2. Metabolic Enzyme/Protease PI3K/Akt/mTOR MAPK/ERK Pathway Apoptosis
  3. Acyltransferase mTOR Ribosomal S6 Kinase (RSK) Apoptosis
  4. AGPAT4-IN-1

AGPAT4-IN-1 (Compound CL26) 是一种共价 AGPAT4 抑制剂，其 IC50 为 795 nM。AGPAT4-IN-1 与 AGPAT4 的 Cys228 位点共价结合，显著抑制 acyltransferase 活性、LPA 到 PA 的转化以及下游 mTOR/S6K 通路。AGPAT4-IN-1 可增强肝细胞癌 (HCC) 肿瘤对 Sorafenib (HY-10201) 的敏感性，并通过协同反应显著诱导细胞凋亡 (apoptosis)。AGPAT4-IN-1 具有抗肿瘤活性，并可降低肝细胞癌异种移植小鼠模型中的致瘤性和干细胞特性。

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AGPAT4-IN-1

AGPAT4-IN-1 Chemical Structure

CAS No. : 2411250-59-2

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AGPAT4-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Acyltransferase 亚型特异性产品:

查看所有亚型
ACAT1 ACAT2 MGAT2 ACAT

查看 mTOR 亚型特异性产品:

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mTOR mTORC1 mTORC2

查看 Ribosomal S6 Kinase (RSK) 亚型特异性产品:

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p70S6K RSK2 RSK3 RSK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AGPAT4-IN-1 (Compound CL26) is a covalent AGPAT4 inhibitor with an IC50 of 795 nM. AGPAT4-IN-1 covalently binds to AGPAT4 at Cys228 and significantly inhibits acyltransferase activity, LPA-to-PA conversion and downstream mTOR/S6K pathways. AGPAT4-IN-1 sensitizes hepatocellular carcinoma (HCC) tumors to Sorafenib (HY-10201) and significantly induces apoptosis with a synergistic response. AGPAT4-IN-1 has antitumor activity and reduces tumorigenicity and stemness in HCC xenograft mouse models[1].

分子量

306.77

Formula

C14H11ClN2O2S
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

AGPAT4-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

AGPAT4-IN-12411250-59-2AcyltransferasemTORRibosomal S6 Kinase (RSK)ApoptosisDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseMammalian target of RapamycinS6KAGPAT4Cys228LPA-to-PA conversionmTOR/S6KHCCSynergistic responseAntitumorStemnessInhibitorinhibitorinhibit

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产品名称：
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