GSK983

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK983 (GSK-983) 是一种有效的细胞渗透性 PCAF/GCN5 PROTAC，可诱导 THP1 细胞中 PCAF 和 GCN5 的浓度依赖性降解，DC50 值分别为 1.5 nM 和 3 nM。

GSK983 (GSK-983) is a potent, cell penetrant PCAF/GCN5 PROTAC, induces concentration-dependent degradation of PCAF and GCN5 in THP1 cells with DC50 value of 1.5 nM and 3 nM, respectively; also potently induces robust and concentration-dependent degradation of PCAF and GCN5 in both macrophages and monocyte-derived dendritic cells (DCs), potently modulate the expression of multiple inflammatory mediators in LPS-stimulated macrophages and dendritic cells.

RT-PCR Cell Line:W12, HKC cells Concentration:10, 100 nM Incubation Time:24, 48 h Result:Induced the expression of interferon-stimulated genes in infected and immortalized cells, increased the gene expression of CSF2, IFIT1 (ISG56), IL6, ISG15, OAS1, OAS2, OASL and TNFSF10 (TRAIL).

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GSK-983 | GSK 983

PROTACs

PROTAC

PROTAC

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827591-02-6

895.856

C45H51BrN8O7

>98% (HPLC)

In Vitro:?DMSO : ≥ 10 mg/mL (30.69 mM)

O=C(N[C@H]1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)C4=NC=CC=C4

4-(5-((5-bromo-1-methyl-6-oxo-1,6-dihydropyridazin-4-yl)amino)-1-methylpiperidin-3-yl)-N-(3-((4-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)propyl)phenyl)(methyl)amino)propyl)-N-methylbenzamide

(-20℃)

With Ice Pack

≥ 2 years