LY456236 free base
LY456236 free base is a selective, non-competitive and orally active antagonist of glutamate receptor 1 (mGlu1), which can inhibit phosphatidylinositol hydrolysis with an IC50 of 0.145 μM. LY456236 free base can also inhibit EGFR, with an IC50 of 0.918 μM. LY456236 free base blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 free base can be used in epilepsy research.
For research use only. We do not sell to patients.
- CAS No.: 338738-57-1
- Formula: C16H15N3O2
- Molecular Weight:281.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
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mGluR 1 |
EGFR 0.918 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | Inhibition |
52.82 %
Compound: LY456236
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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
10.21203/rs.3.rs-23951/v1 |
Chemical Information
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CAS No. 338738-57-1
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Molecular Weight 281.31
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Formula C16H15N3O2
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SMILES
COC1=CC=C(NC2=C3C=C(OC)C=CC3=NC=N2)C=C1
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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
[1]. Ravikumar B, et al. Chemogenomic Analysis of the Druggable Kinome and Its Application to Repositioning and Lead Identification Studies. Cell Chem Biol. 2019 Nov 21;26(11):1608-1622.e6. [Content Brief]
[2]. Kanaya S, et al. Metabotropic glutamate receptor 1 promotes cementoblast proliferation via MAP kinase signaling pathways. Connect Tissue Res. 2016 Sep;57(5):417-26. [Content Brief]
[3]. Shannon HE, et al. Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology. 2005;49 Suppl 1:188-95. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)