AS1842856

For research use only. Not for use in humans.

目录号:S8222

AS1842856 Chemical Structure

CAS No. 836620-48-5

AS1842856 是具有细胞可透性的抑制剂,抑制Foxo1的转录活性,IC50=33 nM。AS1842856 可直接结合活化的Foxo1,但不结合Ser256位磷酸化的Foxo1。AS1842856 可抑制自噬。

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客户使用Selleck生产的AS1842856发表文献13篇:

客户使用该产品的4个实验数据:

  • (E-F) Images and results from microfluidic devices containing human kidney capillaries from young healthy kidneys (n = 6 per group, 2 donors) (E) or aged hypertensive kidneys (n = 5 per group, 1 donor) (F), stimulated to undergo sprouting angiogenesis with VEGF. In the presence of the FOXO1 inhibitor AS1842856 both healthy capillaries and aged capillaries successfully form new capillaries with tip-stalk structures. FOXO1 inhibition enables angiogenic capacity in kidney MVECs like that seen in HUVECs. Capillaries engineered from aged hypertensive kidneys had a higher tendency to form new vascular structures, although these did not show tip cell morphology (F, lower left images). FOXO1 inhibition enhanced new vessel formation with obvious tip cell morphology. Note bpV was less effective in aged capillary.

    Biomaterials, 2017, 141:314-329. AS1842856 purchased from Selleck.

  • (B) The effects of inactivating FOXO1 and Bcl2 on myoblast apoptosis. AnnexinV-FITC-PI detection method was employed for the detection of apoptotic cells by flow cytometry. PI was used as a counterstain to discriminate dead cells from apoptotic ones. The ratio of apoptotic cells was calculated based on AnnexinV and PI straining. Q1 represents the necrotic cell potion, Q2: apoptotic cells in the late stage; Q3: apoptotic cells in the early stage; Q4: normal cells. (C) The plot of cell proliferation analysis in different cell cycles. (D) The plot of cell apoptosis analysis in different stages. AS1842856 (FOXO1 inhibitor) and ABT199 (Bcl2 inhibitor) were utilized for specific knockdown of FOXO1 and Bcl2 activities in myoblast for 24 h at the concentration of 10 μM with equal volume of DMSO as control groups (n = 4). *P b 0.05; **P b 0.01.

    Biochim Biophys Acta Gene Regul Mech, 2017, 1860(6):674-684. AS1842856 purchased from Selleck.

  • AS1842856 treatment on the mRNA levels of gluconeogenic genes in Ad‐PANDER‐infected HepG2 cells.

    J Cell Mol Med, 2018, doi:10.1111/jcmm.14073. AS1842856 purchased from Selleck.

  • The plot of cell proliferation analysis in different cell cycles. Foxo1 inhibitor: AS1842856

    Biochim Biophys Acta, 2017, 1860(6):674-684. AS1842856 purchased from Selleck.

产品安全说明书

FOX抑制剂选择性比较

生物活性

产品描述 AS1842856 是具有细胞可透性的抑制剂,抑制Foxo1的转录活性,IC50=33 nM。AS1842856 可直接结合活化的Foxo1,但不结合Ser256位磷酸化的Foxo1。AS1842856 可抑制自噬。
靶点
Foxo1 [1]
(In HepG2 cells)
33nM
体外研究

AS1842856通过直接与Foxo1结合,抑制了Foxo1所介导的反式激活。在瞬时转染了Foxo1表达载体的HepG2细胞中,AS1842856有效地抑制了Foxo1介导的启动子活性,这一具有剂量依赖性的效果类似于胰岛素处理效果。0.1 μM AS1842856分别抑制了3% Foxo3a-和20% Foxo4-介导的启动子活性。相反地,Foxo1介导的启动子活性降低了70%。Foxo1 抑制剂AS1842856可能通过降低G6Pase和PEPCK的mRNA水平,抑制内源性G6Pase和PEPCK活性,这可能抑制Fao细胞中葡萄糖的生成[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3L1 preadipocytes MoPSSpVv[3Srb36gZZN{[Xl? M2\PUFEvOMLizszN NF7LXWUyOiCmYYnz M2K4O5BmenOrc4TlcpQhfHKnYYTt[Y51KG:oIHPlcIx{KHerdHigRXMyQDR{OEW2JEhl[Xm|IECtNVIqKGGubX;zeEBkd22ybHX0[Yx6KHC{ZY\lcpRm\CC2aHWgZYRqeG:pZX7ld4l{ MXqyOVQ5OzB6NB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-JNK / JNK / p-P38 / P38 / p-ERK / ERK ; 

PubMed: 26568463     


Levels of p-JNK and p-P38 were increased by AS1842856 in RAW264.7 cells. After treatment with AS1842856 (at a concentration of 0.1, 0.5 or 1.0 μM) for 12 h, RAW264.7 cells were incubated with RANKL (50 ng/mL) for 30 min. Total proteins were then extracted for Western blot analysis. Antibodies to ACTB and total JNK, p38 and ERK served as loading controls.

FoxO1 / FoxO3a / FoxO4 ; 

PubMed: 30404794     


Detection of the FoxO1, FoxO3a, and FoxO4 proteins in iSLK-RGB-BAC16 cells treated with 0 (DMSO alone), 5, 7, and 10 μM FoxO1 inhibitor AS1842856 for 48 h. 

Sox2 / Musashi / Nestin / GFAP ; 

PubMed: 27448972     


Western blot analyses of stemness markers and GFAP after incubation with 10 μM of the FoxO inhibitor AS1842856.

26568463 30404794 27448972
体内研究 对患有糖尿病的db/db突变小鼠施以口服AS1842856,通过抑制肝脏糖异生相关基因,导致其空腹血糖值大幅度下降。正常小鼠口服AS1842856后则无此影响。处理以AS1842856还会抑制由于注射丙酮酸酯(正常小鼠以及db/db小鼠)所引起的血糖水平的上升[1]

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: Fao细胞
  • Concentrations: 0, 0.1, 1, 10 μM
  • Incubation Time: 30 min
  • Method: Fao细胞进行血清饥饿1小时,然后加入胰岛素或者AS1842856 共同孵育30分钟。从这些处理过的细胞中提取蛋白溶解产物,通过Western blot来分析磷酸化Foxo1蛋白水平。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: db/db小鼠, ICR小鼠
  • Dosages: 100 mg/kg
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 23 mg/mL (66.2 mM)
Water Insoluble
Ethanol 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 347.38
化学式

C18H22FN3O3

CAS号 836620-48-5
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、MSDS / 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、MSDS / 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID