2. Immunology/Inflammation
  3. AP-1
  4. JPC0661

JPC0661 是一种直接且变构的 ΔFOSB 抑制剂。JPC0661 以微摩尔级 IC50 值(9-52 μM) 抑制 ΔFOSB/JUND 和 ΔFOSB 与 DNA 的结合,在体外可直接抑制 ΔFOSB 介导的转录，其 IC50 值为 0.82 μM。JPC0661 在体内能显著降低 ΔFOSB 在基因组 AP1 位点的占据。JPC0661 通过结合于 ΔFOSB DNA 结合裂隙外的一个全新沟槽，破坏 ΔFOSB/JUND-DNA 复合物的形成。JPC0661 可用于阿尔茨海默病的研究。

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JPC0661

JPC0661 Chemical Structure

CAS No. : 30479-81-3

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JPC0661 相关抗体

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c-Fos FosB Fra1/FOSL1 Fra2/FOSL2 c-Jun

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JPC0661 is a direct and allosteric ΔFOSB inhibitor. JPC0661 inhibits the binding of ΔFOSB/JUND and ΔFOsB to DNA with IC50 values in the micromolar range (9-52 uM), directly inhibits ΔFOSB-mediated transcription with IC50 of 0.82 μM in vitro. JPC0661 significantly reduces ΔFOSB occupancy at genomic AP1 sites in vivo. JPC0661 binds to a novel groove outside the DNA-binding cleft of ΔFOSB and disrupt the formation of the ΔFOSB/JUND-DNA complex. JPC0661 can be used for Alzheimer's disease research[1].
IC50 & Target[1]

FosB

 

体外研究
(In Vitro)

JPC0661 (0-100 μM) 可调节 ΔFOSB 驱动的基因表达，其 IC50 值为 0.82 μM，并可在HEK293 细胞中诱导 ΔFOSB 蛋白积累[1]。
JPC0661 (0-100 μM，24 或 72 小时) 在神经祖细胞、AP1-luc HEK293 细胞以及 Neuro2A 细胞中均表现出良好的耐受性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

JPC0661 相关抗体:

Cell Viability Assay[1]

Cell Line: Neuronal progenitor cells (NPC)
Concentration: 0.16, 0.31, 0.63, 1.25, 2.5, 5.00, 10.00 and 20 μM,
Incubation Time: 24,72 h
Result: Observed no discernable decrease after 24 h and only minimal losses after 72 h.
体内研究
(In Vivo)

JPC0661 ( 50 μM，给药量为 16.7 ng/h，持续 3 天) 能在表达携带瑞典突变 (K670N, M671L) 和印第安纳突变 (V717F) 的人源淀粉样前体蛋白 (APP) 的杂合转基因雄性和雌性小鼠中，导致 ΔFOSB 在其大多数正常基因组定位位点上的结合出现显著且广泛的减少[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Heterozygous transgenic male and female mice (2-3 months)[1]
Dosage: 50 μM in 0.2% DMSO/0.9% saline with 0.96 μL/h
Administration: intra-hippocampal infusion for 3 days
Result: Exhibited an approximately 60% reduction in total binding sites.
Decreased average peak width.
Directly disrupted ΔFOSB–DNA interactions.
Caused a modest decline in promoter proximal peaks (≤1 kb) and a relative enrichment in distal intergenic peaks.
分子量

347.35

Formula

C15H13N3O5S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

JPC0661 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JPC066130479-81-3JPC 0661JPC-0661AP-1Activator Protein 1AP1ΔFOSB/JUND-DNA complexAlzheimer's diseaseΔFOSBInhibitorinhibitorinhibit

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