2. GPCR/G Protein Neuronal Signaling Protein Tyrosine Kinase/RTK JAK/STAT Signaling MAPK/ERK Pathway Apoptosis
  3. mGluR EGFR p38 MAPK Apoptosis
  4. 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 blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 can be used in epilepsy research.

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

LY456236

LY456236 Chemical Structure

CAS No. : 338736-46-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of LY456236:

LY456236 Related Antibodies

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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 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].

IC50 & Target[1][2]

mGluR 1

 

EGFR

0.918 μM (IC50)

In Vitro

LY456236 (2 μM; 30 min) reduces DHPG (HY-12598A)-stimulated OCCM-30 proliferation[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LY456236 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: OCCM-30 cells
Concentration: 2 μM
Incubation Time: 30 min, followed by 72 h incubation with DHPG (HY-12598A)
Result: Reduced DHPG-stimulated OCCM-30 proliferation.
In Vivo

LY456236 shows anticonvulsant effects in mice (3-100 mg/kg; i.p.; once) and rats (10-60 mg/kg; oral; once)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: DBA/2 mice and CD1 mice, seizure models[3]
Dosage: 3-100 mg/kg
Administration: IP, once
Result: Produced dose-related anticonvulsant effects in preventing audiogenic-induced (tonic-clonic) seizures in DBA/2 mice, threshold electroshock-induced seizures in CD1 mice, and 6 Hz electroshock-induced seizures in CD1 mice.
Animal Model: Amygdala-kindled Sprague-Dawley rats[3]
Dosage: 10, 30 and 60 mg/kg
Administration: Oral, once
Result: Produced dose-related decreases in behavioral and electrographic seizures at threshold stimulus intensity. Produced a dose-related increase in the stimulus intensity required to produce generalized seizures.
Molecular Weight

317.78

Formula

C16H16ClN3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (786.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1468 mL 15.7342 mL 31.4683 mL
5 mM 0.6294 mL 3.1468 mL 6.2937 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1468 mL 15.7342 mL 31.4683 mL 78.6708 mL
5 mM 0.6294 mL 3.1468 mL 6.2937 mL 15.7342 mL
10 mM 0.3147 mL 1.5734 mL 3.1468 mL 7.8671 mL
15 mM 0.2098 mL 1.0489 mL 2.0979 mL 5.2447 mL
20 mM 0.1573 mL 0.7867 mL 1.5734 mL 3.9335 mL
25 mM 0.1259 mL 0.6294 mL 1.2587 mL 3.1468 mL
30 mM 0.1049 mL 0.5245 mL 1.0489 mL 2.6224 mL
40 mM 0.0787 mL 0.3934 mL 0.7867 mL 1.9668 mL
50 mM 0.0629 mL 0.3147 mL 0.6294 mL 1.5734 mL
60 mM 0.0524 mL 0.2622 mL 0.5245 mL 1.3112 mL
80 mM 0.0393 mL 0.1967 mL 0.3934 mL 0.9834 mL
100 mM 0.0315 mL 0.1573 mL 0.3147 mL 0.7867 mL
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LY456236 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY456236338736-46-2LY 456236LY-456236mGluREGFRp38 MAPKApoptosisMetabotropic glutamate receptorsEpidermal growth factor receptorErbB-1HER1anticonvulsantDHPGOCCM-30DBA/2CD1 miceseizureInhibitorinhibitorinhibit

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