GSK 3 Inhibitor IX
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Cat.No：IB0690 Solarbio
CAS：667463-62-9
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > PI3K/Akt/mTOR > GSK 3 Inhibitor IX
Product Information
| CAS | 667463-62-9 |
| Name | GSK 3 Inhibitor IX |
| Molecular Formula | C16H10BrN3O2 |
| Molecular Weight | 356.17 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD08705318 |
| SMILES | O/N=C(C1=CC=CC=C1N2)/C2=C3C(NC4=C/3C=CC(Br)=C4)=O |
| InChIKey | SAQUSDSPQYQNBG-UHFFFAOYSA-N |
| InChI | InChI=1S/C16H10BrN3O2/c17-8-5-6-9-12(7-8)19-16(21)13(9)15-14(20-22)10-3-1-2-4-11(10)18-15/h1-7,18-19,21H |
| PubChem CID | 448949 |
| Target Point | GSK-3;CDK |
| Passage | PI3K/Akt/mTOR;Stem Cells |
| Background | GSK 3 Inhibitor IX is a potent, selective, reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complexes. |
| Biological Activity | GSK 3 Inhibitor IX 是一种有效的，选择性的，可逆的，ATP 竞争性的 GSK-3α/β 和 CDK1-cyclinB 复合体抑制剂，能够抑制 (GSK-3α/β)/CDK1/CDK5 的活性，IC50 值分别为 5 nM/320 nM/83 nM[1-4]。 |
| In Vitro | GSK 3 Inhibitor IX是糖原合成酶激酶-3(GSK-3)的特异性抑制剂，GSK-3α/β的IC50为5 nM，对CDK5的选择性> 16倍。 GSK 3 Inhibitor IX在这些激酶的ATP结合口袋内相互作用，降低细胞模型中GSK-3特异性位点上的β-连环蛋白磷酸化，非常模仿非洲爪蟾胚胎中的Wnt信号传导[1]。在人和小鼠胚胎干细胞中，GSK 3 Inhibitor IX维持未分化的表型并维持多能状态特异性转录因子Oct-3/4，Rex-1和Nanog的表达。 GSK 3 Inhibitor IX介导的Wnt激活在功能上是可逆的，因为化合物的撤回导致人和小鼠胚胎干细胞中的正常多分化程序[2]。 GSK 3 Inhibitor IX促进哺乳动物心肌细胞的增殖[3]。GSK 3 Inhibitor IX也是pan-JAK抑制剂，TYK2，JAK1，JAK2和JAK3的IC50值分别为0.03，1.5，8.0，0.5μM。 GSK 3 Inhibitor IX选择性抑制STAT3的磷酸化并诱导人黑素瘤细胞的凋亡[4]。 |
| In Vivo | GSK 3 Inhibitor IX(50mg/kg，po)在小鼠异种移植模型中抑制黑素瘤肿瘤生长[4]。 |
| Cell Experiment | COS1，Hepa(野生型，CEM/LM AhR缺陷型和ELB1 ARNT缺陷型)或SH-SY5Y细胞在含有10％胎牛血清的Dulbecco改良培养基(DMEM)中的6cm培养皿中生长。用于治疗，IO(5μM)，GSK 3 Inhibitor IX(5或10μM)，MeBIO(5或50μM)，LiCl(20或40mM)或模拟溶液(DMSO，0.5％终浓度)当细胞密度达到约70％汇合时，添加到培养基中。在12(SH-SY5Y)或24小时后，仍然在平板中的细胞用裂解缓冲液(1％SDS，1mM原钒酸钠，10mM Tris [pH 7.4])裂解。将裂解物通过26G针头数次，以10，000×g离心5分钟，并调节至相等的蛋白质浓度。加载约8μg的每种样品用于免疫印迹。增强的化学发光用于检测。使用以下一抗：小鼠抗β-连环蛋白CT，小鼠抗磷酸-β-连环蛋白，小鼠抗GSK-3β，小鼠抗GSK-3磷酸化Tyr216，兔抗AhR(芳基烃受体)，和兔抗肌动蛋白。 |
| Animal Experiment | 将无血清培养基中5×10 6个细胞的A2058人黑素瘤细胞皮下接种到NSG小鼠的背部区域以产生异种移植模型。当肿瘤变得可触知时，通过口服管饲法以50mg/kg体重每天一次施用6GSK3抑制剂IX(BIO)或媒介物对照。每隔一天监测肿瘤生长。每3至4天测量肿瘤体积。 |
| Data Literature Source | [1]. Meijer L，et al. GSK-3-selective inhibitors derived from Tyrian purple indirubins. Chem Biol. 2003 Dec;10(12):1255-66. [2]. Sato N，et al. Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor. Nat Med. 2004 Jan;10(1):55-63. Epub 2003 Dec 21. [3]. Tseng AS，et al. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chem Biol. 2006 Sep;13(9):957-63. [4]. Liu L1，et al. 6-Bromoindirubin-3'-oxime inhibits JAK/STAT3 signaling and induces apoptosis of human melanoma cells. Cancer Res. 2011 Jun 1;71(11):3972-9 |
| Unit | Piece |
| Specification | 2mg 5mg 10mg |
GSK 3 Inhibitor IX 是一种有效的，选择性的，可逆的，ATP 竞争性的 GSK-3α/β 和 CDK1-cyclinB 复合体抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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