Merck GSK9311

GSK9311

≥98% (HPLC)

N-[2,3-Dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-N-ethyl-2-methoxybenzamide, (R)-N-(1,3-Dimethyl-6-(2-methylpiperazin-1-yl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-N-ethyl-2-methoxybenzamide

assay

≥98% (HPLC)

form

powder

광학 활성

[α]/D 90 to 100°, c = 0.3 in methanol

색상

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

저장 온도

−20°C

SMILES string

O=C1N(C)C2=CC(N3CCNC[C@H]3C)=C(N(CC)C(C4=C(OC)C=CC=C4)=O)C=C2N1C

GSK9311 is a negative control for the SGC epigenetic probe GSK6853. GSK9311 exhibits 125- and 185-fold reduced potency than its structural analog GSK6853 toward BRPF1 in cell-free and cell-based assays (pIC50 = 6.0/GSK9311 vs. 8.1/GSK6853 in ligand competition binding assay by TR-FRET; IC50 = 3.7 μM/GSK9311 vs. 20 nM/GSK6853 against NanoLuc-BRPF1 bromodomain interaction with Histone H3.3-HaloTag in HEK293 cells), and therefore serves as a good inactive control compound in BRPF1 inhibition studies employing GSK6853. For characterization details of the active probe, GSK6853, please visit the GSK6853 probe summary on the Structural Genomics Consortium (SGC) website.

GSK6853, the active probe, is available from Sigma. To learn more about and purchase GSK6853, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc