An estrogen receptor antagonist
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ZK 164015

Item No. 45945

Technical Information
Formal Name
2-(4-hydroxyphenyl)-3-methyl-1-[10-(pentylsulfonyl)decyl]-1H-indol-5-ol
CAS Number
177583-70-9
Molecular Formula
C30H43NO4S
Formula Weight
Purity
≥95%
A solid
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CC(C1=CC(O)=CC=C1N2CCCCCCCCCCS(CCCCC)(=O)=O)=C2C3=CC=C(C=C3)O
InChi Code
InChI=1S/C30H43NO4S/c1-3-4-12-21-36(34,35)22-13-10-8-6-5-7-9-11-20-31-29-19-18-27(33)23-28(29)24(2)30(31)25-14-16-26(32)17-15-25/h14-19,23,32-33H,3-13,20-22H2,1-2H3
InChi Key
LYJSJVYJLZOMCD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ZK 164015 is an estrogen receptor antagonist (IC50 = 25 nM in a reporter assay).1 It inhibits the proliferation of MCF-7 breast cancer cells stimulated with E2 (17β-estradiol; IC50 = 51 nM) and unstimulated MCF-7 cells (IC50 = 1.4 nM). ZK 164015 does not increase uterine weight in mice.2 It also inhibits the growth of P. falciparum in isolated human red blood cells in a concentration-dependent manner.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Walter, G., Liebl, R., and von Angerer, E. Synthesis and biological evaluation of stilbene-based pure estrogen antagonists. Bioorg. Med. Chem. Lett. 14(18), 4659-4663 (2004).

    2. Biberger, C., and von Angerer, E. 2-Phenylindoles with sulfur containing side chains. Estrogen receptor affinity, antiestrogenic potency, and antitumor activity. J. Steroid Biochem. Mol. Biol. 58(1), 31-43 (1996).

    3. Honfozo, A., Houngue, R., Vandeputte, A., et alAn image-based high-content screening for compounds targeting Toxoplasma gondii repurposed inhibitors effective against the malaria parasite Plasmodium falciparum. Front. Cell. Infect. Microbiol. 13, 1102551 (2023).