Art. -Nr.: HY-134582

dCBP-1

11 Cited Publications

Kundenbewertung

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)).

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Reinheit: 99.37%
CAS. Nr.: 2484739-25-3
Formel: C₅₁H₆₃F₂N₁₁O₁₀
Molecular Weight:1028.11

Speicherung:

-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)

dCBP-1 Chemical Structure

CAS. Nr.: 2484739-25-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: CBP/p300 ligand (HY-138539); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-140193)).

IC₅₀ & Target^[1]

p300/CBP

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
RS4-11	IC₅₀	4.8 nM Compound: dCBP-1	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	[PMID: 37276143]
SK-HEP1	IC₅₀	>20 μM Compound: dCBP-1	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	[PMID: 38316017]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

Multiple myeloma cell line MM1S
Concentration:

10 nM, 100 nM, 250 nM, 500 nM, 1000 nM
Incubation Time:

6 hours
Result:

Revealed rapid degradation with near-complete loss of p300/CBP after 2 hours.

Chemical Information

CAS. Nr. 2484739-25-3
Appearance Solid
Molecular Weight 1028.11
Formel C₅₁H₆₃F₂N₁₁O₁₀
Color Light yellow to yellow
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-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)

All IFOthersRT-PCRWBCell Imaging/StainingFlow Cytometry

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Journal Impact Factor

Nat Immunol

Mechanism for controlled assembly of transcriptional condensates by Aire. [Abstract]

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.
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

Pharmacologic reversion of Merkel cell carcinoma via CBP/p300 inhibition. [Abstract]

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

BAF complex-independent gene activation by SS18::SSX. [Abstract]

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
bioRxiv

2025 Sep 7.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9727 mL

4.8633 mL

9.7266 mL

5 mM

0.1945 mL

0.9727 mL

1.9453 mL

10 mM

0.0973 mL

0.4863 mL

0.9727 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Raghu Vannam, et al. Targeted degradation of the enhancer lysine acetyltransferases CBP and p300. Cell Chem Biol. 2020 Dec 31;S2451-9456(20)30513-4. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

dCBP-1

11 Cited Publications

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dCBP-1

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) dCBP-1

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dCBP-1

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) dCBP-1

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

dCBP-1 Related Classifications

HY-134582 Related Classifications