GLI1-IN-1
GLI1-IN-1 (CBC-1) is a GLI-1 inhibitor with excellent water solubility and anticancer activity. GLI1-IN-1 can induce apoptosis and suppress the growth of colorectal cancer by inhibiting the Hedgehog(HH) (IC50=1.3 μM) pathway.
For research use only. We do not sell to patients.
- CAS No.: 2923907-92-8
- Formula: C42H60N2O9
- Molecular Weight:736.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
IC50: 1.3 μM (Hedgehog)[1].
GLI1-IN-1 (CBC-1) (5-40 μM; 24-48 h) exhibits anticancer activity by inhibiting cell proliferation through suppressing the mRNA and protein expression of the HH pathway in HT-29, SW-480, and HCT-116 cells, with IC50 values of 7.13, 15.31, and 3.33 μM, respectively. GLI1-IN-1 (5-40 μM; 24 h) can also induce apoptosis in HT-29 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29
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Concentration:5, 10, 20, 40 µM;
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Incubation Time:24 h
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Result:Increased the number of apoptotic cells in a concentration-dependent manner.
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Cell Line:HT-29
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Concentration:5, 10, 20, 40 µM;
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Incubation Time:24 h, 48 h
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Result:Decreased the mRNA expression of SHH, SMO, GLI1, and PTCH in a concentration- and time-dependent manner.
Significantly reduced the mRNA expression levels of the apoptosis-related factor BCL-2 and increased the levels of the apoptosis-promoting factor BAX in a dose-dependent manner.
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Cell Line:HT-29
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Concentration:5, 10, 20, 40 µM;
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Incubation Time:24 h
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Result:Decreased the protein expression of SHH, SMO and GLI1 in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tumour xenograft BALB/c/nu/nu nude mice model[1].
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection (i.p.); Once daily for 16 days
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Result:Significantly reduced the size and weight of HT29 tumor xenografts.
Decreased the protein expression of GLI -1.
Chemical Information
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CAS No. 2923907-92-8
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Molecular Weight 736.93
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Formula C42H60N2O9
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SMILES
CN1CCN(CC(O[C@@H]2CC3=CC[C@]([C@](CC[C@@]4(O)[C@@H](OC([C@@H](C)CC)=O)C)(O)[C@]4(C)[C@H](OC(/C=C/C5=CC=CC=C5)=O)C6)(O)C6[C@@]3(C)CC2)=O)CC1
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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)