PROTAC CARM1 degrader-1 hydrochloride
Based on 1 Customer Validation
PROTAC CARM1 degrader-1 hydrochloride is a highly selective CARM1 PROTAC degrader, with a DC50 of 8.1 nM in MCF‑7 cells. PROTAC CARM1 degrader-1 hydrochloride recruits the VHL E3 ubiquitin ligase complex to act on CARM1, inducing a proteasome-dependent degradation process. PROTAC CARM1 degrader-1 hydrochloride 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 hydrochloride 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.
- Purity : 99.94%
- Formula: C71H99ClN12O8S
- Molecular Weight:1316.14
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Biological Activity
Description
IC50 & Target
[1]|
PRMT4 8.1 nM (DC50) |
In Vitro
PROTAC CARM1 degrader-1 hydrochloride (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 hydrochloride (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 hydrochloride (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.
Chemical Information
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Appearance Solid
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Molecular Weight 1316.14
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Formula C71H99ClN12O8S
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Color Off-white to light yellow
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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.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 6.67 mg/mL (5.07 mM; ultrasonic and warming and heat to 60°C; 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). 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). 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)
Purity & Documentation
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Data Sheet (275 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). 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 | 0.7598 mL | 3.7990 mL | 7.5980 mL | 18.9949 mL |
| 5 mM | 0.1520 mL | 0.7598 mL | 1.5196 mL | 3.7990 mL |
PROTAC CARM1 degrader-1 hydrochloride Related Classifications
HY-156152A Related Classifications
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