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Art. -Nr.: HY-183335

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SMO-IN-6

Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC₅₀ of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₃H₂₆Cl₂N₂O₃
Molecular Weight:449.37

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

SMO-IN-6 Chemical Structure

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Alle Caspase Isoform-spezifische Produkte anzeigen :

In Vitro

SMO-IN-6 (Compound 16) (72 h) potently inhibits the proliferation of A431 cutaneous squamous cell carcinoma cells, with a GI₅₀ of 1.4 μM and a therapeutic index of 31 relative to non-tumorigenic HaCaT skin cells^[1].
SMO-IN-6 (1-4 μM; 14 days) inhibits long-term colony formation of A431 cutaneous squamous cell carcinoma cells in a dose-dependent manner, with an inhibition rate exceeding 95% at 4 μM^[1].
SMO-IN-6 (1 μM) potently downregulates the expression of Hedgehog/GLI pathway target genes Gli1, Gli2, Ptch1 and HHip in A431 cutaneous squamous cell carcinoma cells^[1].
SMO-IN-6 (1-4 μM; 16 h) induces apoptosis in A431 cutaneous squamous cell carcinoma cells in a dose-dependent manner, with the apoptosis rate reaching 93% at the concentration of 4 μM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

A431 cutaneous squamous cell carcinoma cells
Concentration:

1, 2 and 4 μM
Incubation Time:

14 day
Result:

Inhibited A431 colony formation in a dose-dependent manner: 1 μM reduced colony formation by over 50%, and 4 μM inhibited over 95% of colony formation.

Apoptosis Analysis^[1]

Cell Line:

A431 cutaneous squamous cell carcinoma cells
Concentration:

1, 2 and 4 μM
Incubation Time:

16 h
Result:

Induced apoptosis in A431 cells in a dose-dependent manner: 1 μM induced apoptosis in 38% of cells, 2 μM in 54% of cells, and 4 μM in up to 93% of cells.

In Vivo

SMO-IN-6 (Compound 16) (10-25 mg/kg; i.p.; 2on1off dosing regimen; 14 days) dose-dependently inhibits cutaneous squamous cell carcinoma tumor growth in BALB/c nude mice^[1].

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

Animal Model:

BALB/c nude mice (female, 6-8 weeks old, 18-20 g, subcutaneously injected with A431 cells)^[1]
Dosage:

10 mg/kg; 25 mg/kg
Administration:

i.p.; 2on1off dosing regimen; 14 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 30%.
Achieved a TGI rate of 56%.
Induced ~40% TUNEL-positive apoptotic cells.
Significantly downregulated GLI1, Ki67, and SOX2 levels in tumor tissues.
Significantly upregulated cleaved-caspase 3 levels in tumor tissues.
Caused no significant body weight loss, morphological abnormalities in major organs, or hematological toxicity.

Chemical Information

Molecular Weight 449.37
Formel C₂₃H₂₆Cl₂N₂O₃
SMILES

C[C@]1(O[C@H](COC2=CC=C(N3CC4CCC(N4)C3)C=C2)CO1)C5=CC=C(Cl)C=C5Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Qin W, et al. Development of truncated-itraconazole analogues as potent Hedgehog/GLI pathway inhibitors and potential therapeutic agents for cutaneous squamous cell carcinoma. Eur J Med Chem. 2026;313:118905. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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