Pomalidomide-NH-PEG6-amide-C2-CPI-1612
Pomalidomide-NH-PEG6-amide-C2-CPI-1612 is a CBP/EP300 PROTAC degrader with a DC50 value of 1.3 μM. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 mediates the formation of a ternary complex between CRBN and the core of CBP, with an EC50 of 1.2 μM. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 inhibits cancer cell growth and exhibits cell line-specific degradation activity. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 can be used in research related to multiple myeloma and leukemia.
(Pink: CBP/EP300 ligand (HY-175898); Blue: Cereblon ligand (HY-41547); Black: linker (HY-140231)).
For research use only. We do not sell to patients.
- Formula: C57H68N10O12
- Molecular Weight:1085.21
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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CBP/p300 1.3 nM (DC50) |
Cereblon |
Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (Compound dCE-1) (0.1-10 μM; 6 h) mediates the formation of a ternary complex between CRBN and the core of CBP in HEK293T cells, with an EC50 of 1.2 μM[1].
Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (0-5 μM; 4-48 h) induces proteasome-dependent, target-specific degradation of CBP and EP300 in LP1 cells, with a CBP DC50 of 1.3 μM, and achieves maximal degradation of CBP within 8 h[1].
Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (5 μM; 16 h) degrades CBP and EP300 in MM1S cells[1].
Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (10 μM) inhibits the growth of various human cancer cell lines, with the strongest activity against leukemia cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM1S multiple myeloma cells
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Concentration:5 μM
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Incubation Time:16 h
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Result:Reduced remaining CBP protein levels to ~30% of DMSO-treated controls.
Reduced remaining EP300 protein levels to ~60% of DMSO-treated controls.
Chemical Information
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Molecular Weight 1085.21
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Formula C57H68N10O12
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SMILES
O=C(N(C(C(N1)=O)CCC1=O)C2=O)C3=C2C(NCCOCCOCCOCCOCCOCCOCCNC(CCCN4N=CC(C5=CC=C(NC([C@@H](C6=CC=CC=C6)NC[C@@H](C)C7=CC=C(C#N)C=C7)=O)N=C5)=C4)=O)=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pomalidomide-NH-PEG6-amide-C2-CPI-1612 Related Classifications
HY-161250 Related Classifications
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