HEAL-116
Based on 1 Customer Validation
HEAL-116 is a potent, specific and orally active 3β-hydroxysteroid dehydrogenase type 1 (3βHSD1) inhibitor with an IC50 of 1.18 μM and a KD of 1.32 μM. HEAL-116 inhibits DHEA (HY-14650) metabolism and DHEA-induced target gene expression and cell proliferation. HEAL-116 can be used for cancer research, such as prostate cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.52%
- CAS. Nr.: 3059767-85-7
- Formel: C20H18ClNO4
- Molecular Weight:371.81
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Speicherung:Powder -20°C, 3 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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
3β-HSD I 1.18 μM (IC50) |
3β-HSD I 1.32 μM (Kd) |
In Vitro
HEAL-116 (0.001-0.1 μM) dose-dependently inhibits DHEA (HY-14650) metabolism in LNCaP cells[1].
HEAL-116 efficiently suppresses endogenous DHEA metabolism in VCaP cells, with an IC50 of 5.86 nM[1].
HEAL-116 (0.1-1 μM) inhibits DHEA-induced androgen receptor target gene expression and cell growth in VCaP and C4-2 cells[1].
HEAL-116 (10 μM) has no dramatic suppression on other cancer-related 75 kinases[1].
HEAL-116 (0.1-1 μM, 48 h) significantly inhibits generation of DHEA or progesterone and biological function of pregnenolonecompanied with Abiraterone (HY-70013) in VCaP-CYP17A1 cells[1].
HEAL-116 (0.1) inhibits DHEA-induced target gene expression and cell proliferation companied with Enzalutamide (HY-70002) in VCaP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:VCaP-derived xenograft mice models[1]
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Dosage:10 mg/kg
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Administration:Administered orally
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Result:Reduced tumor weight.
Had no obvious weight loss.
Almost completely arrested tumor progression companied with Abiraterone (HY-70013).
- RT-PCR
- RNA extraction experimental
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Real Time qPCR (Q-PCR)
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
Chemical Information
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CAS. Nr. 3059767-85-7
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Appearance Solid
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Molecular Weight 371.81
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Formel C20H18ClNO4
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Color White to off-white
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SMILES
OC1=CC(OC=C(C2=CC=C(Cl)C(CN3CCOCC3)=C2)C4=O)=C4C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 5 mg/mL (13.45 mM; warming and heat to 60°C; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (275 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)
Verweise
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 |
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| DMSO | 1 mM | 2.6895 mL | 13.4477 mL | 26.8955 mL | 67.2386 mL |
| 5 mM | 0.5379 mL | 2.6895 mL | 5.3791 mL | 13.4477 mL | |
| 10 mM | 0.2690 mL | 1.3448 mL | 2.6895 mL | 6.7239 mL |
HEAL-116 Related Classifications
HY-175592 Related Classifications
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