3092711-76-4
Chemical Structure
PROTAC HDAC6/ERα degrader 1
- CAS No.: 3092711-76-4
- Formula:C64H77F3N6O12S2
- Molecular Weight:1243.45
InChIKey: OTBJEKWWIIHJOB-JMPPVUBHSA-N
SMILES: FC(F)(F)CN(C1=CC=C(C=C1)OCCCCCCC(N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(N[C@@H](C3=CC=C(C4=C(C)N=CS4)C=C3)C)=O)=O)=O)S(=O)([C@@H]5[C@@]6([H])C(C7=CC=C(C=C7)NC(CCCCCCC(O)=O)=O)=C(C8=CC=C(C=C8)O)[C@](C5)([H])O6)=O
Biological Activity: PROTAC HDAC6/ERα degrader 1 is a dual-target PROTAC that targets HDAC6/ERα, with DC50 values of 1.21 μM (HDAC6), 0.28 μM (ERα) in MCF-7 cells and 0.67 μM (HDAC6), 0.14 μM (ERα) in LCC2 cells, respectively. PROTAC HDAC6/ERα degrader 1 selectively degrades ERα and HDAC6 via the proteasomal pathway, inhibits the transcriptional activation of ERα and blocks the estrogen signaling pathway. PROTAC HDAC6/ERα degrader 1 inhibits the function of HDAC6, attenuates hormone responses, and disrupts autophagy-lysosome function. PROTAC HDAC6/ERα degrader 1 induces cell cycle arrest, apoptosis and ferroptosis, and exhibits antiproliferative activity in breast cancer cells. PROTAC HDAC6/ERα degrader 1 can be used for breast cancer research[1].
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PROTAC HDAC6/ERα degrader 1 | PROTAC HDAC6/ERα degrader 1 is a dual-target PROTAC that targets HDAC6/ERα, with DC50 values of 1.21 μM (HDAC6), 0.28 μM (ERα) in MCF-7 cells and 0.67 μM (HDAC6), 0.14 μM (ERα) in LCC2 cells, respectively. PROTAC HDAC6/ERα degrader 1 selectively degrades ERα and HDAC6 via the proteasomal pathway, inhibits the transcriptional activation of ERα and blocks the estrogen signaling pathway. PROTAC HDAC6/ERα degrader 1 inhibits the function of HDAC6, attenuates hormone responses, and disrupts autophagy-lysosome function. PROTAC HDAC6/ERα degrader 1 induces cell cycle arrest, apoptosis and ferroptosis, and exhibits antiproliferative activity in breast cancer cells. PROTAC HDAC6/ERα degrader 1 can be used for breast cancer research. | |||||||||||||||||||||
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