2. Metabolic Enzyme/Protease
  3. 17β-HSD
  4. SCH-451659

SCH-451659 (STX1383) is an orally active, selective 17β-HSD3 inhibitor with an IC50 of 2.4 nM against h17β-HSD3. SCH-451659 selectively blocks the conversion of androstenedione to testosterone. SCH-451659 reduces testosterone levels in mice. SCH-451659 exhibits anticancer activity against androstenedione-dependent prostate tumors.

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SCH-451659

SCH-451659 Chemical Structure

CAS No. : 502628-66-2

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SCH-451659 Related Antibodies

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Description

SCH-451659 (STX1383) is an orally active, selective 17β-HSD3 inhibitor with an IC50 of 2.4 nM against h17β-HSD3. SCH-451659 selectively blocks the conversion of androstenedione to testosterone. SCH-451659 reduces testosterone levels in mice. SCH-451659 exhibits anticancer activity against androstenedione-dependent prostate tumors[1][2].

IC50 & Target[1]

h17β-HSD3

2.4 nM (IC50)

In Vitro

SCH-451659 potently inhibits h17β-HSD3 in 293-EBNA (HSD3) cells with an IC50 of 2.4 nM, while it exhibits only extremely weak activity against 17β-HSD1 in T47D cells and 17β-HSD2 in MDA-MB-231 cells[1].
SCH-451659 (96 h) inhibits the proliferation of LNCaPwt and PC-3 prostate cancer cells, with IC50 values of 5.9 μM and 5.8 μM against the two cell lines within 96 hours[1].
SCH-451659 (500 nM; for 15 consecutive days) inhibits the proliferation of LNCaP (HSD3) prostate cancer cells stimulated by 10 nM adione[1].

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

SCH-451659 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: LNCaP(HSD3) prostate cancer cells
Concentration: 500 nM (alongside 10 nM adione stimulation)
Incubation Time: over15 days
Result: Inhibited 10 nM adione-stimulated LNCaP(HSD3) cell proliferation by 99.8%.
Did not stimulate or inhibit cell proliferation in the absence of adione.
In Vivo

SCH-451659 (20 mg/kg; subcutaneous injection; once daily; for 5 consecutive weeks) significantly inhibits the growth of androstenedione-dependent prostate tumors[1].
SCH-451659 (20 mg/kg, subcutaneous injection, administered on days 1-5 and 8-12 for a total of 12 days) significantly reduces plasma testosterone levels in normal male MF-1 nude mice, decreasing them to 17.4% of the control group concentration[1].
SCH-451659 (15 mg/kg; p.o.; twice daily; for 4 weeks) reduces serum testosterone levels by 50%, testicular testosterone levels by 85%, and prostate weight by 20% in cynomolgus monkeys[2].

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

Animal Model: MF-1 nude mice (male, castrated, inoculated s.c. with 1×107 LNCaP(HSD3) cells, TP-stimulated then switched to adione stimulation)[1]
Dosage: 20 mg/kg
Administration: s.c.; daily; 5 weeks
Result: Inhibited adione-dependent tumour growth significantly, with final tumour volume reaching 326.2 mm3 at day 35 (vs 592.5 mm3 in adione-only controls, P<0.05).
Reduced plasma testosterone concentration to 4.8 ng/mL.
Left mouse body weights unaffected.
Kept 17β-HSD3 and androgen receptor mRNA expression in tumours unchanged relative to in vitro LNCaP(HSD3) cells.
Molecular Weight

544.56

Formula

C30H39Cl2N3O2
CAS No.
SMILES

CC(C)(C)[C@@H]1N(CCN(C1)C(C2=CC=C(C=C2)Cl)C3=CC=C(C=C3)Cl)C(CC4CCN(CC4)C(C)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SCH-451659 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:

SCH-451659502628-66-2STX1383SCH451659SCH 451659STX 1383STX-138317β-HSD17beta-HSD17β-hydroxysteroid dehydrogenases17 beta-hydroxysteroid dehydrogenaseT47D cells17β-HSD3MDA-MB-231 cells17β-HSD117β-hydroxysteroid dehydrogenase type 3293-EBNA(HSD3) cellsandrostenedione17β-HSD2testosteroneandrogen receptor-positive cancer cellsInhibitorinhibitorinhibit

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