2. Stem Cell/Wnt Apoptosis Epigenetics
  3. Hedgehog Apoptosis DNA Methyltransferase
  4. 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).

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Hedgehog IN-11

Hedgehog IN-11 Chemical Structure

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Hedgehog IN-11 Related Antibodies

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Description

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)[1].

IC50 & Target[1]

MGMT

 

In Vitro

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.

Hedgehog IN-11 Related Antibodies

Cell Migration Assay [1]

Cell Line: T98G cells
Concentration: 0.05, 0.5 and 5 nM
Incubation Time: 24 h
Result: Significantly reduced the migration.

Cell Invasion Assay[1]

Cell Line: T98G cells
Concentration: 0.05, 0.5 and 5 nM
Incubation Time: 24 h
Result: Obviously inhibited the invasion.

Apoptosis Analysis[1]

Cell Line: T98G cells
Concentration: 0.05, 0.5 and 5 nM
Incubation Time: 12 h
Result: Resulted in terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick end labeling (TUNEL)-positive DNA strand breaking.

Western Blot Analysis[1]

Cell Line: T98G cells
Concentration: 0.05, 0.5 and 5 nM
Incubation Time: 24 h
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.
In Vivo

Hedgehog IN-11 (Compound 10c2) (6-12 mg/kg, p.o., for 13 days) exhibits promising in mice vivo efficacy against TMZ-resistant GBM and can effectively augment the therapeutic effects of TMZ[1].

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

Animal Model: T98G xenograft model established in NCG mice (female, 18-20 g)[1]
Dosage: 6 mg/kg (with or without TMZ) and 12 mg/kg alone
Administration: Oral administration (p.o.), for 13 days
Result: Significantly inhibited tumor growth with the tumor growth inhibition (TGI) rates of 60 % for low-dose, 69.7 % for high-dose in monotherapy.
Yields better results with TGI of 76.6% in the combined treatment.
Molecular Weight

602.60

Formula

C33H29F3N4O4
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
Shipping

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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Hedgehog IN-11 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:

Hedgehog IN-11Hedgehog IN11Hedgehog IN 11HedgehogApoptosisDNA MethyltransferaseDNMTsDNA MTasesGBMTMZ-resistanceAntitumorTriazolePhenanthroindolizidineInhibitorinhibitorinhibit

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