2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. dCBP-1

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.

For research use only. We do not sell to patients.

dCBP-1 Chemical Structure

dCBP-1 Chemical Structure

CAS No. : 2484739-25-3

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1 mg USD 119 In-stock
5 mg USD 250 In-stock
10 mg USD 420 In-stock
25 mg USD 920 In-stock
50 mg USD 1480 In-stock
100 mg USD 2370 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

dCBP-1 Related Antibodies

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Customer Validation

These results were obtained using AlphaLISA™ SureFire® Ultra™ assays

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target[1]

p300/CBP

 

Cereblon

 

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.

dCBP-1 Related Antibodies

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.
Molecular Weight

1028.11

Formula

C51H63F2N11O10
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-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)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9727 mL 4.8633 mL 9.7266 mL
5 mM 0.1945 mL 0.9727 mL 1.9453 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • 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.

    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.
  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.44%

SDS (393 KB)

COA (245 KB) HNMR (235 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
References

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
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dCBP-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

dCBP-12484739-25-3dCBP1dCBP 1PROTACsEpigenetic Reader Domainp300CBPCRBNheterobifunctionaldegradermultiplemyelomacellMYCInhibitorinhibitorinhibit

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