LY456236

LY456236 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 can also inhibit EGFR, with an IC50 of 0.918 μM. LY456236 has anticonvulsant effects and blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A) . LY456236 can be used in epilepsy research[1][2][3].

Product Specifications

CAS Number

[338736-46-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; EGFR; mGluR; p38 MAPK

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; JAK/STAT Signaling; MAPK/ERK Pathway; Neuronal Signaling; Protein Tyrosine Kinase/RTK

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Infection; Inflammation/Immunology; Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ly456236.html

Purity

99.57

Solubility

DMSO : 250 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

COC1=CC=C(NC2=C3C=C(OC)C=CC3=NC=N2)C=C1.[H]Cl

Molecular Formula

C16H16ClN3O2

Molecular Weight

317.78

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[3]Shannon HE, et al. Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology. 2005;49 Suppl 1:188-95.