Homo-PROTAC cereblon degrader 1
Based on 1 publication(s) in Google Scholar
Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.
(Pink: Cereblon ligand (HY-10984); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W017440)).
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 2244520-98-5
- Formula: C32H32N6O10
- Molecular Weight:660.63
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
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HY-112588
dBET6
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HY-128845
PROTAC CRBN Degrader-1
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HY-123921
Gefitinib-based PROTAC 3
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HY-103597
Thalidomide-O-COOH
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HY-125845
(S,R,S)-AHPC
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HY-A0003
Lenalidomide
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HY-100947
VH-298
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HY-128600
ERD-308
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HY-101763A
(S,R,S)-AHPC monohydrochloride
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HY-100972
ARV-771
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HY-A0003R
Lenalidomide (Standard)
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HY-103596
Thalidomide-4-OH
Publications Citing Use of MedChemExpress (MCE) Homo-PROTAC cereblon degrader 1
MoreAll PROTACs Isoforms
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Biological Activity
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Cereblon |
Homo-PROTAC cereblon degrader 1 (0.1-1 μM, 0-72 h) inhibits Cereblon expression in MM1S cells and can gradually restore it[1].
Homo-PROTAC cereblon degrader 1 (0-1 μM, 16 h) inhibits Cereblon in the multiple myeloma cell lines U266, OPM-2, and RPMI-8226, as well as in the embryonic kidney cell line HEK293T, and the acute myeloid leukemia cell lines K562 and OCI-AML5[1].
Homo-PROTAC cereblon degrader 1 (0-10 μM, 4 days) slightly inhibits the cell viability of LP-1, KMS-27, and RPMI 8226[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM1S
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Concentration:1 μM; 100 nM; 100 nM
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Incubation Time:24 h; 0 min, 15 min, 30 min, 1 h, 3 h, 6 h, 24 h; 0, 4, 8, 24, 48, 72 h
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Result:Effectively inhibited Cereblon in a dose-dependent and time-dependent manner, had little effect on IKZF1 and IKZF3, and recovered after 24 hours.
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Cell Line:U266, OPM-2, RPMI-8226, HEK293T, K562, OCI-AML5
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Concentration:0, 0.1, 1 μM
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Incubation Time:16 h
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Result:Inhibited the expression of Cereblon.
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Cell Line:LP-1, KMS-27, RPMI 8226
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Concentration:0, 0.1, 1, 10 μM
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Incubation Time:4 days
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Result:Slightly inhibited cell viability.
Chemical Information
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CAS No. 2244520-98-5
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Appearance Solid
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Molecular Weight 660.63
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Formula C32H32N6O10
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Color Light yellow to yellow
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SMILES
O=C(N1C2CCC(NC2=O)=O)C3=CC=CC(NCCOCCOCCNC4=C5C(C(N(C6CCC(NC6=O)=O)C5=O)=O)=CC=C4)=C3C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Solvent & Solubility
DMSO : 200 mg/mL (302.74 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 (stored under nitrogen). 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 (stored under nitrogen). 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 (7.57 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 (stored under nitrogen)
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 (272 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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 (stored under nitrogen). 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 | 1.5137 mL | 7.5685 mL | 15.1371 mL | 37.8427 mL |
| 5 mM | 0.3027 mL | 1.5137 mL | 3.0274 mL | 7.5685 mL | |
| 10 mM | 0.1514 mL | 0.7569 mL | 1.5137 mL | 3.7843 mL | |
| 15 mM | 0.1009 mL | 0.5046 mL | 1.0091 mL | 2.5228 mL | |
| 20 mM | 0.0757 mL | 0.3784 mL | 0.7569 mL | 1.8921 mL | |
| 25 mM | 0.0605 mL | 0.3027 mL | 0.6055 mL | 1.5137 mL | |
| 30 mM | 0.0505 mL | 0.2523 mL | 0.5046 mL | 1.2614 mL | |
| 40 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9461 mL | |
| 50 mM | 0.0303 mL | 0.1514 mL | 0.3027 mL | 0.7569 mL | |
| 60 mM | 0.0252 mL | 0.1261 mL | 0.2523 mL | 0.6307 mL | |
| 80 mM | 0.0189 mL | 0.0946 mL | 0.1892 mL | 0.4730 mL | |
| 100 mM | 0.0151 mL | 0.0757 mL | 0.1514 mL | 0.3784 mL |
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