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GSK 4112 Sale

(Synonyms: SR6452) 目录号 : GC10715

An agonist of the heme-dependent nuclear receptor REV-ERBα

GSK 4112 Chemical Structure

Cas No.:1216744-19-2

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10mM (in 1mL DMSO)
¥620.00
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5mg
¥347.00
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10mg
¥672.00
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50mg
¥2,688.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: 2.3 μM

GSK4112 is a synthetic antagonist of the Nuclear Heme Receptor REV-ERB.

Rev-erbα and Rev-erbβ are heme sensors and atypical members of the nuclear receptor superfamily. As a member of the nuclear receptor superfamily, REV-ERBR functions as a receptor for the porphoryin heme. REV-ERBR can suppress the transcription of its target genes in a heme-dependent manner.

In vitro: Previous study showed that GSK4112 addition to either the REV-ERBR or REV-ERBβ assay led to enhanced repression. Cells were treated the with GSK4112 and similar pattern in GAL4 chimeric receptor assay was observed. In addition, GSK4112 suppressed reporter gene expression. GSK4112 also suppressed transcription driven by the Bmal1 promoter dose-dependently. GSK4112 activity was found to be associated with REV-ERBR [1].

In vivo: GSK4112 was found to display poor pharmacokinetic properties (rat liver microsomal Cint > 1.0 mL/min/mg protein; lack of oral bioavailability (F < 1% in mice)), which likely limited its use to biochemical and cell-based assays. As a result, GSK4112 was unlikely to be suitable for in vivo studies [1].

Clinical trial: N/A

Reference:
[1] Daniel Grant,Lei Yin,Jon L.  Collins et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear Heme receptor Rev-erbα. ACS CHEMICAL BIOLOGY5(10):925-32.

Chemical Properties

Cas No. 1216744-19-2 SDF
别名 SR6452
分子式 C18H21ClN2O4S 分子量 396.89
溶解度 ≥ 11.9mg/mL in DMSO 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。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.5196 mL 12.5979 mL 25.1959 mL
5 mM 0.5039 mL 2.5196 mL 5.0392 mL
10 mM 0.252 mL 1.2598 mL 2.5196 mL
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