dCBP-1
Based on 11 publication(s) in Google Scholar
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.
(Pink: CBP/p300 ligand (HY-138539); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-140193)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.37%
- No. CAS: 2484739-25-3
- Fòrmula: C51H63F2N11O10
- Peso molecular:1028.11
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Almacenamiento:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)
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
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Publications Citing Use of MedChemExpress (MCE) dCBP-1
More- Nat Immunol. 2024 Sep;25(9):1580-1592. [Abstract]
- Nat Genet. 2025 Oct;57(10):2468-2481. [Abstract]
- Mol Cell. 2025 Dec 18;85(24):4526-4544.e18. [Abstract]
- Adv Sci (Weinh). 2026 Mar 1:e17231. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Dec 30;122(52):e2516667122. [Abstract]
- Proc Natl Acad Sci U S A. 2024 Jun 25;121(26):e2405905121. [Abstract]
- Cancers (Basel). 2024 Jan 21;16(2):457. [Abstract]
- iScience. 2024 May 16;27(6):110011. [Abstract]
- bioRxiv. 2026 Jan 27:2026.01.26.701739. [Abstract]
- bioRxiv. 2026 Jan 29:2026.01.29.702555. [Abstract]
- bioRxiv. 2025 Sep 7.
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Actividad biológica
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p300/CBP |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RS4-11 | IC50 |
4.8 nM
Compound: dCBP-1
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Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
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[PMID: 37276143] |
| SK-HEP1 | IC50 |
>20 μM
Compound: dCBP-1
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Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 5 days by CCK-8 assay
Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 5 days by CCK-8 assay
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[PMID: 38316017] |
dCBP-1 (10-1000 nM; 6 hours) treatment shows near-complete degradation of p300/CBP in MM1S cells. dCBP-1 is also able to induce near-complete p300/CBP degradation across other multiple myeloma cell lines tested, including MM1R, KMS-12-BM, and KMS34[1].
Treatment of the human haploid cell line HAP1 for 6 h with dCBP-1 reveals almost complete loss of both CBP and p300 between 10 and 1000 nM doses. A time course analysis with 250 nM dCBP-1 revealed almost complete degradation of p300/CBP within an hour of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Multiple myeloma cell line MM1S
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Concentration:10 nM, 100 nM, 250 nM, 500 nM, 1000 nM
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Incubation Time:6 hours
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Result:Revealed rapid degradation with near-complete loss of p300/CBP after 2 hours.
Chemical Information
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No. CAS 2484739-25-3
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Appearance Solid
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Peso molecular 1028.11
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Fòrmula C51H63F2N11O10
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Color Light yellow to yellow
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SMILES
CNC(N(CC1)CC2=C1N(N=C2N3C(C=C(C(F)F)C(C4=CN(C)N=C4)=C5)=C5CCC3)C6CCN(C(CCOCCOCCOCCOCCNC7=CC8=C(C(N(C9C(NC(CC9)=O)=O)C8=O)=O)C=C7)=O)CC6)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)
Publications (11)
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Journal Impact Factor
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Most Recent
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Nat Immunol
2024 Sep;25(9):1580-1592. PMID: 39169234
dCBP-1 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2024 Sep;25(9):1580-1592. [Abstract]
Aire condensate volume quantification in 4D6 cells treated with DMSO, dCBP-1 (0.25 μM; 4 h). dCBP-1 significantly decreased Aire condensate size without affecting Aire expression levels.
dCBP-1 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2024 Sep;25(9):1580-1592. [Abstract]
Average Aire ChIP-seq profiles spanning super-enhancers and centered at Aire peaks within super-enhancers in 4D6 cells treated with DMSO, dCBP-1 (0.25 μM; 4 h). dCBP-1 impaired WT Aire binding to super-enhancers.
dCBP-1 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2024 Sep;25(9):1580-1592. [Abstract]
5′-ethynyl uridine quantitative PCR (5EU–qPCR) analysis of Aire transcriptional activity in 4D6 cells treated with dCBP-1 (0.25 μM; 4 h). dCBP-1 had a negative impact on transcription of Aire-bound loci.
dCBP-1 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2024 Sep;25(9):1580-1592. [Abstract]
Immunoblot analysis of Aire-FLAG-in 4D6 cells treated with dCBP-1 (0.25 μM; 4 h). dCBP-1 notably reduced the levels of both H3K27ac and CBP/p300.
dCBP-1 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2024 Sep;25(9):1580-1592. [Abstract]
Combined Aire-FLAG immunofluorescence and nascent RIC8A RNA-FISH imaging in 4D6 cells treated with dCBP-1 (0.25 μM; 4 h). The smaller condensates visible with dCBP-1 were transcriptionally inactive, as evidenced by the lack of nascent RNA-FISH foci of the Aire target gene, RIC8A.
dCBP-1 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2024 Sep;25(9):1580-1592. [Abstract]
Flow cytometric analysis of UAS-mKate2 expression versus GFP-P2A-Gal4DBD-CTT expression and their ratios in 4D6 cells treated with dCBP-1 (0.25 μM; 24 h). dCBP-1 decreased the AD reporter activity of Gal4DBD-CTT.
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Nat Genet
Targeting histone H2B acetylated enhanceosomes via p300/CBP degradation in prostate cancer. [Abstract]2025 Oct;57(10):2468-2481. PMID: 41044247 -
Mol Cell
NAT10 promotes cancer metastasis by modulating p300/CBP activity through chromatin-associated tRNA. [Abstract]2025 Dec 18;85(24):4526-4544.e18. PMID: 41344331 -
Adv Sci (Weinh)
BCR::ABL1-Induced Enhancer Reprogramming Uncovers Hypersensitivity of Ph+B-ALL Cells to Enhancer-Targeting Drugs. [Abstract]2026 Mar 1:e17231. PMID: 41764406 -
Proc Natl Acad Sci U S A
2025 Dec 30;122(52):e2516667122. PMID: 41439710 -
Proc Natl Acad Sci U S A
A MOZ-TIF2 leukemia mouse model displays KAT6-dependent H3K23 propionylation and overexpression of a set of active developmental genes. [Abstract]2024 Jun 25;121(26):e2405905121. PMID: 38889153 -
Cancers (Basel)
CIC-DUX4 Chromatin Profiling Reveals New Epigenetic Dependencies and Actionable Therapeutic Targets in CIC-Rearranged Sarcomas. [Abstract]2024 Jan 21;16(2):457. PMID: 38275898 -
iScience
Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. [Abstract]2024 May 16;27(6):110011. PMID: 38868181 -
bioRxiv
2026 Jan 27:2026.01.26.701739. PMID: 41659547 -
bioRxiv
Chromatin modifiers KMT2D, BAF, and p300 are required for de novo binding of transcription factors on enhancers. [Abstract]2026 Jan 29:2026.01.29.702555. PMID: 41659470 -
Solvente y solubilidad
DMSO : 50 mg/mL (48.63 mM; ultrasonic and warming and heat to 80°C; 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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (4.86 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)
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 (271 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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9727 mL | 4.8633 mL | 9.7266 mL | 24.3165 mL |
| 5 mM | 0.1945 mL | 0.9727 mL | 1.9453 mL | 4.8633 mL | |
| 10 mM | 0.0973 mL | 0.4863 mL | 0.9727 mL | 2.4316 mL | |
| 15 mM | 0.0648 mL | 0.3242 mL | 0.6484 mL | 1.6211 mL | |
| 20 mM | 0.0486 mL | 0.2432 mL | 0.4863 mL | 1.2158 mL | |
| 25 mM | 0.0389 mL | 0.1945 mL | 0.3891 mL | 0.9727 mL | |
| 30 mM | 0.0324 mL | 0.1621 mL | 0.3242 mL | 0.8105 mL | |
| 40 mM | 0.0243 mL | 0.1216 mL | 0.2432 mL | 0.6079 mL |
dCBP-1 Related Classifications
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