PROTAC CARM1 degrader-1
PROTAC CARM1 degrader-1 is a highly selective CARM1 PROTAC degrader, with a DC50 of 8.1 nM in MCF‑7 cells. PROTAC CARM1 degrader-1 recruits the VHL E3 ubiquitin ligase complex to act on CARM1, inducing a proteasome-dependent degradation process. PROTAC CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in breast cancer cells, inhibits breast cancer cell migration, and exhibits no significant inhibitory effect on cell proliferation. PROTAC CARM1 degrader-1 is applicable for related research on breast cancer.
(Pink: CARM1 ligand (HY-114965); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3032785-00-2
- Formula: C71H98N12O8S
- Molecular Weight:1279.68
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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
[1]|
PRMT4 8.1 nM (DC50) |
In Vitro
PROTAC CARM1 degrader-1 (Compound 3b) (0.01‑500 nM; 24 h) potently induces the degradation of CARM1 protein in MCF‑7 cells (DC50 = 8.1 nM, Dmax = 97%), and exhibits high selectivity over PRMT1, PRMT5, and PRMT6; moreover, the CARM1 degradation activity is abolished upon co-treatment with MG132 (HY-13259), MLN4924 (HY-70062), VH-032 (HY-120217) or TP-064 (HY-114965) [1].
PROTAC CARM1 degrader-1 (0.5 μM; 48 h) downregulates the asymmetric dimethylation modification of the CARM1 substrates BAF155 and PABP1 in MCF‑7 cells[1].
PROTAC CARM1 degrader-1 (0.5 μM; 20 h) exerts a significant migration inhibitory effect on MDA-MB-231 triple-negative breast cancer cells, with no apparent anti-proliferative activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:6.25, 12.5, 25, 50, 100, 500 nM (24 h)
0.5 μM (1-48 h) -
Incubation Time:24 h
0, 1, 2, 4, 8, 24, 48 h (0.5 μM) -
Result:Induced potent CARM1 protein degradation (DC50 = 8.1 nM, Dmax = 97%)；exhibited high selectivity, no obvious degradation for PRMT1, PRMT5, PRMT6.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5 μM
7.5 μM of MG132, 20 μM of VH-032, 2 μM of MLN4924, and 10 μM of TP-064 (cotreated) -
Incubation Time:24 h
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Result:Abolished the CARM1 degradation activity upon co‑treatment with MG132, MLN4924, VH‑032 or TP‑064.
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Cell Line:MDA-MB-231, BT474 cells
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Concentration:0.5 μM
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Incubation Time:48 h
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Result:Downregulated the asymmetric dimethylation modification of the CARM1 substrates BAF155 and PABP1 in MCF‑7 cells.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5 μM
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Incubation Time:7 days
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Result:Did not exert significant antiproliferative effect on MCF‑7 and MDA‑MB‑231 cells.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5 μM
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Incubation Time:20 h
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Result:Produced obvious migration‑inhibitory effect on MDA‑MB‑231 triple‑negative breast cancer cells.
Chemical Information
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CAS No. 3032785-00-2
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Molecular Weight 1279.68
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Formula C71H98N12O8S
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SMILES
O=C([C@H]1N(C([C@@H](NC(CN2CCN(CC3CCN(CC4CCN(C(COC5=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-1 Related Classifications
HY-156152 Related Classifications
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