1. PROTAC Epigenetics Cell Cycle/DNA Damage
  2. PROTACs Aurora Kinase
  3. HLB-0532259

HLB-0532259 is a PROTAC degrader for Aurora-A and N-Myc. HLB-0532259 degrades Aurora-Ain a non-MYCN amplified MCF-7 with a DC50 of 20.2 nM, degrades N-Myc in MYCN amplified cells SK-N-BE and Kelly with DC50 of 179 nM and 229 nM. HLB-0532259 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-168440); Black: linker (HY-W007957); Blue: ligand for E3 ligase Cereblon (HY-41547))

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HLB-0532259 Chemical Structure

HLB-0532259 Chemical Structure

CAS No. : 2566733-45-5

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Description

HLB-0532259 is a PROTAC degrader for Aurora-A and N-Myc. HLB-0532259 degrades Aurora-Ain a non-MYCN amplified MCF-7 with a DC50 of 20.2 nM, degrades N-Myc in MYCN amplified cells SK-N-BE and Kelly with DC50 of 179 nM and 229 nM. HLB-0532259 exhibits antitumor efficacy in mouse models[1]. (Pink: ligand for target protein (HY-168440); Black: linker (HY-W007957); Blue: ligand for E3 ligase Cereblon (HY-41547))

Molecular Weight

748.83

Formula

C40H44N8O7

CAS No.
SMILES

O=C(N(C)C)C(N1C2CCCC2)=CC3=C1N=C(NC4=CC=C(C(NCCCCCCOC5=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=CC=C5)=O)C=C4)N=C3

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
HLB-0532259
Cat. No.:
HY-168439
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