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Cat. No.: HY-184494

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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.

For research use only. We do not sell to patients.

Formula: C₃₃H₅₅N₃O₃
Molecular Weight:541.81

Storage:

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

GLI-IN-1 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All PKC Isoforms :

In Vitro

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.

Related Protocols :

Mesenchymal stromal/stem cell osteogenic differentiation

Chemical Information

Molecular Weight 541.81
Formula C₃₃H₅₅N₃O₃
SMILES

CCCCCCCC/C=C\CCCCCCCC(NC1=CC(C[C@@H](CO)NC([C@H](C(C)C)N2C)=O)=C2C=C1)=O
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

Handling Instructions (2659 KB)

References

[1]. Haddad M, et al. Design of PKC-Targeting Benzolactams as Gli Inhibitors[J]. ACS Medicinal Chemistry Letters, 2026.

Calculators

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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.

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100 mg

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