GSK-3 Inhibitor IX (BIO)
(Synonyms: (2'Z,3'E)-6-溴靛玉红-3'-肟,GSK-3 Inhibitor IX) 目录号 : GC14987
GSK-3 Inhibitor IX (BIO)是一种强效、选择性和可逆的糖原合成酶激酶-3（GSK-3）抑制剂，对GSK-3α/β的IC50值为5nM。
Cas No.:667463-62-9
Sample solution is provided at 25 µL, 10mM.
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GSK-3 Inhibitor IX (BIO) is a potent, selective and reversible inhibitor of glycogen synthase kinase-3 (GSK-3) with an IC50 value of 5nM for GSK-3α/β[1]. GSK-3 is a serine/threonine protein kinase and one of the protein kinases with the most substrates in cells. GSK-3 is associated with a variety of diseases, such as cancer, Alzheimer's disease, bipolar disorder (BPD), Parkinson's disease, aging, inflammation and metabolic diseases[2]. GSK-3 Inhibitor IX is the first pharmacological agent that can maintain the self-renewal of human and mouse embryonic stem cells (ESCs)[3]. GSK-3 Inhibitor IX can promote the proliferation of mammalian cardiomyocytes[4].
In vitro, GSK-3 Inhibitor IX (0-20µM) treated human melanoma cells (A2058 cells) for 24h reduced cell viability in a dose-dependent manner with an IC50 value of approximately 5µM, reduced the expression of the anti-apoptotic protein Mcl-1 in the cells, and inhibited the phosphorylation of Janus-activated kinase (JAK) family members JAK1, JAK2, and TYK2[5].
In vivo, GSK-3 Inhibitor IX (50mg/kg/day) was orally treated for 2 weeks in mice bearing melanoma cell xenografts, significantly inhibiting tumor growth in the mice[5].
References:
[1] Meijer L, Skaltsounis A L, Magiatis P, et al. GSK-3-selective inhibitors derived from Tyrian purple indirubins[J]. Chemistry & biology, 2003, 10(12): 1255-1266.
[2] Wang L, Li J, Di L. Glycogen synthesis and beyond, a comprehensive review of GSK3 as a key regulator of metabolic pathways and a therapeutic target for treating metabolic diseases[J]. Medicinal research reviews, 2022, 42(2): 946-982.
[3] Zhu H, Liu C, Sun J, et al. Effect of GSK-3 inhibitor on the proliferation of multipotent male germ line stem cells (mGSCs) derived from goat testis[J]. Theriogenology, 2012, 77(9): 1939-1950.
[4] Tseng A S, Engel F B, Keating M T. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes[J]. Chemistry & biology, 2006, 13(9): 957-963.
[5] Liu L, Nam S, Tian Y, et al. 6-Bromoindirubin-3′-oxime inhibits JAK/STAT3 signaling and induces apoptosis of human melanoma cells[J]. Cancer research, 2011, 71(11): 3972-3979.
GSK-3 Inhibitor IX (BIO)是一种强效、选择性和可逆的糖原合成酶激酶-3（GSK-3）抑制剂，对GSK-3α/β的IC50值为5nM[1]。GSK-3是一种丝氨酸/苏氨酸蛋白激酶，是细胞中底物最多的蛋白激酶之一，GSK-3与多种疾病有关，例如癌症、阿尔茨海默氏病、双相情感障碍（BPD）、帕金森氏病、衰老、炎症和代谢疾病等[2]。GSK-3 Inhibitor IX是第一种能够维持人和小鼠胚胎干细胞（ESC）自我更新的药理学试剂[3]。GSK-3 Inhibitor IX能够促进哺乳动物心肌细胞增殖[4]。
在体外，GSK-3 Inhibitor IX（0-20µM）处理人黑色素瘤细胞（A2058细胞）24h，以剂量依赖性方式降低了细胞活力，IC50值约为5µM，降低了细胞内抗凋亡蛋白Mcl-1的表达，抑制了Janus激活激酶（JAK）家族JAK1、JAK2和TYK2的磷酸化[5]。
在体内，GSK-3 Inhibitor IX（50mg/kg/day）通过口服治疗黑色素瘤细胞异种移植小鼠2周，显著抑制了小鼠体内肿瘤的生长[5]。
| Cell experiment [1]: | |
Cell lines | A2058 cells |
Preparation Method | Cells were seeded on 6-well plates with 50,000 cells per well in 3mL of RPMI 1640 medium supplemented with 10% FBS and 1% P/S. After 24h incubation, cells were treated with 0-20µM GSK-3 Inhibitor IX (BIO) for 24h. Cell viability was determined using the MTS assay. |
Reaction Conditions | 0-20µM; 24h |
Applications | A2058 human melanoma cells are sensitive to GSK-3 Inhibitor IX (BIO) with an IC50 value of approximately 5μM. |
| Animal experiment [1]: | |
Animal models | Immunodeficient NOD/SCID/IL2Rgamma null (NSG) mice |
Preparation Method | A2058 human melanoma cells at a density of 5×106 cells in serum-free medium were inoculated subcutaneously into the dorsal area of NSG mice to create the xenograft model. When tumors became palpable, GSK-3 Inhibitor IX (BIO) or vehicle control was administered via oral gavage once daily at a dose of 50mg/kg body weight once daily for 2 weeks. Tumor growth was monitored every other day. Tumor volumes were measured every 3 to 4 days. |
Dosage form | 50mg/kg/day; 2 weeks; p.o. |
Applications | GSK-3 Inhibitor IX (BIO) suppresses melanoma tumor growth in a mouse xenograft model. |
References: | |
| Cas No. | 667463-62-9 | SDF | |
| 别名 | (2'Z,3'E)-6-溴靛玉红-3'-肟,GSK-3 Inhibitor IX | ||
| 化学名 | 6-bromo-3-[3-(hydroxyamino)indol-2-ylidene]-1H-indol-2-one | ||
| Canonical SMILES | C1=CC2=C(C(=C3C4=C(C=C(C=C4)Br)NC3=O)N=C2C=C1)NO | ||
| 分子式 | C16H10BrN3O2 | 分子量 | 356.17 |
| 溶解度 | ≥ 35.6 mg/mL in DMSO, ≥ 14.4 mg/mL in EtOH with gentle warming | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8076 mL | 14.0382 mL | 28.0765 mL |
| 5 mM | 0.5615 mL | 2.8076 mL | 5.6153 mL |
| 10 mM | 0.2808 mL | 1.4038 mL | 2.8076 mL |
| 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 | 只 |
| 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet