TRIM24-C34, BRPF1B/TRIM24 Dual Inhibitor

TRIM24-C34 is a potent, selective and cell permeable BRPF1B and TRIM24 dual inhibitor. TRIM24-C34 binds to bromodomain BRPF1B with a Kd of 137 nM, and the transcriptional regulator TRIM24 (also an E3 ubiquitin ligase) with a Kd of 222 nM. It has very good selectivity against other 45 bromodomains. Cellular activity of TRIM24-C34 was demonstrated using FRAP assays as well as cell viability data. It showed no significant cytotoxicity in the cell lines tested.

Product information

CAS Number: 1242907-48-7

Molecular Weight: 499.54

Formula: C24H25N3O7S

Chemical Name: 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide

Smiles: COC1C=CC(=CC=1)OC1C=C2C(=CC=1NS(=O)(=O)C1=CC(OC)=C(C=C1)OC)N(C)C(=O)N2C

InChiKey: KNVIUMWNYXDULF-UHFFFAOYSA-N

InChi: InChI=1S/C24H25N3O7S/c1-26-19-13-18(25-35(29,30)17-10-11-21(32-4)23(12-17)33-5)22(14-20(19)27(2)24(26)28)34-16-8-6-15(31-3)7-9-16/h6-14,25H,1-5H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 20 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

TRIM24-C34 was used at 10 µM final concentration in various in vitro assays.

References:

1. Bennett J, et al. Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. (2015) J Med Chem. In press.

Products are for research use only. Not for human use.