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HEAL-116

Name: HEAL-116
Brand: TargetMol
SKU: T213010
Rating: 4.5 (1 reviews)

Catalog No. T213010 Copy Product Info

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HEAL-116 is a potent, specific, and orally active inhibitor of the type 1 3β-hydroxysteroid dehydrogenase (3βHSD1), with an IC50 value of 1.18 μM and a KD value of 1.32 μM. It inhibits both the metabolism of DHEA and DHEA-induced expression of target genes as well as cell proliferation. HEAL-116 is applicable in cancer research, including studies on prostate cancer.

HEAL-116

Copy Product Info

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Catalog No. T213010

HEAL-116

Cas No. 3059767-85-7

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	10-14 weeks	10-14 weeks
50 mg	Inquiry	10-14 weeks	10-14 weeks

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	HEAL-116 is a potent, specific, and orally active inhibitor of the type 1 3β-hydroxysteroid dehydrogenase (3βHSD1), with an IC50 value of 1.18 μM and a KD value of 1.32 μM. It inhibits both the metabolism of DHEA and DHEA-induced expression of target genes as well as cell proliferation. HEAL-116 is applicable in cancer research, including studies on prostate cancer.
Targets&IC50	3β-HSD1:1.18 μM
In vitro	HEAL-116 displays a dose-dependent inhibition of DHEA metabolism in LNCaP cells (0.001-0.1 μM). It effectively suppresses endogenous DHEA metabolism in VCaP cells, with an IC 50 of 5.86 nM. At concentrations of 0.1-1 μM, HEAL-116 inhibits DHEA-induced androgen receptor target gene expression and cell growth in both VCaP and C4-2 cells. At a concentration of 10 μM, HEAL-116 does not significantly inhibit 75 other cancer-related kinases. When used in combination with Abiraterone (0.1-1 μM, 48 h), HEAL-116 significantly reduces the production of DHEA, progesterone, and the biological function of pregnenolone in VCaP-CYP17A1 cells. Additionally, at 0.1 μM, HEAL-116 combined with Enzalutamide inhibits DHEA-induced target gene expression and cell proliferation in VCaP cells.
In vivo	Administered orally at a dose of 10 mg/kg, HEAL-116 effectively inhibits tumor growth in a xenograft mouse model sourced from VCaP.

Chemical Properties

Molecular Weight	371.82
Formula	C₂₀H₁₈ClNO₄
Cas No.	3059767-85-7
Smiles	O=C1C(=COC2=CC(O)=CC=C12)C=3C=CC(Cl)=C(C3)CN4CCOCC4

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc