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GSK6853,≥98% (HPLC)

别名:(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

Empirical Formula (Hill Notation): C22H27N5O3 CAS号: 1910124-24-1 分子量: 409.48 MDL编号: MFCD30489734
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): SML1985
CAS号: 1910124-24-1
MDL号: MFCD30489734
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$303.07

说明

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
 
GSK6853 是一种 GSK5959 结构类似物,具有改善的水溶性(140 μg/mL 对 GSK5959 在 pH 7.4 PBS 中的 8 μg/mL)、对 BRPF1 溴结构域的亲和力(pKd = 9.5 对 GSK5959 的 8.0)、细胞功效(pIC50 对 7.7)。 GSK5959 为 6.0;针对 NanoLuc-BRPF1 溴结构域与 HEK293 细胞中组蛋白 H3.3-HaloTag 的相互作用)和选择性,对一组 48 个通道/受体/酶显示出很少或没有抑制效力,并且对其他通道的亲和力降低了 1600 倍以上 测试的溴结构域(在 GSK5959 的情况下 >90 倍),包括 BRPF2 (BRD1) 和 BRPF3 的溴结构域。 GSK6853 在小鼠体内通过腹腔注射给药时显示出良好的生物利用度(Cmax = 469 ng/mL,Tmax = 0.25 h,F = 85%;3 mg/kg i.p.)。 结构类似物 GSK9311 作为良好的无活性对照(在无细胞和基于细胞的测定中分别降低 125 和 185 倍的效力)。
 

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.
 

属性

测定

≥98% (HPLC)

形式

powder

旋光性

[α]/D -45 to -55°, c = 0.3 in methanol

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

−20°C

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

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16