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SML2684

Sigma-Aldrich

dTRIM24

≥98% (HPLC)

Synonym(s):

(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

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About This Item

Empirical Formula (Hill Notation):
C55H68N8O13S2
CAS Number:
Molecular Weight:
1113.30
UNSPSC Code:
12352200
NACRES:
NA.77

ligand

VL-269

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

O=C(N1C)N(C)C2=C1C=C(OC3=CC=CC(OCCC)=C3)C(NS(C4=CC(C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)=CC=C4)(=O)=O)=C2

Biochem/physiol Actions

dTRIM24, a conjugate of IACS-9571 a TRIM24 bromodomain ligand and VL-269 a VHL E3 ubiquitin ligase ligand, is a selective bifunctional degrader of bromodomain-containing transcriptional regulator TRIM24 (transcriptional intermediary factor 1a). dTRIM24 induces rapid and sustain proteasome degradation of TRIM24 in 293FT cells.

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Lara N Gechijian et al.
Nature chemical biology, 14(4), 405-412 (2018-03-07)
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

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