2. Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling
  3. Acyltransferase STAT
  4. DM245

DM245 是一种 EPAC1 激活剂和 STAT3 磷酸化抑制剂，其靶点 pIC50 为 4.801。DM245 可激活 EPAC1 以提升 Rap1-GTP 水平，且不会激活 EPAC2 或 PKA。DM245 可降低内皮细胞中 IL-6/IL-6Rα 诱导的 STAT3 磷酸化水平。DM245 可抑制 TGF-β1 诱导的成纤维细胞向肌成纤维细胞转化，降低 αSMA 和 I 型胶原蛋白水。

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DM245

DM245 Chemical Structure

CAS No. : 3106606-60-1

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DM245 相关抗体

Top Publications Citing Use of Products

查看 Acyltransferase 亚型特异性产品:

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ACAT1 ACAT2 MGAT2 ACAT DGAT1

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor with a target pIC50 of 4.801. DM245 activates EPAC1 to increase Rap1-GTP levels, with no activation of EPAC2 or PKA. DM245 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM245 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing αSMA and Collagen I levels. DM245 exhibits minimal cytotoxicity in normal human lung fibroblasts, with negligible loss of intact nuclei after 72 h exposure[1].

IC50 & Target

p-STAT3

 

体外研究
(In Vitro)

DM245 与 EPAC1 CNBD 结合，pIC50 为 4.80，表明其对 EPAC1 环核苷酸结合域具有微摩尔级亲和力[1]。
DM245 (100 μM) 可在转染 EPAC1 的 U2OS 细胞中显著激活 EPAC1-Rap1 信号通路[1]。
DM245 (1 μM) 可显著减弱 HUVECs 中由 IL-6/IL-6Rα 诱导的 STAT3 磷酸化[1]。
DM245 (对数浓度范围；预处理 1 h，TGF-β1 刺激 72 h) 可抑制 TGF-β1 诱导的正常人肺成纤维细胞向肌成纤维细胞的转化，在抑制 αSMA (pIC50 = 4.58) 和 I 型胶原蛋白 (pIC50 = 4.34) 方面具有微摩尔级中等活性[1]。
DM245 (对数浓度范围；72 h) 在可有效抑制 TGF-β1 诱导的成纤维细胞向肌成纤维细胞转化的浓度下，对正常人肺成纤维细胞仅表现出极低的细胞毒性[1]。

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

DM245 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: normal human lung fibroblasts (Lonza, CC-512)
Concentration: logarithmic concentration range (same as fibroblast-to-myofibroblast transition assay)
Incubation Time: 72 h
Result: Showed minimal change in nuclear counts under matched conditions, with shallow or nonmeasurable cytotoxic concentration-response curves within the tested range.
分子量

415.44

Formula

C25H21NO5
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

DM245 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:

DM2453106606-60-1DM 245DM-245AcyltransferaseSTATDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseTGF-β1Rap1-GTPPKAfibroblast-to-myofibroblast transitionendothelial cellsnormal human lung fibroblastsEPAC1STAT3 phosphorylationEPAC2IL-6/IL-6RαInhibitorinhibitorinhibit

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