EL-102
Based on 1 Customer Validation
EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.44%
- CAS No.: 1233948-61-2
- Formule: C19H16N2O3S2
- Masse moléculaire:384.47
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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DMOG (Standard)HIF-PH Inhibitor
Activité biologique
Description
IC50 & Target
IC50: 24 nM (CWR22), 21.7 nM (22Rv1), 40.3 nM (DU145), 37.0 nM (PC-3), 14.4 nM (DLKP), 16.3 nM (DLKPA)[1]
In Vitro
EL-102 (0-120 nM; 72 h) inhibits prostate cancer cells proliferation in vitro[1]. EL-102 (0-100 nM; 72 h) shows cytotoxicity to prostate cancer cell lines[1]. EL-102 (10-100 nM; 24-72 h) induces cellular apoptosis and affects cell cycle[1]. EL-102 (10-100 nM; 24-48 h) affects PARP cleavage in DU145 cells[1]. EL-102 (5 nM; 0-60 min) inhibits tubulin polymerisation activity[1]. EL-102 (0-100 nM; 1 hour) inhibits Hif1α protein expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA cell lines
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Concentration:0-120 nM
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Incubation Time:72 hours
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Result:Inhibited proliferation of CWR22, 22Rv1, DU145, PC-3, DLKP and doxorubicin-selected variant DLKPA cells with IC50s of 24, 21.7, 40.3, 37.0, 14.4 and 16.3 nM, respectively.
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Cell Line:CWR22, 22Rv1, DU145 and PC-3 cell lines
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Concentration:0-100 nM
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Incubation Time:72 hours
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Result:Exibited cytotoxicity to prostate cancer cell lines, and showed no additive effect on the inhibition of cell viability with docetaxel.
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Cell Line:CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA cell lines
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Concentration:10 and 100 nM
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Incubation Time:24, 48 and 72 hours
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Result:Induced cell apoptosis to inhibits cell viability with a dose of 100 nM.
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Cell Line:DU145 cell line
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Concentration:10 and 100 nM
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Incubation Time:24 and 48 hours
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Result:Increased PARP cleavage in DU145 cells and showed a more dramatic effect with docetaxel adding.
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Cell Line:DU145 cell line
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Concentration:10 and 100 nM
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Incubation Time:24, 48 and 72 hours
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Result:Increased loss of cells from G1 phase and accumulated cells in G2/M phase.
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Cell Line:Prostate cancer cells
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Concentration:10 , 50 and 100 nM
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Incubation Time:24 and 48 hours
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Result:Modestly inhibited Hif1α expression at doses of 50 and 100 nM in normoxia.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice with CWR22 xenografts[1]
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Dosage:12 and 15 mg/kg
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Administration:Oral gavage; 12 and 15 mg/kg 5-day on and 2-day off; from 13 to 37 days after tumour transplantation
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Result:Showed no effect on tumor growth, but enhanced the effect of docetaxel on tumor .
Chemical Information
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CAS No. 1233948-61-2
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Appearance Solid
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Masse moléculaire 384.47
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Formule C19H16N2O3S2
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Color Light yellow to yellow
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SMILES
O=S(C1=CC=C(OC)C=C1)(NC2=CC(C3=CSC(C#N)=C3)=CC=C2C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
In Vitro:
DMSO : ≥ 36 mg/mL (93.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureté et documentation
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Fiche technique (276 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6010 mL | 13.0049 mL | 26.0098 mL | 65.0246 mL |
| 5 mM | 0.5202 mL | 2.6010 mL | 5.2020 mL | 13.0049 mL | |
| 10 mM | 0.2601 mL | 1.3005 mL | 2.6010 mL | 6.5025 mL | |
| 15 mM | 0.1734 mL | 0.8670 mL | 1.7340 mL | 4.3350 mL | |
| 20 mM | 0.1300 mL | 0.6502 mL | 1.3005 mL | 3.2512 mL | |
| 25 mM | 0.1040 mL | 0.5202 mL | 1.0404 mL | 2.6010 mL | |
| 30 mM | 0.0867 mL | 0.4335 mL | 0.8670 mL | 2.1675 mL | |
| 40 mM | 0.0650 mL | 0.3251 mL | 0.6502 mL | 1.6256 mL | |
| 50 mM | 0.0520 mL | 0.2601 mL | 0.5202 mL | 1.3005 mL | |
| 60 mM | 0.0433 mL | 0.2167 mL | 0.4335 mL | 1.0837 mL | |
| 80 mM | 0.0325 mL | 0.1626 mL | 0.3251 mL | 0.8128 mL |
EL-102 Related Classifications
HY-16187 Related Classifications
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