1. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  2. STAT Survivin Apoptosis
  3. STAT3-IN-38

STAT3-IN-38 (Compound 4m) 是一种 STAT3 抑制剂 (rhSTAT3 的 KD:45.33 µM),也是一个 Celastrol (HY-13067) 的衍生物。STAT3-IN-38 可结合 STAT3 蛋白的 SH2 结构域,抑制 STAT3 的 pTyr705 位点磷酸化及其下游基因 (SurvivinMcl-1) 表达。STAT3-IN-38 可阻断结直肠癌细胞的细胞周期并诱导其凋亡(Apoptosis)。

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STAT3-IN-38 Chemical Structure

STAT3-IN-38 Chemical Structure

CAS No. : 3033049-16-7

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查看 STAT 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STAT3-IN-38 (Compound 4m) is an inhibitor of STAT3 (KD of rhSTAT3: 45.33  µM). STAT3-IN-38 binds to the SH2 domain of STAT3 protein and suppresses the STAT3’s phosphorylation at site pTyr705 as well as its downstream genes (Survivin and Mcl-1). STAT3-IN-38 could block cell-cycle and induce Apoptosis in colorectal cancer cells[1].

IC50 & Target

STAT3

45.33 μM (Kd)

体外研究
(In Vitro)

STAT3-IN-38 (0.5-1 μM, 6 h) 可抑制 HCT116 细胞中 STAT3 的磷酸化,并降低 STAT3 靶蛋白 survivin 和骨髓细胞白血病 1 (Mcl-1) 的水平[1]
STAT3-IN-38 (0.02-12.5 μM, 48 h) 可抑制 A549、HCT116 和 HepG2 细胞的增殖[1]
STAT3-IN-38 (1-5 μM, 48 h) 可诱导 HCT116 细胞凋亡和细胞周期停滞[1]
STAT3-IN-38 (1-10 µM,6 天) 可降低人结直肠癌类器官组织 (CCOs) 的活力[1]

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

Cell Cycle Analysis[1]

Cell Line: HCT-116
Concentration: 1, 2.5, 5 μM
Incubation Time: 48 h
Result: Delayed cell cycle distribution, with a leading cell cycle arrest in G2/M phase at low concentrations and in S and G2/M phases at high concentrations.

Cell Cytotoxicity Assay[1]

Cell Line: A549、HCT-116、HepG2
Concentration: 0.02, 0.1, 0.5, 2.5, 12.5 μM
Incubation Time: 48 h
Result: Inhibited the proliferation of A549, HCT116, and HepG2 cells (IC50s = 0.93, 0.61, and 1.79 µM, respectively).

Western Blot Analysis[1]

Cell Line: HCT-116
Concentration: 0.5, 0.75, 1 μM
Incubation Time: 6 h
Result: Decreased the level of p-STAT3 at site pTyr705 in a concentration dependent manner, and the function was stronger than celastrol at 1.0 μM.
Down-regulated the level of Survivin and Mcl-1.
分子量

559.80

Formula

C35H45NO3S

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
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  • 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.

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产品名称:
STAT3-IN-38
目录号:
HY-169797
需求量: