CMP8
CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively.
For research use only. We do not sell to patients.
- CAS No.: 851107-28-3
- Formula: C33H34ClNO3
- Molecular Weight:528.08
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[2]|
MGERα 29 nM (IC50) |
MGRERα 41 nM (IC50) |
hERα 1100 nM (IC50) |
hERβ 2200 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
41 nM
Compound: 20h
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Activity at ERalpha L384M/M421G/G521R mutant in HeLa cells assessed as activation of SEAP reporter gene
Activity at ERalpha L384M/M421G/G521R mutant in HeLa cells assessed as activation of SEAP reporter gene
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[PMID: 16942012] |
In Vivo
Chemical Information
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CAS No. 851107-28-3
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Molecular Weight 528.08
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Formula C33H34ClNO3
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SMILES
O=C1CCC2(CC3=CC=C(Cl)C=C3)CC4=C(C=CC(O)=C4)C2=C1C5=CC=C(OCCN6CCCCC6)C=C5
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Purity & Documentation
References
[1]. Miyazaki Y, et al. Destabilizing domains derived from the human estrogen receptor. J Am Chem Soc. 2012 Mar 7;134(9):3942-5. [Content Brief]
[2]. Kinzel O, et al. A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies. J Med Chem. 2006 Sep 7;49(18):5404-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)