HO-3867

For research use only. Not for use in humans.

目录号:S7501

HO-3867 Chemical Structure

CAS No. 1172133-28-6

HO-3867, 姜黄素的一种类似物, 是选择性的STAT3抑制剂。抑制STAT3的磷酸化、转录和DNA结合活性,而不影响其他活性STATs的表达。HO-3867 可诱导凋亡。

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RMB 1611.09 现货
RMB 4904.98 现货
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客户使用Selleck生产的HO-3867发表文献17篇:

客户使用该产品的4个实验数据:

  • Cell apoptosis as measured by TUNEL. Representative sections as determined at 12 hours after reperfusion (3100 magnification). Apoptotic nuclei were stained red, and the software of Image J was used to analyse quantity of TUNEL-positive cells in the livers. Scale bars5100 lm. *P<0.05, **P<0.01, ***P<0.001 compared with IR group.

    Liver Transpl, 2016, 22(12):1697-1709. HO-3867 purchased from Selleck.

  • The inhibitory effect of IL-6/IL-6R on TRPM7 currents is blocked by the STAT3 inhibitor HO-3867, but not by the inhibitor MAPK signaling pathway. (A) Relative currents normalized to TRPM7 currents recorded during perfusion with divalent-free extracellular solution. The specific STAT3 inhibitor HO-3867 did not inhibit TRPM7 inward currents at -100 mV, but blocked the effect of IL-6/sIL-6R (n = 3, * p < 0.05 vs. control, # p < 0.05 vs. IL-6/sIL-6R). (B) The specific MAPK−MEK inhibitor PD98059, did not inhibit TRPM7 inward currents at -100 mV, and did not block the effect of IL-6/sIL-6R (n = 3, * p < 0.05 vs. control). All currents were normalized to controls at -100 mV.

    PLOS ONE, 2016, 11(3): e0152120.. HO-3867 purchased from Selleck.

  • Inhibition of Stat3 activity on autophagy and hepatic IRI. (A) Pathological analyses showing that inhibition of Stat3 activity increased histopathologic injury in livers subjected to IRI treatment (×200). Scale bars=20μm. And quantified IR-induced liver injury by measuring Suzuki's score. (B) Levels of serum AST and ALT were increased when Stat3 activity was inhibited. (C) Quantitative analysis using TUNEL showing that inhibition of Stat3 activity increased hepatic apoptosis. (D) Immunohistochemistry showing that Cleaved caspase-3 expression increased when Stat3 was inhibited (magnification × 200). Scale bars=20μm. (E) Western blot analysis showing that ATG5 expression was decreased while Bax increased when the expression of p-stat3 (Tyr705) was decreased. (F) Quantitative analysis using transmission electron microscopy (TEM) showing that the number of autophagosomes per cross-sectioned cell were significantly decreased when Stat3 was inhibited. Each data point represents mean±standard deviation of three independent experiments. ***P < 0.001 vs 2h group.

    J Cell Biochem, 2018, 119(4):3440-3450. HO-3867 purchased from Selleck.

  • Interleukin (IL)-22-mediated protection against sodium nitroprussiate (SNP)-induced apoptosis in fibroblast-like synoviocytes established from rheumatoid arthritis (RA) patients (RA-FLS) is mediated by upregulation of the anti-apoptotic proteins Bcl2 and Bcl-xL. Cells were pretreated with HO-3867 (10 lmol/L) or STA21 (25 lmol/L) 2 h before the addition of IL-22 (100 ng/mL). Cells were then cultured for 30 min prior to the addition of SNP (1.33 mmol/L) and incubation for an additional 24 h. a. Western blot analysis of Bcl-2 protein expression in RA-FLS. A representative Western blot is shown in the left panel. Expression of Bcl-2 was quantified by densitometric analysis (right panel). Data represent the mean SD of three independent experiments. b. Western blot analysis of Bcl-xL in RA-FLS. A representative Western blot is shown in the left panel. Expression of Bcl-xL was quantified by densitometric analysis (right panel). Data represent the mean SD of three independent experiments. Each value is expressed as the ratio of the measured protein level to that of b-actin. *P < 0.05, #P > 0.05 versus control, &P < 0.05 versus SNP, %P < 0.05 versus SNP+ IL-22.

    Int J Rheum Dis, 2017, 20(2):214-224. HO-3867 purchased from Selleck.

产品安全说明书

STAT抑制剂选择性比较

生物活性

产品描述 HO-3867, 姜黄素的一种类似物, 是选择性的STAT3抑制剂。抑制STAT3的磷酸化、转录和DNA结合活性,而不影响其他活性STATs的表达。HO-3867 可诱导凋亡。
靶点
STAT3 [1]
体外研究

HO-3867在A2780和其他测试的卵巢癌细胞系中产生显著的细胞毒性, 对非癌卵巢上皮细胞的毒性较低。HO-3867诱导A2780细胞中G(2)-M细胞周期阻滞,并通过caspase-8 和caspase-3的活化促进细胞凋亡。HO-3867阻断人卵巢癌细胞系中JAK/STAT3通路。[1]

体内研究 HO-3867 (100 ppm,口服)抑制小鼠体内卵巢癌异种移植瘤的生长,而没有显著的毒性信号,会抑制pSTAT3,并下调STAT3靶向蛋白。[1] HO-3867通过对STAT3的抑制使顺铂耐药性卵巢癌敏感化。[2] HO-3867 (100 ppm 口服) 通过减少氧化应激并增加PTEN在大鼠肺中的表达,减弱左心室衰竭诱发的肺动脉高血压。 [3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • Cell lines: A2780 (A2780R),PA-1,SKOV3,OV4,和 OVCAR3 细胞;人卵巢表面上皮细胞
  • Concentrations: ~20 μM
  • Incubation Time: 24小时
  • Method:

    细胞活性使用MTT通过比色法测定。在活细胞线粒体中,黄色MTT被还原转化为甲瓒,变为紫色。细胞在75毫米烧饼中生长为~80%覆盖率,将其胰蛋白化,计数,以7,000细胞/孔的平均密度接种于96孔板,培育过夜,然后用HO-3867处理24小时。所有实验使用8份相同的测试样品进行,每次至少进行3次。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 负荷卵巢癌 A2780 肿瘤异种移植物的小鼠
  • Dosages: ~100 ppm
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 13 mg/mL warmed (27.98 mM)
Ethanol 6 mg/mL warmed (12.91 mM)
Water Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 464.55
化学式

C28H30F2N2O2

CAS号 1172133-28-6
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID