OH14
Based on 1 Customer Validation
OH14 is a cellular FLICE-like inhibitory protein (cFLIP) inhibitor and TNF-related apoptosis-inducing ligand (TRAIL) sensitizer. OH14 selectively binds to the DED1 pocket of cFLIP, disrupting its recruitment to the TRAIL-death inducing signalling complex without affecting procaspase-8 recruitment to FADD, allowing procaspase-8 activation. OH14 promotes TRAIL-mediated apoptosis and impairs cell viability in breast cancer systems when combined with TRAIL. OH14 can be used for the research of breast cancer.
For research use only. We do not sell to patients.
- Purity: 99.57%
- CAS No.: 1018153-87-1
- Formula: C14H11Cl2NO4S
- Molecular Weight:360.21
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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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Biological Activity
OH14 (75-100 μM; 1 h) sensitizes MCF-7 breast cancer cells and HeLa cells to TNF-related apoptosis-inducing ligand (TRAIL)-induced apoptosis in a dose-dependent manner, as measured by increased cleaved caspase 3/7 activity and Annexin V staining, respectively[1].
OH14 (100 μM; 1 h) requires the R38 residue in cFLIP to sensitize HeLa cells to TRAIL-induced apoptosis, while overexpression of wild-type, H7A, or K18I/R45A mutant cFLIP does not impair this sensitizing activity[1].
OH14 (100 μM; 1 h) significantly sensitizes MCF-7, BT474, and MDA-MB-231 breast cancer cell lines to TRAIL-induced cell death, with variable effects across other breast cancer subtypes[1].
OH14 (100 μM; 1 h) disrupts TRAIL-mediated recruitment of cFLIP to FADD in HeLa cells, as measured by loss of FRET signal between cFLIP-YFP and FADD-CFP[1].
OH14 (100 μM; 1 h) specifically disrupts TRAIL-mediated recruitment of cFLIP to the FADD complex in MCF-7 cells, while allowing procaspase-8 cleavage and activation[1].
OH14 (10 μM; 10 days) sensitizes MCF-7 breast cancer cells to TRAIL-induced reduction in colony formation, without affecting colony growth when administered alone[1].
OH14 (10 μM; 24 h) is non-toxic to HEK293 non-tumorigenic human embryonic kidney cells, either alone or in combination with TRAIL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 breast cancer cells, HeLa cells
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Concentration:75 μM, 100 μM
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Incubation Time:1 h pre-incubation, followed by 24 h TRAIL treatment
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Result:Observed a dose-dependent sensitization effect.
Significantly increased cleaved caspase 3/7 activity in MCF-7 cells.
Significantly increased Annexin V staining in HeLa cells.
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Cell Line:Panel of breast cancer cell lines: MCF-7, BT474, MDA-MB-231, HCC1954, SUM149
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Concentration:100 μM
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Incubation Time:1 h pre-incubation, followed by 18 h TRAIL treatment
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Result:Significantly sensitized MCF-7, BT474, and MDA-MB-231 breast cancer cell lines to TRAIL.
Observed similar but statistically insignificant trends in HCC1954 and SUM149 cells.
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Cell Line:MCF-7 breast cancer cells
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Concentration:100 μM
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Incubation Time:1 h pre-incubation, followed by 2 h TRAIL treatment
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Result:Disrupted the TRAIL-induced interaction between FADD and both short and long forms of cFLIP.
Did not inhibit the interaction between FADD and procaspase-8.
Increased the ratio of cleaved cFLIP (43 kDa) to noncleaved cFLIP (55 kDa).
Induced cleavage of procaspase-8 to its active 43 kDa form when combined with TRAIL.
Chemical Information
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CAS No. 1018153-87-1
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Appearance Solid
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Molecular Weight 360.21
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Formula C14H11Cl2NO4S
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Color White to off-white
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SMILES
CC1=C(C=C(C(S(=O)(NC2=CC=CC=C2C(O)=O)=O)=C1)Cl)Cl
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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 : 35 mg/mL (97.17 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 (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. 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 | 2.7762 mL | 13.8808 mL | 27.7616 mL | 69.4040 mL |
| 5 mM | 0.5552 mL | 2.7762 mL | 5.5523 mL | 13.8808 mL | |
| 10 mM | 0.2776 mL | 1.3881 mL | 2.7762 mL | 6.9404 mL | |
| 15 mM | 0.1851 mL | 0.9254 mL | 1.8508 mL | 4.6269 mL | |
| 20 mM | 0.1388 mL | 0.6940 mL | 1.3881 mL | 3.4702 mL | |
| 25 mM | 0.1110 mL | 0.5552 mL | 1.1105 mL | 2.7762 mL | |
| 30 mM | 0.0925 mL | 0.4627 mL | 0.9254 mL | 2.3135 mL | |
| 40 mM | 0.0694 mL | 0.3470 mL | 0.6940 mL | 1.7351 mL | |
| 50 mM | 0.0555 mL | 0.2776 mL | 0.5552 mL | 1.3881 mL | |
| 60 mM | 0.0463 mL | 0.2313 mL | 0.4627 mL | 1.1567 mL | |
| 80 mM | 0.0347 mL | 0.1735 mL | 0.3470 mL | 0.8675 mL |
OH14 Related Classifications
HY-182307 Related Classifications
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