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GSK6853

产品编号:4086164
规格:≥98% (HPLC)
CAS NO:1910124-24-1
包装规格:5 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品编号包装单位单价(元)国内现货国外库存询价单
40861645 MG1590
产品别名

1910124-24-1

GSK6853

(R)-N-(1,3-Dimethyl-6-(2-methylpiperazin-1-yl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide

N-[2,3-Dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide

结构式
基本信息
Empirical Formula【经验(实验)分子式】
C22H27N5O3
Molecular weight
409.48
MDL number
MFCD30489734
Biochem/physiol Actions【生化/生理作用】
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). For characterization details of GSK6853, please visit the GSK6853 probe summary on the Structural Genomics Consortium (SGC) website.

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【特点和优势】
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.
产品性质
Assay【测定】
≥98% (HPLC)
form【形式】
powder
optical activity【旋光性】
[α]/D -45 to -55°, c = 0.3 in methanol
color【颜色】
white to beige
solubility【溶解性】
DMSO: 2 mg/mL, clear
storage temp.【储存温度】
−20℃
SMILES string
O=C1N(C)C2=CC(N3CCNC[C@H]3C)=C(NC(C4=C(OC)C=CC=C4)=O)C=C2N1C
安全信息
Storage Class Code【储存分类代码】
13 - Non Combustible Solids
WGK
WGK 3
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