PROTAC CARM1 degrader-1 TFA
Based on 1 Customer Validation
PROTAC CARM1 degrader-1 TFA is a highly selective CARM1 PROTAC degrader, with a DC50 of 8.1 nM. PROTAC CARM1 degrader-1 TFA recruits the VHL E3 ubiquitin ligase complex to act on CARM1, inducing a proteasome-dependent degradation process. PROTAC CARM1 degrader-1 TFA downregulates the methylation level of CARM1 substrates. PROTAC CARM1 degrader-1 TFA 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 : 95.04%
- Formula: C73H99F3N12O10S
- Molecular Weight:1393.70
-
Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PRMT4 8.1 nM (DC50) |
VHL |
In Vitro
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MDA-MB-231 cells
-
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.
-
Cell Line:MDA-MB-231 cells
-
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
-
Result:Abolished the CARM1 degradation activity upon co‑treatment with MG132, MLN4924, VH‑032 or TP‑064.
-
Cell Line:MDA-MB-231, BT474 cells
-
Concentration:0.5 μM
-
Incubation Time:48 h
-
Result:Downregulated the asymmetric dimethylation modification of the CARM1 substrates BAF155 and PABP1 in MCF‑7 cells.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0.5 μM
-
Incubation Time:7 days
-
Result:Did not exert significant antiproliferative effect on MCF‑7 and MDA‑MB‑231 cells.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0.5 μM
-
Incubation Time:20 h
-
Result:Produced obvious migration‑inhibitory effect on MDA‑MB‑231 triple‑negative breast cancer cells.
Chemical Information
-
Appearance Solid
-
Molecular Weight 1393.70
-
Formula C73H99F3N12O10S
-
Color White to off-white
-
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.O=C(O)C(F)(F)F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (71.75 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 (sealed storage, away from moisture and light). 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 and light). 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
-
Data Sheet (282 KB)
-
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)
-
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 and light). 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 | 0.7175 mL | 3.5876 mL | 7.1751 mL | 17.9379 mL |
| 5 mM | 0.1435 mL | 0.7175 mL | 1.4350 mL | 3.5876 mL | |
| 10 mM | 0.0718 mL | 0.3588 mL | 0.7175 mL | 1.7938 mL | |
| 15 mM | 0.0478 mL | 0.2392 mL | 0.4783 mL | 1.1959 mL | |
| 20 mM | 0.0359 mL | 0.1794 mL | 0.3588 mL | 0.8969 mL | |
| 25 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7175 mL | |
| 30 mM | 0.0239 mL | 0.1196 mL | 0.2392 mL | 0.5979 mL | |
| 40 mM | 0.0179 mL | 0.0897 mL | 0.1794 mL | 0.4484 mL | |
| 50 mM | 0.0144 mL | 0.0718 mL | 0.1435 mL | 0.3588 mL | |
| 60 mM | 0.0120 mL | 0.0598 mL | 0.1196 mL | 0.2990 mL |
PROTAC CARM1 degrader-1 TFA Related Classifications
HY-156152B Related Classifications
Powered by Bioz