PROTAC RAR Degrader-1 - CAS 1351169-27-1

PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).

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Molecular Formula
Molecular Weight

PROTAC RAR Degrader-1

    • Specification
      • Solubility
        10 mM in DMSO
        Please store the product under the recommended conditions in the Certificate of Analysis.
        Room temperature in continental US; may vary elsewhere
        IUPAC Name
        2-[3-[[2-[2-[2-[2-[[(2S)-2-[[(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]amino]-4-methylpentanoyl]amino]ethoxy]ethoxy]ethoxy]acetyl]amino]propoxy]-4-[(E)-3-(3,5-ditert-butylphenyl)-3-oxoprop-1-enyl]benzoic acid
        Benzoic acid, 2-[[(18S,21S,22R)-22-amino-21-hydroxy-18-(2-methylpropyl)-5,17,20-trioxo-23-phenyl-7,10,13-trioxa-4,16,19-triazatricos-1-yl]oxy]-4-[(1E)-3-[3,5-bis(1,1-dimethylethyl)phenyl]-3-oxo-1-propen-1-yl]-; 2-[[(18S,21S,22R)-22-Amino-21-hydroxy-18-(2-methylpropyl)-5,17,20-trioxo-23-phenyl-7,10,13-trioxa-4,16,19-triazatricos-1-yl]oxy]-4-[(1E)-3-[3,5-bis(1,1-dimethylethyl)phenyl]-3-oxo-1-propen-1-yl]benzoic acid; 2-(((18S,21S,22R)-22-Amino-21-hydroxy-18-isobutyl-5,17,20-trioxo-23-phenyl-7,10,13-trioxa-4,16,19-triazatricosyl)oxy)-4-((E)-3-(3,5-di-tert-butylphenyl)-3-oxoprop-1-en-1-yl)benzoic acid
    • Properties
      • Boiling Point
        1079.7±65.0°C at 760 Torr
        1.160±0.06 g/cm3
        InChI Key
        Canonical SMILES
    • Reference Reading
      • 1. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers.
        Itoh, Y., Kitaguchi, R., Ishikawa, M., Naito, M. and Hashimoto, Y., 2011. Bioorganic & medicinal chemistry, 19(22), pp.6768-6778.
        Compounds that regulate the function(s) of nuclear receptors (NRs) are useful for biological studies and as candidate therapeutic agents. Most such compounds are agonists or antagonists. On the other hand, we have developed specific protein degradation inducers, which we designated as SNIPERs (Specific and Nongenetic IAPs-dependent Protein ERasers), for selective degradation of target proteins. SNIPERs are hybrid molecules consisting of an appropriate ligand for the protein of interest, coupled to a ligand for inhibitor of apoptosis proteins (IAPs), which target the bound protein for polyubiquitination and proteasomal degradation. We considered that protein knockdown with SNIPERs would be a promising alternative approach for modulating NR function. In this study, we designed and synthesized degradation inducers targeting retinoic acid receptor (RAR), estrogen receptor (ER), and androgen receptor (AR). These newly synthesized RAR, ER, and AR SNIPERs, 9, 11, and 13, respectively, were confirmed to significantly reduce the levels of the corresponding NRs in live cells.
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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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