GSK6853

Empirical Formula (Hill Notation):	C22H27N5O3
CAS Number:	1910124-24-1
Molecular Weight:	409.48
MDL number:	MFCD30489734

Кат. номер

SML1985-5MG

SML1985-25MG

Biochem/physiol Actions
GSK6853 is a GSK5959 structural analog with improved aqueous solubility (140 µg/mL vs. 8 µg/mL for GSK5959 in pH 7.4 PBS), affinity toward BRPF1 bromodomain (pKd = 9.5 vs 8.0 for GSK5959), cellular efficacy (pIC50 = 7.7 vs 6.0 for GSK5959; against NanoLuc-BRPF1 bromodomain interaction with Histone H3.3-HaloTag in HEK293 cells), and selectivity, displaying little or no inhibitory potency against a panel of 48 channels/receptors/enzymes and >1600-fold reduced affinity toward other bromodomains tested (>90-fold in the case of GSK5959), including those of BRPF2 (BRD1) and BRPF3. GSK6853 displays good bioavailability when administered via intraperitoneal injection in mice in vivo (Cmax = 469 ng/mL, Tmax = 0.25 h, F = 85%; 3 mg/kg i.p.). The structural analog GSK9311 serves as a good inactive control (125- and 185-fold reduced potency in cell-free and cell-based assays, respectively). GSK9311 is the negative control for the active enantiomer, GSK6853. GSK9311 is available from Sigma. To learn more about and purchase GSK9311, click here,.
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc,
Features and Benefits
GSK6853 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC,.

assay	≥98% (HPLC)
form	powder
optical activity	[α]/D -45 to -55°, c = 0.3 in methanol
color	white to beige
solubility	DMSO: 2 mg/mL, clear
storage temp.	−20°C
SMILES string	O=C1N(C)C2=CC(N3CCNC[C@H]3C)=C(NC(C4=C(OC)C=CC=C4)=O)C=C2N1C

RIDADR	NONH for all modes of transport
WGK Germany	WGK 3
Flash Point F	Not applicable
Flash Point C	Not applicable