L134
Based on 1 Customer Validation
L134 is a BRD4 PROTAC degrader with a DC50 of 7.36 nM. L134 induces BRD4 protein degradation without inhibiting BRD4 gene expression, and recruits the E3 ubiquitin ligase DCAF11 to mediate this process, which can be blocked by proteasome inhibitors (MG132 (HY-13259), PS341 (HY-10227)) and E1 ubiquitin ligase inhibitors (PYR41 (HY-13296), MLN4924 (HY-70062)). L134 inhibits cancer cell migration, promotes cancer cell apoptosis and exerts antiproliferative activity. L134 can be used in studies related to triple-negative breast cancer.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-169359); Black: linker (HY-W004640)).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.37%
- CAS No.: 3120166-93-7
- 화학식: C48H51ClF3N7O7S
- 분자량:962.47
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
|
BRD4 7.36 nM (DC50) |
L134 (10 nM-1000 nM; 12 h) potently degrades BD1, a domain of BRD4, in HEK293T cells stably expressing the BD1 reporter gene, with significant degradation effects observable at concentrations as low as 10 nM[1].
L134 (10 nM-1000 nM; 1 h-24 h) efficiently degrades BRD4 in MDA-MB-231 cells via the ubiquitin-proteasome pathway, with a DC50 of 7.36 nM. A significant degradation effect is observed within 1 h of treatment with 1 μM[1].
L134 (1 μM; 12 h)-mediated degradation of BRD4 in HEK293T reporter cells depends on DCAF11, as it promotes the formation of a complex between BRD4 and the E3 ubiquitin ligase DCAF11[1].
L134 (48 h) inhibits the proliferation of various breast cancer cell lines, with the strongest inhibitory activity against MDA-MB-468 cells (IC50 = 0.02 μM) and MDA-MB-231 cells (IC50 = 0.07 μM)[1].
L134 (12 h-24 h) inhibits the migration of MDA-MB-231 breast cancer cells[1].
L134 (0.5 μM-1.0 μM; 48 h) inhibits the migration of MDA-MB-231 breast cancer cells in a dose-dependent manner[1].
L134 induces apoptosis in MDA-MB-231 breast cancer cells via its intact PROTAC structure, which is confirmed by increased levels of cleaved PARP and cleaved Caspase-7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0.1 nM, 1.0 nM, 10 nM, 100 nM, 1000 nM; 1 μM; 5 μM MG132 (HY-13259), 50 nM PS341 (HY-10227), 30 μM PYR41 (HY-13296), 2 μM MLN4924 (HY-70062), 20 μM CQ, 0.25 μM Baf A1 (pretreatment)
-
Incubation Time:0 h, 1 h, 2 h, 3 h, 6 h, 8 h, 12 h, 24 h; 1 h pretreatment
-
Result:Induced rapid BRD4 degradation, with significant reduction observed within 1 h of 1 μM treatment.
Caused concentration-dependent degradation at 12 h, with significant effects seen at 10 nM.
Exhibited a DC50 of 7.36 nM for BRD4 degradation.
Had its BRD4-degrading activity completely or significantly attenuated by pretreatment with proteasome inhibitors (MG132, PS341), E1 ubiquitin ligase inhibitor (PYR41), or NEDD8-activating enzyme inhibitor (MLN4924).
Showed no change in BRD4-degrading activity when pretreated with lysosomal inhibitors (CQ, Baf A1).
-
Cell Line:DCAF11-knockdown HEK293T reporter cells, HEK293T cells
-
Concentration:1 μM
-
Incubation Time:12 h
-
Result:Failed to significantly reduce BRD4 levels in DCAF11-knockdown cells.
Induced strong BRD4 degradation in sgControl cells.
Promoted the interaction between exogenously expressed BD1 and DCAF11.
Facilitated the interaction between endogenous BRD4 and DCAF11.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0 μM, 0.5 μM, 1.0 μM
-
Incubation Time:48 h
-
Result:Induced a dose-dependent reduction in the number of migrated MDA-MB-231 cells.
Caused significant inhibition observed at both 0.5 μM and 1.0 μM compared to control.
Chemical Information
-
CAS No. 3120166-93-7
-
Appearance Solid
-
분자량 962.47
-
화학식 C48H51ClF3N7O7S
-
Color Light yellow to yellow
-
SMILES
CC1=CC=C(C(/C=C2C(NC3=C\2C=CC(C(F)(F)F)=C3)=O)=C1)OCC(NCCCOCCOCCOCCCNC(C[C@@H]4N=C(C5=C(N6C4=NN=C6C)SC(C)=C5C)C7=CC=C(C=C7)Cl)=O)=O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (51.95 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. 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. 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)
순도&문서
-
Data Sheet (276 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 1.0390 mL | 5.1950 mL | 10.3899 mL | 25.9748 mL |
| 5 mM | 0.2078 mL | 1.0390 mL | 2.0780 mL | 5.1950 mL | |
| 10 mM | 0.1039 mL | 0.5195 mL | 1.0390 mL | 2.5975 mL | |
| 15 mM | 0.0693 mL | 0.3463 mL | 0.6927 mL | 1.7317 mL | |
| 20 mM | 0.0519 mL | 0.2597 mL | 0.5195 mL | 1.2987 mL | |
| 25 mM | 0.0416 mL | 0.2078 mL | 0.4156 mL | 1.0390 mL | |
| 30 mM | 0.0346 mL | 0.1732 mL | 0.3463 mL | 0.8658 mL | |
| 40 mM | 0.0260 mL | 0.1299 mL | 0.2597 mL | 0.6494 mL | |
| 50 mM | 0.0208 mL | 0.1039 mL | 0.2078 mL | 0.5195 mL |
L134 Related Classifications
HY-169358 Related Classifications
Powered by Bioz