2. Metabolic Enzyme/Protease
  3. 3β-HSD
  4. HEAL-116

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.

HEAL-116

HEAL-116 Chemical Structure

CAS No. : 3059767-85-7

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HEAL-116 Related Antibodies

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3β-HSD I

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Description

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[1].

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.

HEAL-116 Related Antibodies
In Vivo

HEAL-116 (10 mg/kg, p.o.) inhibits tumor growth in VCaP-derived xenograft mice models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: VCaP-derived xenograft mice models[1]
Dosage: 10 mg/kg
Administration: Administered orally
Result: Reduced tumor weight.
Had no obvious weight loss.
Almost completely arrested tumor progression companied with Abiraterone (HY-70013).
Molecular Weight

371.81

Formula

C20H18ClNO4
CAS No.
SMILES

OC1=CC(OC=C(C2=CC=C(Cl)C(CN3CCOCC3)=C2)C4=O)=C4C=C1
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HEAL-116 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HEAL-1163059767-85-7HEAL116HEAL 1163β-HSD3βHSDDHEALNCaPVCaPC4-2Prostate cancerInhibitorinhibitorinhibit

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