKGZCSJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H36N4O3/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
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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
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| Synonyms |
PF-06670910; PF 06670910; PF06670910; PF-CBP1; PF-CBP-1; PF-CBP 1.
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| HS Tariff Code |
2934.99.9001
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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