Hedgehog IN-11
Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM).
For research use only. We do not sell to patients.
- Formula: C33H29F3N4O4
- Molecular Weight:602.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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- References
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Help & FAQs
All DNA Methyltransferase Isoforms
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Biological Activity
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MGMT |
Hedgehog IN-11 (Compound 10c2) (72 h) exhibits anti-proliferative efficacy toward U87MG, T98G, U343/TMZ, and U251/TMZ cells, with an IC50s of 0.27, 0.70, 0.35, and 0.65 nM, resepectively, and exhibits significantly lower cytotoxicity toward GES-1 cells, with a half cytotoxic concentration (CC50) of 1.12 nM[1].
Hedgehog IN-11 (0.05-5 nM, 24 h-12 d) inhibits colony formation, migration, and invasion of T98G cells[1].
Hedgehog IN-11 (0.05-50 nM, 12 h) induces cell apoptosis and suppresses the expression of MGMT by inhibiting the Hedgehog signaling pathway in T98G cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T98G cells
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Concentration:0.05, 0.5 and 5 nM
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Incubation Time:24 h
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Result:Significantly reduced the migration.
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Cell Line:T98G cells
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Concentration:0.05, 0.5 and 5 nM
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Incubation Time:24 h
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Result:Obviously inhibited the invasion.
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Cell Line:T98G cells
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Concentration:0.05, 0.5 and 5 nM
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Incubation Time:12 h
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Result:Resulted in terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick end labeling (TUNEL)-positive DNA strand breaking.
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Cell Line:T98G cells
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Concentration:0.05, 0.5 and 5 nM
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Incubation Time:24 h
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Result:Resulted in elevated expression of cleaved caspase-3, cleaved poly ADP-ribose polymerase (PARP) and phosphorylated H2AX (γ-H2AX) in a dose-dependent manner.
Demonstrated dose-dependent inhibition of Gli1 and MGMT.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:T98G xenograft model established in NCG mice (female, 18-20 g)[1]
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Dosage:6 mg/kg (with or without TMZ) and 12 mg/kg alone
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Administration:Oral administration (p.o.), for 13 days
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Result:Significantly inhibited tumor growth with the tumor growth inhibition (TGI) rates of 60 % for low-dose, 69.7 % for high-dose in monotherapy.
Yielded better results with TGI of 76.6% in the combined treatment.
Chemical Information
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Molecular Weight 602.60
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Formula C33H29F3N4O4
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SMILES
O=C(OC1=CC2=C(C3=C(C4=C2C=C(C(OC)=C4)OC)CN5CCC[C@]5(C3)[H])C=C1)C(N=N6)=CN6CC7=CC=C(C(F)(F)F)C=C7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hedgehog IN-11 Related Classifications
HY-175299 Related Classifications
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