2. Stem Cell/Wnt TGF-beta/Smad
  3. TGF-beta/Smad
  4. TGF-β/Smad-IN-2

TGF-β/Smad-IN-2 是一种具有口服活性的 TGF-β/Smad 抑制剂。TGF-β/Smad-IN-2 抑制 TGF-β 诱导的成纤维细胞向肌成纤维细胞分化以及胶原沉积，在 LL29 细胞中对胶原减少的 IC50 值为 102 μM。TGF-β/Smad-IN-2 通过调节 SMAD3/SMAD7 信号通路发挥其作用。TGF-β/Smad-IN-2 降低肺纤维化小鼠的肺指数。TGF-β/Smad-IN-2 可用于肺纤维化的研究。

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TGF-β/Smad-IN-2

TGF-β/Smad-IN-2 Chemical Structure

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TGF-β/Smad-IN-2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TGF-β/Smad-IN-2 is an orally active TGF-β/Smad inhibitor. TGF-β/Smad-IN-2 inhibits TGF-β-induced fibroblast-to-myofibroblast differentiation and collagen deposition, with an IC50 value of 102 μM for collagen reduction in LL29 cells. TGF-β/Smad-IN-2 exerts its effects through modulation of the SMAD3/SMAD7 signaling pathway. TGF-β/Smad-IN-2 reduces lung index in pulmonary fibrosis mice. TGF-β/Smad-IN-2 can be used for the study of pulmonary fibrosis[1].

体外研究
(In Vitro)

TGF-β/Smad-IN-2 (Compound 10b) (50-100 μM, 48 h) 显著下调纤维化标志物 (FN1, α-SMA, COLLAGEN1α1, COLLAGEN3α1, TIMP1, VIMENTIN) 的 mRNA 表达，并抑制 LL29 细胞和 DHLF 细胞中 TGF-β 诱导的成纤维细胞向肌成纤维细胞分化[1].
TGF-β/Smad-IN-2 (50-100 μM, 48 h) 降低 DHLF 细胞中 α-SMA、COLLAGEN3α1 和 p-COFILIN 的蛋白水平，并在 TGF-β 刺激下恢复 E-CADHERIN 表达[1].

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

TGF-β/Smad-IN-2 相关抗体:

Real Time qPCR[1]

Cell Line: LL29 cells and DHLF cells
Concentration: 50,100 μM
Incubation Time: 48 h
Result: Downregulated mRNA expression of fibrotic markers (FN1, α-SMA, COLLAGEN1α1, COLLAGEN3α1, TIMP1, VIMENTIN).
体内研究
(In Vivo)

TGF-β/Smad-IN-2 (Compound 10b) (150-300 mg/kg，灌胃给药，每日一次，14 天) 改善 Bleomycin (BLMN) (HY-17565A) 诱导的肺纤维化 C57BL/6 小鼠的体重恢复和存活率，并降低肺指数[1].

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

Animal Model: BLMN (2 mg/kg in normal saline) was intratracheally administered to 6-week-old male C57BL/6 mice to establish the pulmonary fibrosis model[1]
Dosage: 150, 300 mg/kg
Administration: i.g., once daily, 14 days
Result: Achieved lung index reduction.
Showed no significant changes in body weight and no abnormal hematological parameters (RBC, WBC, hemoglobin, platelets) or pathological changes.
Reduced the mRNA and protein expression of fibrotic markers (FN1, α-SMA, COLLAGEN1α1, TIMP3) in lung tissues.
Appeared downregulation of phosphorylated Smad3 and upregulation of Smad7 in lung tissues.
Showed improvement in lung function (reduced respiratory resistance and elastance, increased quasi-static compliance).
Achieved reduction in collagen deposition in lung tissues.
分子量

284.35

Formula

C17H20N2O2
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

TGF-β/Smad-IN-2 相关分类

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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:

TGF-β/Smad-IN-2TGF-beta/SmadTransforming growth factor betapulmonary fibrosisTGF-β/SmadLL29 cellsDHLF cellsInhibitorinhibitorinhibit

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