A mutant ERα antagonist and ligand used for bump and hole
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CMP8

Item No. 36585

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
9a-[(4-chlorophenyl)methyl]-1,2,9,9a-tetrahydro-7-hydroxy-4-[4-[2-(1-piperidinyl)ethoxy]phenyl]-3H-fluoren-3-one
CAS Number
851107-28-3
Molecular Formula
C33H34ClNO3
Formula Weight
528.1
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
346 nm
SMILES
O=C1C(C2=CC=C(OCCN3CCCCC3)C=C2)=C4C5=CC=C(C=C5CC4(CC1)CC6=CC=C(C=C6)Cl)O
InChi Code
InChI=1S/C33H34ClNO3/c34-26-8-4-23(5-9-26)21-33-15-14-30(37)31(32(33)29-13-10-27(36)20-25(29)22-33)24-6-11-28(12-7-24)38-19-18-35-16-2-1-3-17-35/h4-13,20,36H,1-3,14-19,21-22H2
InChi Key
YHOXIEXEPIIKMD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $36

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    5 mg

    $294

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    10 mg

    $522

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    Product Description

    CMP8 is a mutant estrogen receptor α (ERα) antagonist and ligand used for bump and hole, a technique to study single protein isoforms when familial homology would interfere with other isoform-selective approaches.1 It is selective for an ERα triple mutant containing a lysine-to-methionine substitution at position 384 (ErαL384M), a methionine-to-glycine substitution at position 421 (ErαM421G), and a glycine-to-arginine substitution at position 521 (ErαG521R), over wild-type ERα and ERβ (IC50s= 29, 1,085, and 2,232 nM, respectively). It reduces reporter gene expression in HeLa cells expressing the triple mutant ERα (EC50 = 41 nM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gallinari, P., Lahm, A., Koch, U., et al. A functionally orthogonal estrogen receptor-based transcription switch specifically induced by a nonsteroid synthetic ligand. Chem. Biol. 12(8), 883-893 (2005).