dTRIM 24 - CAS 2170695-14-2

dTRIM 24 is a potent and selective BRD9 bromodomain degrader composed of the TRIM24 ligand IACS-9571 conjugated to a VHL ligand.

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Molecular Formula
C55H68N8O13S2
Molecular Weight
1113.33

dTRIM 24

    • Specification
      • Purity
        ≥98%
        Solubility
        Soluble in DMSO, Ethanol
        Appearance
        White Solid
        Shelf Life
        2 years
        Storage
        Store at -20°C
        IUPAC Name
        (2S,4R)-1-[(2S)-2-[[2-[2-[2-[2-[[3-[[1,3-dimethyl-2-oxo-6-(3-propoxyphenoxy)benzimidazol-5-yl]sulfamoyl]benzoyl]amino]ethoxy]ethoxy]ethoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
        Synonyms
        (2S,4R)-1-((S)-15-(tert-Butyl)-1-(3-(N-(1,3-dimethyl-2-oxo-6-(3-propoxyphenoxy)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)sulfamoyl)phenyl)-1,13-dioxo-5,8,11-trioxa-2,14-diazahexadecan-16-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide; dTRIM24; dTRIM-24
    • Properties
      • Density
        1.316±0.06 g/cm3
        InChI Key
        QUQTXFIMYFMULC-OGOZKGDESA-N
        InChI
        InChI=1S/C55H68N8O13S2/c1-8-20-75-40-12-10-13-41(28-40)76-47-30-45-44(61(6)54(69)62(45)7)29-43(47)60-78(70,71)42-14-9-11-38(26-42)51(66)56-19-21-72-22-23-73-24-25-74-33-48(65)59-50(55(3,4)5)53(68)63-32-39(64)27-46(63)52(67)57-31-36-15-17-37(18-16-36)49-35(2)58-34-77-49/h9-18,26,28-30,34,39,46,50,60,64H,8,19-25,27,31-33H2,1-7H3,(H,56,66)(H,57,67)(H,59,65)/t39-,46+,50-/m1/s1
        Canonical SMILES
        CCCOC1=CC=CC(=C1)OC2=C(C=C3C(=C2)N(C(=O)N3C)C)NS(=O)(=O)C4=CC=CC(=C4)C(=O)NCCOCCOCCOCC(=O)NC(C(=O)N5CC(CC5C(=O)NCC6=CC=C(C=C6)C7=C(N=CS7)C)O)C(C)(C)C
    • Reference Reading
      • 1. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands.
        Gechijian, L.N., Buckley, D.L., Lawlor, M.A., Reyes, J.M., Paulk, J., Ott, C.J., Winter, G.E., Erb, M.A., Scott, T.G., Xu, M. and Seo, H.S., 2018. Nature chemical biology, 14(4), pp.405-412.
        The addressable pocket of a protein is often not functionally relevant in disease. This is true for the multidomain, bromodomain-containing transcriptional regulator TRIM24. TRIM24 has been posited as a dependency in numerous cancers, yet potent and selective ligands for the TRIM24 bromodomain do not exert effective anti-proliferative responses. We therefore repositioned these probes as targeting features for heterobifunctional protein degraders. Recruitment of the VHL E3 ubiquitin ligase by dTRIM24 elicits potent and selective degradation of TRIM24. Using dTRIM24 to probe TRIM24 function, we characterize the dynamic genome-wide consequences of TRIM24 loss on chromatin localization and gene control. Further, we identify TRIM24 as a novel dependency in acute leukemia. Pairwise study of TRIM24 degradation versus bromodomain inhibition reveals enhanced anti-proliferative response from degradation. We offer dTRIM24 as a chemical probe of an emerging cancer dependency, and establish a path forward for numerous selective yet ineffectual ligands for proteins of therapeutic interest.
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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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