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GSK6853 Sale

目录号 : GC13025

A selective chemical probe for the bromodomain of BRPF1

GSK6853 Chemical Structure

Cas No.:1910124-24-1

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5mg
¥711.00
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10mg
¥1,260.00
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25mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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产品描述

pIC50: 8.1

GSK6853 is a BRPF1 inhibitor.

The BRPF (Bromodomain and PHD Fingercontaining) protein family are key scaffolding proteins for assembly of MYST histone acetyltransferase complexes.

In vitro: In previous study, GSK6853 was tested in the BROMOscan panel of bromodomain binding assays and the results showed that consistent with the previous findings, it showed excellent BRPF1 potency (pKd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested. In addition, screening GSK6853 against a panel of 48 unrelated assays revealed only off-target activities that were relatively weak compared to its high BRPF1 potency [1].

In vivo: To assess the suitability of GSK6853 for in vivo studies, its DMPK characteristics were studied in male CD1 mice by i.v., po, and i.p. administration. The results indicated that the i.p. route of administration would be suitable for dosing this molecule in further PK/PD models. Moreover, in order to be able to compare biochemical potency measurements to free blood concentrations, the fraction unbound in the CD1 mouse was also tested with a resulting value of 7.9% [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Bamborough, P. ,Barnett, H.A.,Becher, I., et al. GSK6853, a chemical probe for inhibition of the BRPF1 bromodomain. ACS Med. Chem. Lett. 7(6), 552-557 (2016).

Chemical Properties

Cas No. 1910124-24-1 SDF
化学名 N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-benzamide
Canonical SMILES C[C@H](CNCC1)N1C2=C(NC(C3=CC=CC=C3OC)=O)C=C4C(N(C)C(N4C)=O)=C2
分子式 C22H27N5O3 分子量 409.5
溶解度 ≤30mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mg 5 mg 10 mg
1 mM 2.442 mL 12.21 mL 24.42 mL
5 mM 0.4884 mL 2.442 mL 4.884 mL
10 mM 0.2442 mL 1.221 mL 2.442 mL
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