PROTAC SMARCA2/4 degrader-38
Based on 1 Customer Validation
PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC50: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research.
(Pink: Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.46%
- CAS No.: 3081688-77-6
- Formula: C43H47N7O5S
- Molecular Weight:773.94
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Storage: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]
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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
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Apoptosis Compound Library
HY-L003
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Anti-Blood Cancer Compound Library
HY-L079
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PROTAC Library
HY-L151
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Cell Death Library
HY-L162
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Anti-Hematopathy Compound Library
HY-L171
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Multi-Target Compound Library
HY-L176
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MCE Bioactive Compound Library
HY-L001V
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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SMARCA2 3.0 nM (DC50) |
SMARCA4 4.0 nM (DC50) |
VHL |
PROTAC SMARCA2/4 degrader-38 (Compound A11) (25-100 nM, 3 d) inhibits the proliferation activity of MV-4-11 cell lines (IC50: 4.9 nM) and MOLM-13 cell lines (IC50: 23.3 nM) in AML cells, and SU-DHL-4 (IC50: 87.7 nM) and WSU-DLCL-2 (IC50: 336.7 nM) in diffuse large B-cell lymphoma[1].
PROTAC SMARCA2/4 degrader-38 (100-1000 nM, 48 h) induces cell cycle arrest at G0/G1 phase in MV-4-11 and MOLM-13 cells in a concentration-dependent manner[1].
PROTAC SMARCA2/4 degrader-38 (100-1000 nM, 72 h) induces apoptosis in MV-4-11 and MOLM-13 cells[1].
PROTAC SMARCA2/4 degrader-38 (11.1-1000 nM, 24 h) inhibits the transcriptional expression of AML oncogenes in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 cells and MOLM-13 cells
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Concentration:100 nM, 300 nM and 1000 nM
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Incubation Time:48 h
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Result:Induced a large accumulation of G0/G1 cells in MV-4-11 and MOLM-13 cells.
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Cell Line:MV-4-11 cells and MOLM-13 cells
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Concentration:100 nM, 300 nM and 1000 nM
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Incubation Time:72 h
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Result:Induced apoptosis in MV-4-11 and MOLM-13 cells.
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Cell Line:MOLM-13 cells; MV-4-11 cells
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Concentration:100 nM, 300 nM and 1000 nM; 11.1 nM, 33.3 nM, 100 nM, 300 nM and 1000 nM
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Incubation Time:72 h; 24 h
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Result:Up-regulated apoptosis-related cleaved poly ADP-ribose polymerase (PARP) and cleaved caspase-3 proteins levels.
Down-regulated MYC protein level.
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Cell Line:MV-4-11 cells
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Concentration:11.1 nM, 33.3 nM, 100 nM, 300 nM and 1000 nM
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Incubation Time:24 h
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Result:Down-regulated the expression of E2F1, CDC25A, TRAP1, PU. 1, CD44 and BCL-2 genes.
| Species | Dose | Route | Plasma Concentration | Tmax | T1/2 | AUC | MRT | Bioavailability |
|---|---|---|---|---|---|---|---|---|
| Rat | 1 mg/kg | i.v. | 1953 ng/mL | 0.033 h | 1.91 h | 358 ng·h/mL | 0.70 h | / |
| Rat | 10 mg/kg | p.o. | 6.41 ng/mL | 0.42 h | 2.10 h | 8.22 ng·h/mL | 0.81 h | 0.62 % |
Chemical Information
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CAS No. 3081688-77-6
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Appearance Solid
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Molecular Weight 773.94
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Formula C43H47N7O5S
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Color Off-white to light yellow
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SMILES
O=C([C@H]1N(C([C@@H](NC(C2(C3=CC=C(C4=CC(C5=CC=CC=C5O)=NN=C4N)C=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (129.21 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)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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. 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 | 1.2921 mL | 6.4604 mL | 12.9209 mL | 32.3022 mL |
| 5 mM | 0.2584 mL | 1.2921 mL | 2.5842 mL | 6.4604 mL | |
| 10 mM | 0.1292 mL | 0.6460 mL | 1.2921 mL | 3.2302 mL | |
| 15 mM | 0.0861 mL | 0.4307 mL | 0.8614 mL | 2.1535 mL | |
| 20 mM | 0.0646 mL | 0.3230 mL | 0.6460 mL | 1.6151 mL | |
| 25 mM | 0.0517 mL | 0.2584 mL | 0.5168 mL | 1.2921 mL | |
| 30 mM | 0.0431 mL | 0.2153 mL | 0.4307 mL | 1.0767 mL | |
| 40 mM | 0.0323 mL | 0.1615 mL | 0.3230 mL | 0.8076 mL | |
| 50 mM | 0.0258 mL | 0.1292 mL | 0.2584 mL | 0.6460 mL | |
| 60 mM | 0.0215 mL | 0.1077 mL | 0.2153 mL | 0.5384 mL | |
| 80 mM | 0.0162 mL | 0.0808 mL | 0.1615 mL | 0.4038 mL | |
| 100 mM | 0.0129 mL | 0.0646 mL | 0.1292 mL | 0.3230 mL |
PROTAC SMARCA2/4 degrader-38 Related Classifications
HY-173333 Related Classifications
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