PROTAC CBP/P300 Degrader-1
Based on 2 publication(s) in Google Scholar
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.
(Pink: CBP/p300 ligand (HY-138539); Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 2484739-48-0
- Formula: C46H53F2N11O6
- Molecular Weight:893.98
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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)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PROTAC CBP/P300 Degrader-1
MoreAll PROTACs Isoforms
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Biological Activity
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Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
0.4 nM
Compound: P-034
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Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability by CellTitre-Glo assay
Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability by CellTitre-Glo assay
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[PMID: 35978697] |
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.
Chemical Information
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CAS No. 2484739-48-0
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Appearance Solid
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Molecular Weight 893.98
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Formula C46H53F2N11O6
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Color Light yellow to green yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell
2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746 -
bioRxiv
High-throughput affinity measurements of direct interactions between activation domains and co-activators. [Abstract]2024 Aug 20:2024.08.19.608698. PMID: 39229005
Solvent & Solubility
DMSO : 100 mg/mL (111.86 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, 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.
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.
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: ≥ 5 mg/mL (5.59 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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, 6 months; -20°C, 1 month (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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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, 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 |
PROTAC CBP/P300 Degrader-1 Related Classifications
HY-138536 Related Classifications
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