3070968-56-5
Chemical Structure
ERα degrader 13
- CAS No.: 3070968-56-5
- Formula:C50H48N4O5S2
- Molecular Weight:849.07
InChIKey: XNCXGLUWWRIIJQ-OZCIJLEVSA-N
SMILES: CCN(C1=CC=C2N=C(C(SC2=C1)=C/C3=N/CCCCCCC(NCCOC4=CC=C(C=C4)C(C5=C(SC6=C5C=CC(O)=C6)C7=CC=C(C=C7)O)=O)=O)C8=C3C=CC=C8)CC
Biological Activity: ERα degrader 13 is an orally active, methylene blue-Raloxifene (HY-13738) conjugated photoactivatable ERα degrader with a Kd value of 27.1 nM. Upon irradiation at 660 nm, ERα degrader 13 generates ROS and heat near the ligand-binding domain of ERα, triggering oxidation, residue unfolding, and ERα degradation via the ubiquitin-proteasome system. ERα degrader 13 inhibits cancer cell proliferation and induces tumor regression in breast cancer xenograft models. ERα degrader 13 can be used in breast cancer-related research[1].
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ERα degrader 13 | ERα degrader 13 is an orally active, methylene blue-Raloxifene (HY-13738) conjugated photoactivatable ERα degrader with a Kd value of 27.1 nM. Upon irradiation at 660 nm, ERα degrader 13 generates ROS and heat near the ligand-binding domain of ERα, triggering oxidation, residue unfolding, and ERα degradation via the ubiquitin-proteasome system. ERα degrader 13 inhibits cancer cell proliferation and induces tumor regression in breast cancer xenograft models. ERα degrader 13 can be used in breast cancer-related research. | |||||||||||||||||||||
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