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.
For research use only. We do not sell to patients.
- Purity: 98.52%
- CAS No.: 3059767-85-7
- Formula: C20H18ClNO4
- Molecular Weight:371.81
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Orally Active Compound Library
HY-L061
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Anti-Prostate Cancer Compound Library
HY-L124
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Highly Selective Inhibitors Library
HY-L158
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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3β-HSD I 1.18 μM (IC50) |
3β-HSD I 1.32 μM (Kd) |
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.
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).
Chemical Information
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CAS No. 3059767-85-7
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Appearance Solid
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Molecular Weight 371.81
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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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)
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 | 2.6895 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 |
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