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9-ING-41
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
9-ING-41图片
CAS NO:1034895-42-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
9-ING-41 是一种基于马来酰亚胺的 ATP 竞争性和选择性的糖原合酶激酶-3β (GSK-3β) 抑制剂,IC50为 0.71 μM。9-ING-41 显著导致癌细胞的细胞周期停滞,自噬和凋亡。9-ING-41 具有抗癌活性,并具有增强化疗药物抗肿瘤作用的潜力。
生物活性

9-ING-41 is a maleimide-based ATP-competitive and selectiveglycogen synthase kinase-3β (GSK-3β)inhibitor with anIC50of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest,autophagyandapoptosisincancercells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs[1][2][3][4].

IC50& Target[1]

GSK-3β

0.71 μM (IC50)

体外研究
(In Vitro)

9-ING-41 (2, 4 μM; 48 hours) decreases neuroblastoma cell viability induces apoptosis[2].
9-ING-41 (1, 2 μM; 24 hours) is a potent cell cycle-blocking agent for lymphoma cells[2].
9-ING-41 (10 μM; for 72 hours) increases the expression of LC3, an autophagy marker[3].
9-ING-41 (compound 26; 5 μM; for 6, 12, 24, 36 h) results in a pronounced decrease in NFκB-mediated expression of XIAP, the most potent antiapoptotic protein, leading to subsequent apoptosis in BXPC3 pancreatic cancer cells[1].
9-ING-41 (0.5, 1.0, 1.5, 2.0 μM) inhibits the proliferation rate of all TCL and MCL lines with concentrations as low as 1.0 mM[2].
9-ING-41 (10 μM; for 72 hours) causes cell cycle blockage at G2/M after 24 hours. 9-ING-41 treatment induces apoptotic cell death in bladder cancer cells[3].
9-ING-41 (25 μM; for 96 hours) significantly decreases expression of Cdk1 and Cyclin B1 proteins and leads to a decreased expression of antiapoptotic molecules, Bcl-2 and XIAP[3].
9-ING-41 (0.1-1 μM) inhibits GSK-3 leading to a decreased expression of the NF-κB target XIAP and significant apoptosis in neuroblastoma cells as shown by PARP cleavage, an apoptosis marker[4].

Cell Viability Assay[2]

Cell Line:TCL and MCL lines
Concentration:2, 4 μM
Incubation Time:48 hours
Result:Induced apoptosis.

Cell Cycle Analysis[2]

Cell Line:Lymphoma cells (Jeko, Mino, and OCI-Ly cell lines)
Concentration:1, 2 μM
Incubation Time:24 hours
Result:Led to cell cycle arrest in G2/M.

Cell Autophagy Assay[3]

Cell Line:T24 cancer cells
Concentration:25 μM
Incubation Time:24 hours
Result:Showed extensive vacuolation and formation of autophagosome like structures in the cytoplasm.
Showed an increased expression of LC3, an autophagy marker.

Western Blot Analysis[4]

Cell Line:SK-N-DZ and SK-N-BE neuroblastoma cells
Concentration:0.1, 1 μM
Incubation Time:48 hours
Result:Inhibited GSK-3 leading to a decreased expression of the NF-κB target XIAP.
体内研究
(In Vivo)

9-ING-41 (40 mg/kg/every other day; for 17 days) has single-agent antitumor activity in a mouse model of MCL[2].

Animal Model:NSG (NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ) mice[2]
Dosage:40 mg/kg
Administration:Every other day; for 17 days
Result:Had single-agent antitumor activity in a mouse model of MCL.
Clinical Trial
分子量

404.35

性状

Solid

Formula

C22H13FN2O5

CAS 号

1034895-42-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(123.66 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4731 mL12.3655 mL24.7310 mL
5 mM0.4946 mL2.4731 mL4.9462 mL
10 mM0.2473 mL1.2366 mL2.4731 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

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

  • 1.

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

    Solubility: 2.5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.18 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。