1. JAK/STAT Signaling NF-κB Immunology/Inflammation
  2. Pim NF-κB Interleukin Related
  3. PIM1-IN-8

PIM1-IN-8 是一种 PIM1/p65 通路抑制剂。PIM1-IN-8 抑制活化成纤维细胞中 α-SMA 和 I 型胶原的表达,并阻断 TGF-β 诱导的迁移。PIM1-IN-8 在 Bleomycin (BLM) (HY-17565A) 诱导的肺纤维化小鼠模型中缓解肺纤维化。PIM1-IN-8 可用于特发性肺纤维化 (IPF) 的研究。

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PIM1-IN-8

PIM1-IN-8 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PIM1-IN-8 is a PIM1/p65 pathway inhibitor. PIM1-IN-8 suppresses the expression of α-SMA and collagen I in activated fibroblasts and blocks TGF-β induced migration. PIM1-IN-8 alleviates pulmonary fibrosis in a Bleomycin (BLM) (HY-17565A)-induced pulmonary fibrosis mice model. PIM1-IN-8 can be used for the study of idiopathic pulmonary fibrosis (IPF)[1].

体外研究
(In Vitro)

PIM1-IN-8 (Compound B6) (20-50 μM, 48 h) 在 TGF-β (10 ng/mL) 诱导的 NIH-3T3 细胞中显示出抑制活性 (IR = 91.2),并在 GES-1 细胞中具有高细胞存活率 (VR = 99.7)[1]
PIM1-IN-8 (3.125-100 μM, 24-48 h) 在浓度 ≥ 50μM 时抑制 NIH-3T3 和 GES-1 细胞中的成纤维细胞活化和增殖[1]
PIM1-IN-8 (2.5-10 μM) 显著抑制 NIH-3 T3 细胞中 α-SMA 和 I 型胶原的表达[1]
PIM1-IN-8 (2.5-10 μM,24 h) 阻断 A549 细胞中 TGF-β 诱导的迁移[1]

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

Cell Viability Assay[1]

Cell Line: NIH-3 T3 and Ges-1 cells
Concentration: 3.125, 6.25, 12.5, 25, 50, 100 μM
Incubation Time: 24, 48 h
Result: Inhibited fibroblast activation and proliferation in NIH-3 T3 and Ges-1 cells.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Blocked TGF-β induced migration in A549 cells
体内研究
(In Vivo)

PIM1-IN-8 (Compound B6) (10-40 mg/kg,腹腔注射,连续给药 14 天) 在 Bleomycin (BLM) (HY-17565A) 诱导的肺纤维化小鼠模型中减轻肺纤维化[1]

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

Animal Model: Lung fibrosis was induced in male C57BL/6 mice (8-10 weeks old, 18-22 g) using Bleomycin (BLM) at a dose of 3 mg/kg.[1]
Dosage: 10, 20, 40 mg/kg
Administration: i.p. daily for 14 days
Result: Did not show toxicity at 500 mg/kg oral administration in mice.
Alleviated lung structural damage, including alveolar space collapse, thickened alveolar septa, and substantial collagen deposition.
Inhibited the expression of collagen I and α-SMA.
Reduced the levels of P21 and P16 in the lung tissue of IPF mice treated to 0.42 and 0.65, respectively.
Reduced the levels of IL-1β, IL-6 and the phosphorylation of P65.
Increased the levels of IL-10.
分子量

299.32

Formula

C17H17NO4

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
PIM1-IN-8
目录号:
HY-175277
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