Merck
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SML1985

Sigma-Aldrich

GSK6853

≥98% (HPLC)

All Photos(1)
Synonym(s):
(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 Number:
1910124-24-1
Molecular Weight:
409.48
MDL番号:
MFCD30489734

アッセイ

≥98% (HPLC)

形状

powder

光学活性

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

色

white to beige

溶解性

DMSO: 2 mg/mL, clear

保管温度

−20°C

SMILES string

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

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GSK6853 ≥98% (HPLC)

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GSK690693 ≥98% (HPLC)

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SML0428

GSK690693

GSK484 ≥98% (HPLC)

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SML1658

GSK484

GSK983 ≥98% (HPLC)

Sigma-Aldrich

SML1824

GSK983

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

powder

form

powder

color

white to beige

color

white to beige

color

white to beige

color

white to beige

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 5 mg/mL (clear solution)

solubility

H2O: 2 mg/mL, clear (warmed)

solubility

DMSO: 10 mg/mL, clear

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

optical activity

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

optical activity

-

optical activity

-

optical activity

[α]/D +175 to +195°, c = 1 in methylene chloride

生物化学的／生理学的作用

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

特徴および利点

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.

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable

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