dTRIM24( dTRIM 24 | dTRIM24 | dTRIM-24 )

Catalog No. M13466 CAS No. 2170695-14-2

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

dTRIM24
Note

Research use only, not for human use.
Brief Description

dTRIM24 is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).
Description

dTRIM24 is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).
In Vitro

dTRIM24 is a degrader of TRIM24 bromodomain. Recruitment of the VHL E3 ubiquitin ligase by dTRIM24 elicits potent and selective degradation of TRIM24. The anti-proliferative consequences of chemical degradation versus inhibition of TRIM24 are assessed. Growth over time is determined for MOLM-13 cells treated with dTRIM24, IACS-9571, VL-269, and eTRIM24. dTRIM24 suppresses growth to a greater extent than does IACS-9571, accompanied by apoptosis measured as enhanced PARP cleavage. In agreement with a sustained proliferative defect observed following dTRIM24 treatment, near-complete degradation of TRIM24 is observed in dTRIM24-treated cells throughout the duration of the experiment.
In Vivo

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Synonyms

dTRIM 24 | dTRIM24 | dTRIM-24
Pathway

PROTACs
Target

PROTAC
Recptor

PROTAC
Research Area

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Indication

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CAS Number

2170695-14-2
Formula Weight

1113.312
Molecular Formula

C55H68N8O13S2
Purity

>98% (HPLC)
Solubility

Ethanol : < 1 mg/mL
SMILES

O=C([C@H]1N(C([C@H](C(C)(C)C)NC(COCCOCCOCCNC(C2=CC=CC(S(=O)(NC3=C(OC4=CC=CC(OCCC)=C4)C=C(C(N5C)=C3)N(C)C5=O)=O)=C2)=O)=O)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)C=C6
Chemical Name

(2S,4R)-1-((S)-15-(tert-butyl)-1-(3-(N-(1,3-dimethyl-2-oxo-6-(3-propoxyphenoxy)-2,3-dihydro-1 -benzo[ ]imidazol-5-yl)sulfamoyl)phenyl)-1,13-dioxo-5,8,11-trioxa-2,14-diazahexadecan-16-oyl)-4-hydroxy- (4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamid

1. Gechijian LN, et al. Nat Chem Biol. 2018 Mar 5. doi: 10.1038/s41589-018-0010-y.

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