SGI-1776-VHL-02
Based on 1 Customer Validation
SGI-1776-VHL-02 is a stereoselective PIM PROTAC degrader. SGI-1776-VHL-02 promotes the ubiquitination and degradation of PIM1, PIM2 and PIM3. SGI-1776-VHL-02 downregulates c-myc protein levels, induces Apoptosis. SGI-1776-VHL-02 has anti-cancer activity against prostate cancer. SGI-1776-VHL-02 can be used in studies related to prostate cancer.
(Pink: Pim ligand (HY-13287); Blue: VHL ligand (HY-112078); Black: linker (HY-W015300)).
For research use only. We do not sell to patients.
- Purity: 96.67%
- CAS No.: 3013618-84-0
- Formula: C50H62F3N9O6S
- Molecular Weight:974.14
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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
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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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Epigenetics Compound Library
HY-L005
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Immunology/Inflammation Compound Library
HY-L007
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JAK/STAT Compound Library
HY-L008
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Anti-Cancer Compound Library
HY-L025
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Glutamine Metabolism Compound Library
HY-L064
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Anti-Cancer Metabolism Compound Library
HY-L083
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Transcription Factor-Targeted Library
HY-L090
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Anti-Prostate Cancer Compound Library
HY-L124
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Cancer Stem Cells Compound Library
HY-L135
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Mitochondrial Protection Compound Library
HY-L144
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PROTAC Library
HY-L151
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Anti-Ovarian Cancer Compound Library
HY-L173
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Multi-Target Compound Library
HY-L176
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MCE Bioactive Compound Library
HY-L001V
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Cell Proliferation Compound Library
HY-L201
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Lactic Acid Metabolic Compound Library
HY-L204
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High-Throughput Bioactive Compound Library
HY-L205
All PROTACs Isoforms
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Biological Activity
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PIM1 |
PIM2 |
PIM3 |
SGI-1776-VHL-02 (0.75-10 μM; 24 h) dose-dependently degrades doxycycline-induced PIM1 in PC3-dox-PIM1 cells, with the effective degradation starting at a concentration of 0.75 μM[1].
SGI-1776-VHL-02 (0.75-10 μM; 24 h) stereoselectively degrades doxycycline-induced PIM1 in PC3-dox-PIM1 cells, whereas its inactive epimer control fails to induce such degradation[1].
SGI-1776-VHL-02 (1.5 μM; 24 h) does not alter the level of PIM1 mRNA in PC3 cells, confirming that its effect on PIM1 is post-transcriptional[1].
SGI-1776-VHL-02 (1.5-3.75 μM; 24 h) degrades all three PIM kinase isoforms in PC3 cells, with PIM3 degraded at 1.5 μM and PIM2 degraded at 3.75 μM[1].
SGI-1776-VHL-02 (0.75-6.25 μM; 10 days) inhibits colony formation of prostate cancer cell lines PC3, LNCaP and C4-2[1].
SGI-1776-VHL-02 (3.75 μM; 24 h) downregulates c-myc protein levels in PC3 and LNCaP prostate cancer cells[1].
SGI-1776-VHL-02 (3.75 μM; 4 h) induces apoptosis in PC3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3, LNCaP, and C4-2 prostate cancer cells
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Concentration:0.75-6.25 μM
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Incubation Time:10 days, with media replacement every 96 h
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Result:Showed a more potent inhibitory effect on colony formation in PC3, LNCaP, and C4-2 cells compared to its parent inhibitor SGI-1776.
Efficiently reduced colony formation at tested concentrations.
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Cell Line:PC3 and LNCaP prostate cancer cells
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Concentration:3.75 μM
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Incubation Time:24 h
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Result:Downmodulated c-myc after treatment in both PC3 and LNCaP cells.
Showed no c-myc downmodulation effect with the parent inhibitor SGI-1776 or PIM447-VHL-01.
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Cell Line:PC3 cells
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Concentration:3.75 μM (SGI-1776-VHL-02); 2 nM (docetaxel)
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Incubation Time:4 h (SGI-1776-VHL-02 pre-treatment); 48 h (docetaxel incubation)
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Result:Increased apoptosis significantly to 24% of cells as a single agent.
Increased the percentage of apoptotic cells significantly to 40% when co-treated with docetaxel, which was greater than the combination of docetaxel and SGI-1776.
Chemical Information
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CAS No. 3013618-84-0
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Appearance Solid
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Molecular Weight 974.14
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Formula C50H62F3N9O6S
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Color White to off-white
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SMILES
O=C(N1[C@@H](C[C@H](C1)O)C(N[C@H](C2=CC=C(C3=C(N=CS3)C)C=C2)C)=O)[C@H](C(C)(C)C)NC(CCCCCCC(N(CC4)CCC4CNC5=NN6C(C7=CC(OC(F)(F)F)=CC=C7)=CN=C6C=C5)=O)=O
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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
DMSO : 100 mg/mL (102.65 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). 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 (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 |
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| DMSO | 1 mM | 1.0265 mL | 5.1327 mL | 10.2655 mL | 25.6637 mL |
| 5 mM | 0.2053 mL | 1.0265 mL | 2.0531 mL | 5.1327 mL | |
| 10 mM | 0.1027 mL | 0.5133 mL | 1.0265 mL | 2.5664 mL | |
| 15 mM | 0.0684 mL | 0.3422 mL | 0.6844 mL | 1.7109 mL | |
| 20 mM | 0.0513 mL | 0.2566 mL | 0.5133 mL | 1.2832 mL | |
| 25 mM | 0.0411 mL | 0.2053 mL | 0.4106 mL | 1.0265 mL | |
| 30 mM | 0.0342 mL | 0.1711 mL | 0.3422 mL | 0.8555 mL | |
| 40 mM | 0.0257 mL | 0.1283 mL | 0.2566 mL | 0.6416 mL | |
| 50 mM | 0.0205 mL | 0.1027 mL | 0.2053 mL | 0.5133 mL | |
| 60 mM | 0.0171 mL | 0.0855 mL | 0.1711 mL | 0.4277 mL | |
| 80 mM | 0.0128 mL | 0.0642 mL | 0.1283 mL | 0.3208 mL | |
| 100 mM | 0.0103 mL | 0.0513 mL | 0.1027 mL | 0.2566 mL |
SGI-1776-VHL-02 Related Classifications
HY-186146 Related Classifications
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