1. PI3K/Akt/mTOR Stem Cell/Wnt Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. GSK-3 CDK Lipoxygenase
  3. Indirubin-3'-monoxime

Indirubin-3'-monoxime  (Synonyms: Indirubin-3'-oxime)

目录号: HY-19807 纯度: 99.89%
COA 产品使用指南

Indirubin-3'-monoxime 是一种有效的 GSK-3β 抑制剂,对 5-Lipoxygenase 的抑制作用较弱,IC50 值分别为 22 nM 和 7.8-10 µM;Indirubin-3'-monoxime 同时对 CDK5/p25 和 CDK1/cyclin B 也有较强作用,IC50 值分别为 100 和 180 nM。

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Indirubin-3'-monoxime Chemical Structure

Indirubin-3'-monoxime Chemical Structure

CAS No. : 160807-49-8

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Other Forms of Indirubin-3'-monoxime:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.

IC50 & Target[1][3]

GSK-3β

22 nM (IC50)

CDK5/p25

100 nM (IC50)

CDK1/cyclin B

180 nM (IC50)

5-LOX

7.8-10 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
62 μM
Compound: Indirubin-3'-monoxime
Inhibitory activity on the proliferation of Human lung carcinoma A549 cancer cells using MTT or sulforhodamine B assay
Inhibitory activity on the proliferation of Human lung carcinoma A549 cancer cells using MTT or sulforhodamine B assay
[PMID: 15993584]
Cancer cell lines IC50
> 100 μM
Compound: Indirubin-3'-monoxime
Inhibitory activity on the proliferation of Human colon carcinoma Co12 cancer cells using MTT or sulforhodamine B assay
Inhibitory activity on the proliferation of Human colon carcinoma Co12 cancer cells using MTT or sulforhodamine B assay
[PMID: 15993584]
HCT-116 IC50
12 μM
Compound: 16
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
[PMID: 19783149]
Hep 3B2 IC50
9 μM
Compound: Indirubin-3'-oxime
Growth inhibition of human Hep3B cells after 72 hrs by MTS/PMS system based colorimetric assay
Growth inhibition of human Hep3B cells after 72 hrs by MTS/PMS system based colorimetric assay
[PMID: 25988923]
HL-60 IC50
> 100 μM
Compound: Indirubin-3'-monoxime
Inhibitory activity on the proliferation of Human myeloid leukemia HL-60 cancer cells using MTT or sulforhodamine B assay
Inhibitory activity on the proliferation of Human myeloid leukemia HL-60 cancer cells using MTT or sulforhodamine B assay
[PMID: 15993584]
HL-60 IC50
15.7 μM
Compound: 16
Antiproliferative activity against human HL60 cells after 5 days by MTT assay
Antiproliferative activity against human HL60 cells after 5 days by MTT assay
[PMID: 19783149]
HT-1080 IC50
4.8 μM
Compound: Indirubin-3'-monoxime
Inhibitory activity on the proliferation of Human fibrosarcoma HT1080 cancer cells using MTT or sulforhodamine B assay
Inhibitory activity on the proliferation of Human fibrosarcoma HT1080 cancer cells using MTT or sulforhodamine B assay
[PMID: 15993584]
IMR-90 IC50
18.2 μM
Compound: 16
Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
[PMID: 19783149]
K562 IC50
> 30 μM
Compound: 16
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
[PMID: 19783149]
KB IC50
19.2 μM
Compound: Indirubin-3'-oxime
Growth inhibition of human KB cells after 72 hrs by MTS/PMS system based colorimetric assay
Growth inhibition of human KB cells after 72 hrs by MTS/PMS system based colorimetric assay
[PMID: 25988923]
MCF7 IC50
25.5 μM
Compound: Indirubin-3'-oxime
Growth inhibition of human MCF7 cells after 72 hrs by MTS/PMS system based colorimetric assay
Growth inhibition of human MCF7 cells after 72 hrs by MTS/PMS system based colorimetric assay
[PMID: 25988923]
MKN-45 IC50
36.7 μM
Compound: Indirubin-3'-oxime
Growth inhibition of human MKN45 cells after 72 hrs by MTS/PMS system based colorimetric assay
Growth inhibition of human MKN45 cells after 72 hrs by MTS/PMS system based colorimetric assay
[PMID: 25988923]
MV4-11 IC50
0.15 μM
Compound: 10
Antiproliferative activity against wild type FLT3 expressing human MV411 cells after 72 hrs by WST8 assay
Antiproliferative activity against wild type FLT3 expressing human MV411 cells after 72 hrs by WST8 assay
[PMID: 20153646]
NCI-H460 IC50
32.6 μM
Compound: Indirubin-3'-oxime
Growth inhibition of human NCI-H460 cells after 72 hrs by MTS/PMS system based colorimetric assay
Growth inhibition of human NCI-H460 cells after 72 hrs by MTS/PMS system based colorimetric assay
[PMID: 25988923]
RS4-11 IC50
3.56 μM
Compound: 10
Antiproliferative activity against human RS4:11 cells having FLT3-ITD mutation after 72 hrs by WST8 assay
Antiproliferative activity against human RS4:11 cells having FLT3-ITD mutation after 72 hrs by WST8 assay
[PMID: 20153646]
SF-268 IC50
37 μM
Compound: Indirubin-3'-oxime
Growth inhibition of human SF268 cells after 72 hrs by MTS/PMS system based colorimetric assay
Growth inhibition of human SF268 cells after 72 hrs by MTS/PMS system based colorimetric assay
[PMID: 25988923]
SH-SY5Y IC50
> 25 μM
Compound: 7a
Survival of human SH-SY5Y cells after 24 hrs by MTS reduction assay
Survival of human SH-SY5Y cells after 24 hrs by MTS reduction assay
[PMID: 16854069]
SH-SY5Y IC50
> 25 μM
Compound: 7a
Death of human SH-SY5Y cells in presence of 20 uM Q-VD-OPh by MTS reduction assay
Death of human SH-SY5Y cells in presence of 20 uM Q-VD-OPh by MTS reduction assay
[PMID: 16854069]
SH-SY5Y IC50
12 μM
Compound: 7a
Survival of human SH-SY5Y cells after 48 hrs by MTS reduction assay
Survival of human SH-SY5Y cells after 48 hrs by MTS reduction assay
[PMID: 16854069]
SH-SY5Y IC50
13 μM
Compound: 7a
Death of human SH-SY5Y cells in absence of 20 uM Q-VD-OPh by MTS reduction assay
Death of human SH-SY5Y cells in absence of 20 uM Q-VD-OPh by MTS reduction assay
[PMID: 16854069]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL6-induced Stat1 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL6-induced Stat1 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL10-induced Stat3 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL10-induced Stat3 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated interferon-gamma-induced Stat1 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated interferon-gamma-induced Stat1 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL6-induced Stat3 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL6-induced Stat3 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL15-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL15-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL7-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL7-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL4-induced Stat6 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL4-induced Stat6 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL4-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL4-induced Stat5 phosphorylation in BALB/c mouse CD4+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL6-induced Stat1 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL6-induced Stat1 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL10-induced Stat3 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL10-induced Stat3 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL6-induced Stat3 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL6-induced Stat3 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL15-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL15-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL7-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL7-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL4-induced Stat6 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL4-induced Stat6 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
T-cell IC50
< 20 μM
Compound: 13, 13M
Inhibition of JAK-mediated IL4-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
Inhibition of JAK-mediated IL4-induced Stat5 phosphorylation in BALB/c mouse CD8+ T cells by Phospho-Flow cytometry
[PMID: 18157122]
体外研究
(In Vitro)

Indirubin-3'-monoxime 通过与 ATP 竞争抑制 GSK-3β,Ki 为 0.85 μM,Km 为 110 μM。Indirubin-3'-monoxime 还抑制由 GSK-3β 引起的 tau 磷酸化,IC50 值约为 100 nM。Indirubin-3'-monoxime 完全抑制 AT100 表位的磷酸化[1]
Indirubin-3'-monoxime 抑制血管平滑肌细胞 (VSMC) 增殖,IC50 为 ~2 μM。Indirubin-3'-monoxime 减弱了 PDGF 刺激的 VSMC 的迁移。Indirubin-3'-monoxime 干扰 VSMC 中的迁移反应,还抑制单核细胞中促迁移 LT 的产生。此外,Indirubin-3'-monoxime 抑制单核细胞和中性粒细胞中 5-脂氧合酶 (5-LO) 产物的合成,具有相同的效力 (IC50分别为 5.0±1.1 和 3.7±1.2 μM) . Indirubin-3'-monoxime 是 5-LO 的抑制剂,在无细胞试验中的 IC50 为 7.8-10 μM[3]

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

体内研究
(In Vivo)

Indirubin-3'-monoxime (0.1、0.2 和 0.4 mg/kg,ip) 剂量依赖性地逆转 HFD 喂养小鼠的认知障碍并对抗升高的氧化应激标志物。Indirubin-3'-monoxime 还可以剂量依赖性地降低血清葡萄糖、TG、TC 和胰岛素水平,并改善 HFD 喂养小鼠的 β 细胞功能。此外,与 HFD 组相比,Indirubin-3'-monoxime 处理显著降低了 HOMA-IR 水平。Indirubin-3'-monoxime (0.4 mg/kg) 显著减弱 HFD 组中增加的 EL[2]

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

分子量

277.28

Formula

C16H11N3O2

CAS 号
性状

固体

颜色

Brown to red

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (450.81 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6065 mL 18.0323 mL 36.0646 mL
5 mM 0.7213 mL 3.6065 mL 7.2129 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.02 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.89%

参考文献
Kinase Assay
[1]

GSK-3β is expressed in and purified from insect Sf9 cells. It is assayed, following a 1/100 dilution in 1 mg/mL BSA, 10 mM DTT, with 5 μL of 40 μM GS-1 peptide as a substrate, in buffer A, in the presence of 15 μM[γ-32P]ATP (3000 Ci/mmol; 1 mCi/mL) in a final volume of 30 μL. After 30-min incubation at 30°C, 25-μL aliquots of supernatant are spotted onto 2.5×3-cm pieces of Whatman P81 phosphocellulose paper, and, 20 s later, the filters are washed five times (for at least 5 min each time) in a solution of 10 mL of phosphoric acid/liter of water. The wet filters are counted in the presence of 1 mL of ACS scintillation fluid[1].

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

Cell Assay
[3]

Cytotoxicity of Indirubin-3'-monoxime in monocytes is analysed by MTT assay in a 96-well format using a multi-well scanning spectrophotometer. Neutrophils (5×106 cells/mL) or monocytes (2×106 cells/mL) are incubated for 30 min with Indirubin-3'-monoxime, and the viability of the cells is analysed by MTT assay. Compared with vehicle (0.3% DMSO), no significant acute cytotoxicity is observed (neutrophils: 103.9±4.4%; monocytes: 129.4±5.4%; n=3, each)[3].

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

Animal Administration
[2]

Male mice (5-6 weeks old) are randomLy assigned into five groups (n=10). Group 1: receive normal pellet diet (NPD); Group 2: receive a HFD; Group 3-5 receive HFD for 8 weeks followed by Indirubin-3'-monoxime treatment (0.1, 0.2 and 0.4 mg/kg i.p, respectively) once daily for 1 week. Indirubin-3'-monoxime is dissolved in (2.5% v/v) DMSO in saline. The mice in NPD and HFD groups receive an equivalent volume of vehicle (2.5% v/v DMSO in saline). Doses of Indirubin-3'-monoxime are selected. Mice are kept under standard husbandry conditions (22±1°C and 60% humidity) and maintained on a 12/12-h light/dark schedule with free access to food and water for 8 weeks. Body weight is recorded weekly throughout the experimental period[2].

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

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6065 mL 18.0323 mL 36.0646 mL 90.1616 mL
5 mM 0.7213 mL 3.6065 mL 7.2129 mL 18.0323 mL
10 mM 0.3606 mL 1.8032 mL 3.6065 mL 9.0162 mL
15 mM 0.2404 mL 1.2022 mL 2.4043 mL 6.0108 mL
20 mM 0.1803 mL 0.9016 mL 1.8032 mL 4.5081 mL
25 mM 0.1443 mL 0.7213 mL 1.4426 mL 3.6065 mL
30 mM 0.1202 mL 0.6011 mL 1.2022 mL 3.0054 mL
40 mM 0.0902 mL 0.4508 mL 0.9016 mL 2.2540 mL
50 mM 0.0721 mL 0.3606 mL 0.7213 mL 1.8032 mL
60 mM 0.0601 mL 0.3005 mL 0.6011 mL 1.5027 mL
80 mM 0.0451 mL 0.2254 mL 0.4508 mL 1.1270 mL
100 mM 0.0361 mL 0.1803 mL 0.3606 mL 0.9016 mL
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产品名称:
Indirubin-3'-monoxime
目录号:
HY-19807
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