dFKBP-1 - CAS 1799711-22-0

dFKBP-1, a potent and PROTAC-based FKBP12 degrader, contains the FKBP12 ligand SLF, the thalidomide based Cereblon ligand, and a linker.

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Molecular Formula
Molecular Weight


    • Specification
      • Purity
        Soluble in DMSO
        Store at 2-8°C, stored under nitrogen
        IUPAC Name
        [(1R)-3-(3,4-dimethoxyphenyl)-1-[3-[[4-[4-[[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetyl]amino]butylamino]-4-oxobutanoyl]amino]phenyl]propyl] (2S)-1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carboxylate
        (1R)-3-(3,4-Dimethoxyphenyl)-1-(3-{[4-({4-[({[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]oxy}acetyl)amino]butyl}amino)-4-oxobutanoyl]amino}phenyl)propyl (2S)-1-(3,3-dimethyl-2-oxopentanoyl)-2-piperidinecarboxylate; 2-Piperidinecarboxylic acid, 1-(3,3-dimethyl-1,2-dioxopentyl)-, (1R)-3-(3,4-dimethoxyphenyl)-1-[3-[[4-[[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]amino]-1,4-dioxobutyl]amino]phenyl]propyl ester, (2S)-
    • Properties
      • Density
        1.3±0.1 g/cm3
        InChI Key
        Canonical SMILES
    • Reference Reading
      • 1. Phthalimide conjugation as a strategy for in vivo target protein degradation.
        Winter, G.E., Buckley, D.L., Paulk, J., Roberts, J.M., Souza, A., Dhe-Paganon, S. and Bradner, J.E., 2015. Science, 348(6241), pp.1376-1381.
        The development of effective pharmacological inhibitors of multidomain scaffold proteins, notably transcription factors, is a particularly challenging problem. In part, this is because many small-molecule antagonists disrupt the activity of only one domain in the target protein. We devised a chemical strategy that promotes ligand-dependent target protein degradation using as an example the transcriptional coactivator BRD4, a protein critical for cancer cell growth and survival. We appended a competitive antagonist of BET bromodomains to a phthalimide moiety to hijack the cereblon E3 ubiquitin ligase complex. The resultant compound, dBET1, induced highly selective cereblon-dependent BET protein degradation in vitro and in vivo and delayed leukemia progression in mice. A second series of probes resulted in selective degradation of the cytosolic protein FKBP12. This chemical strategy for controlling target protein stability may have implications for therapeutically targeting previously intractable proteins.
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It is commonly abbreviated as: C1V1 = C2V2

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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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