GLI-IN-1
GLI-IN-1 is a potent, PKC-dependent Gli inhibitor. GLI-IN-1 binds to the C1 domain of PKC, forms hydrogen-bonding interactions with the M239 residue, and mediates the inhibition of downstream Gli via a PKC-mediated, Smoothened-independent mechanism. GLI-IN-1 can be used in studies of Gli-driven cancers and osteogenic differentiation.
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- Formel: C33H55N3O3
- Molecular Weight:541.81
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
GLI-IN-1 (Compound 7e) (30 h) potently inhibits the Smo-dependent Gli signaling pathway in Shh-LIGHT2 cells, with an IC50 value of 21 nM[1].
GLI-IN-1 (30 h) potently inhibits the Smo-independent constitutive Gli signaling pathway in Sufu-KO-LIGHT cells, with an IC50 of 24 nM[1].
GLI-IN-1 potently inhibits Gli-dependent osteogenic differentiation in C3H10T1/2 mesenchymal stem cells, with an IC50 of 22 nM[1].
GLI-IN-1 shows no detectable cytotoxicity in Shh-LIGHT2, Sufu-KO-LIGHT and C3H10T1/2 cells, with a CC50 >5000 nM[1].
GLI-IN-1 exhibits favorable metabolic stability in liver microsomes, with an intrinsic clearance rate of 3.2 μL min−1 mg−1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 541.81
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Formel C33H55N3O3
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SMILES
CCCCCCCC/C=C\CCCCCCCC(NC1=CC(C[C@@H](CO)NC([C@H](C(C)C)N2C)=O)=C2C=C1)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)