PROTAC CARM1 degrader-2
PROTAC CARM1 degrader-2 is a selective PROTAC-based CARM1 degrader with a DC50 of 8.8 nM in breast cancer cells. PROTAC CARM1 degrader-2 mediates CARM1 protein degradation in a ubiquitin ligase- and proteasome-dependent manner, and reduces the methylation level of downstream substrates of CARM1. PROTAC CARM1 degrader-2 can be used in breast cancer-related research.
(Pink: CARM1 ligand (HY-114965); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3032785-06-8
- Formula: C72H100N12O7S
- Molecular Weight:1277.71
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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
Biological Activity
Description
IC50 & Target
DC50: 8.8 nM (CARM1)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | DC50 |
8.8 nM
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CARM1 degradation activity in human MCF7 breast cancer cells assessed by Western blot analysis of CARM1 protein levels following 24 h incubation.
CARM1 degradation activity in human MCF7 breast cancer cells assessed by Western blot analysis of CARM1 protein levels following 24 h incubation.
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37703322 |
In Vitro
PROTAC CARM1 degrader-2 (compound 3e) (6.25-500 nM; 24 h) potently degrades CARM1 in MCF7 human breast cancer cells with a DC50 of 8.8 nM and a Dmax of 98%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 human breast cancer cells
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Concentration:0.5 μM
6.25, 1.25, 25, 50, 100, 500 nM -
Incubation Time:24 h
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Result:Induced robust CARM1 degradation in MCF7 cells, comparable to the activity of the related degrader 3b.
Achieved potent CARM1 degradation activity with a DC50 of 8.8 nM and a maximum degradation (Dmax) of 98%.
Chemical Information
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CAS No. 3032785-06-8
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Molecular Weight 1277.71
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Formula C72H100N12O7S
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SMILES
O=C([C@H]1N(C([C@@H](NC(CN2CCN(CC3CCN(CC4CCN(C(CCC5=CC=C(OC6=CC=CC(C(N(C)CC7=CC(C8CCN(CCNC)CC8)=NC=C7)=O)=C6)C=C5)=O)CC4)CC3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C9=CC=C(C%10=C(C)N=CS%10)C=C9)C
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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)
PROTAC CARM1 degrader-2 Related Classifications
HY-156153 Related Classifications
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