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  3. PROTAC CBP/P300 Degrader-1

PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines.

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

PROTAC CBP/P300 Degrader-1 Chemical Structure

PROTAC CBP/P300 Degrader-1 Chemical Structure

CAS No. : 2484739-48-0

Size Price Stock Quantity
1 mg USD 477 In-stock
5 mg USD 1050 In-stock
10 mg USD 1650 In-stock
25 mg USD 3300 In-stock
50 mg USD 5300 In-stock
100 mg USD 8500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PROTAC CBP/P300 Degrader-1

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines[1].

IC50 & Target[1]

Cereblon

 

In Vitro

PROTAC CBP/P300 Degrader-1 shows LNCaP prostate cancer cell viability inhibition (IC50=0.4 nM). PROTAC CBP/P300 Degrader-1 (10 nM) induces degradation of P300 (≥ 80%)[1].
PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancel cell lines (IC50s ranging from 0.1-141.4 nM for HEL, NOMO-1, MOLM-13, HL-60, MEG-01, MM.IS, MM.1R, NCL-H929, RPM-8226, AMO-1, WSU-DLCL2, Karpas-422, Pfeiffer, SU-DHL-1, LNCap clone FGC, VCap; 22RV1, NCI-H520, NCI-H703, LK-2, MCE-7, and SK-BR-3 cells)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

893.98

Formula

C46H53F2N11O6

CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(N1CC2=C(CC1)N(C(CC3)CCN3C(CCCCCNC4=C(C(N5C(CCC6=O)C(N6)=O)=O)C(C5=O)=CC=C4)=O)N=C2N7C8=CC(C(F)F)=C(C(C=N9)=CN9C)C=C8CCC7)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 173.33 mg/mL (193.89 mM; Need ultrasonic; 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 1.1186 mL 5.5930 mL 11.1859 mL
5 mM 0.2237 mL 1.1186 mL 2.2372 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 6.5 mg/mL (7.27 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 6.5 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 (65.0 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, 6 months; -20°C, 1 month (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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1186 mL 5.5930 mL 11.1859 mL 27.9648 mL
5 mM 0.2237 mL 1.1186 mL 2.2372 mL 5.5930 mL
10 mM 0.1119 mL 0.5593 mL 1.1186 mL 2.7965 mL
15 mM 0.0746 mL 0.3729 mL 0.7457 mL 1.8643 mL
20 mM 0.0559 mL 0.2796 mL 0.5593 mL 1.3982 mL
25 mM 0.0447 mL 0.2237 mL 0.4474 mL 1.1186 mL
30 mM 0.0373 mL 0.1864 mL 0.3729 mL 0.9322 mL
40 mM 0.0280 mL 0.1398 mL 0.2796 mL 0.6991 mL
50 mM 0.0224 mL 0.1119 mL 0.2237 mL 0.5593 mL
60 mM 0.0186 mL 0.0932 mL 0.1864 mL 0.4661 mL
80 mM 0.0140 mL 0.0699 mL 0.1398 mL 0.3496 mL
100 mM 0.0112 mL 0.0559 mL 0.1119 mL 0.2796 mL
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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.

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Product Name:
PROTAC CBP/P300 Degrader-1
Cat. No.:
HY-138536
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