CPI-637
Based on 13 publication(s) in Google Scholar
CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.87%
- No. CAS: 1884712-47-3
- Fòrmula: C22H22N6O
- Peso molecular:386.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CPI-637
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Hemasphere. 2021 Jul 8;5(8):e610. [Abstract]
- J Exp Clin Cancer Res. 2024 Mar 5;43(1):69. [Abstract]
- Sci Adv. 2023 Oct 6;9(40):eadi8343. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- Oncogene. 2021 Apr;40(15):2711-2724. [Abstract]
- Cell Rep. 2021 Feb 16;34(7):108744. [Abstract]
- Chin Med. 2024 Mar 5;19(1):42. [Abstract]
- Front Cell Infect Microbiol. 2021 Jul 19:11:686035. [Abstract]
- Endocr Relat Cancer. 2020 Mar;27(3):187-198. [Abstract]
- Am J Pathol. 2021 Jun;191(6):1094-1107. [Abstract]
- bioRxiv. 2025 February 22.
- Patent. US20230255966A1.
Actividad biológica
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BRD4 BD1 11 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
3.13 μM
Compound: 2; CPI-637
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Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition by Celltiter-Glo assay
Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition by Celltiter-Glo assay
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[PMID: 34962793] |
| HEK293 | EC50 |
0.3 μM
Compound: 28; CPI-637
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Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter gene based BRET assay
Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter gene based BRET assay
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[PMID: 27190605] |
| LNCaP | IC50 |
0.65 μM
Compound: 2; CPI-637
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Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition by Celltiter-Glo assay
Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition by Celltiter-Glo assay
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[PMID: 34962793] |
| LNCaP C4-2B | IC50 |
3.35 μM
Compound: 2; CPI-637
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Antiproliferative activity against human LNCaP C4-2B cells assessed as inhibition of cell growth by Celltiter-Glo assay
Antiproliferative activity against human LNCaP C4-2B cells assessed as inhibition of cell growth by Celltiter-Glo assay
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[PMID: 34962793] |
CPI-637 (Compound 28) inhibits MYC expression in AMO-1 cells (EC50 value of 0.60 μM) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1884712-47-3
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Appearance Solid
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Peso molecular 386.45
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Fòrmula C22H22N6O
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Color White to off-white
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SMILES
O=C1NC2=CC=CC(C3=CC4=C(N(C)N=C4C5=CN(C)N=C5)C=C3)=C2N[C@H](C)C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Hemasphere
The Novel Oral BET-CBP/p300 Dual Inhibitor NEO2734 Is Highly Effective in Eradicating Acute Myeloid Leukemia Blasts and Stem/Progenitor Cells. [Abstract]2021 Jul 8;5(8):e610. PMID: 34258514 -
J Exp Clin Cancer Res
KLF7 regulates super-enhancer-driven IGF2BP2 overexpression to promote the progression of head and neck squamous cell carcinoma. [Abstract]2024 Mar 5;43(1):69. PMID: 38443991 -
Sci Adv
Deficient chaperone-mediated autophagy facilitates LPS-induced microglial activation via regulation of the p300/NF-κB/NLRP3 pathway. [Abstract]2023 Oct 6;9(40):eadi8343. PMID: 37801503 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Oncogene
2021 Apr;40(15):2711-2724. PMID: 33712705 -
Cell Rep
An acetyl-histone vulnerability in PI3K/AKT inhibition-resistant cancers is targetable by both BET and HDAC inhibitors. [Abstract]2021 Feb 16;34(7):108744. PMID: 33596421 -
Chin Med
Cayratia albifolia C.L.Li exerts anti-rheumatoid arthritis effect by inhibiting macrophage activation and neutrophil extracellular traps (NETs). [Abstract]2024 Mar 5;19(1):42. PMID: 38444022 -
Front Cell Infect Microbiol
CPI-637 as a Potential Bifunctional Latency-Reversing Agent That Targets Both the BRD4 and TIP60 Proteins. [Abstract]2021 Jul 19:11:686035. PMID: 34350133 -
Endocr Relat Cancer
2020 Mar;27(3):187-198. PMID: 31951590 -
Am J Pathol
MYC-Mediated Ribosomal Gene Expression Sensitizes Enzalutamide-resistant Prostate Cancer Cells to EP300/CREBBP Inhibitors. [Abstract]2021 Jun;191(6):1094-1107. PMID: 33705753 -
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Solvente y solubilidad
DMSO : 9.62 mg/mL (24.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.96 mg/mL (2.48 mM); Clear solution
This protocol yields a clear solution of ≥ 0.96 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.6 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.96 mg/mL (2.48 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.96 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.6 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5877 mL | 12.9383 mL | 25.8766 mL | 64.6914 mL |
| 5 mM | 0.5175 mL | 2.5877 mL | 5.1753 mL | 12.9383 mL | |
| 10 mM | 0.2588 mL | 1.2938 mL | 2.5877 mL | 6.4691 mL | |
| 15 mM | 0.1725 mL | 0.8626 mL | 1.7251 mL | 4.3128 mL | |
| 20 mM | 0.1294 mL | 0.6469 mL | 1.2938 mL | 3.2346 mL |
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