上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
GSK 3 Inhibitor IX (Synonyms: 6-Bromoindirubin-3′-oxime; BIO; MLS 2052) 纯度: 99.74%
GSK 3 Inhibitor IX (6-Bromoindirubin-3′-oxime; BIO) 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。
GSK 3 Inhibitor IX Chemical Structure
CAS No. : 667463-62-9
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
10 mM * 1 mL in DMSO | ¥935 | In-stock | |
5 mg | ¥850 | In-stock | |
10 mg | ¥1200 | In-stock | |
50 mg | ¥4500 | In-stock | |
100 mg | 询价 | ||
200 mg | 询价 |
* Please select Quantity before adding items.
GSK 3 Inhibitor IX 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Apoptosis Compound Library
- Cell Cycle/DNA Damage Compound Library
- Kinase Inhibitor Library
- PI3K/Akt/mTOR Compound Library
- Stem Cell Signaling Compound Library
- Wnt/Hedgehog/Notch Compound Library
- Anti-Cancer Compound Library
- Clinical Compound Library
- Anti-Aging Compound Library
- Drug Repurposing Compound Library
- Reprogramming Compound Library
- Oxygen Sensing Compound Library
- Glycolysis Compound Library
- Cytoskeleton Compound Library
- Anti-Alzheimer’s Disease Compound Library
- Anti-Breast Cancer Compound Library
- Anti-Pancreatic Cancer Compound Library
- Anti-Blood Cancer Compound Library
- Anti-Cancer Metabolism Compound Library
- Neurodegenerative Disease-related Compound Library
- Glucose Metabolism Compound Library
生物活性 |
GSK 3 Inhibitor IX (6-Bromoindirubin-3′-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively. |
||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target[1] |
|
||||||||||||||||
体外研究 (In Vitro) |
GSK 3 Inhibitor IX (BIO) is a specific inhibitor of glycogen synthase kinase-3 (GSK-3), with IC50 of 5 nM for GSK-3α/β, shows > 16-fold selectivity over CDK5. GSK 3 Inhibitor IX interacts within the ATP binding pocket of these kinases, reduces β-catenin phosphorylation on a GSK-3-specific site in cellular models, closely mimicks Wnt signaling in Xenopus embryos[1]. In human and mouse embryonic stem cells, GSK 3 Inhibitor IX (BIO) maintains the undifferentiated phenotype and sustains expression of the pluripotent state-specific transcription factors Oct-3/4, Rex-1 and Nanog. GSK 3 Inhibitor IX (BIO)-mediated Wnt activation is functionally reversible, as withdrawal of the compound leads to normal multidifferentiation programs in both human and mouse embryonic stem cells[2]. GSK 3 Inhibitor IX (BIO) promotes proliferation in mammalian cardiomyocytes[3]. GSK 3 Inhibitor IX (BIO) is also a pan-JAK inhibitor, with IC50 values of 0.03, 1.5, 8.0, 0.5 μM for TYK2, JAK1, JAK2 and JAK3, respectively. GSK 3 Inhibitor IX (BIO) selectively inhibits phosphorylation of STAT3 and induces apoptosis of human melanoma cells[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
体内研究 (In Vivo) |
GSK 3 Inhibitor IX (BIO) (50 mg/kg, p.o.) suppresses melanoma tumor growth in a mouse xenograft model[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
Clinical Trial |
|
||||||||||||||||
分子量 |
356.17 |
||||||||||||||||
Formula |
C16H10BrN3O2 |
||||||||||||||||
CAS 号 |
667463-62-9 |
||||||||||||||||
运输条件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
储存方式 |
|
||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : ≥ 23 mg/mL (64.58 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
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。 |
||||||||||||||||
参考文献 |
|
Cell Assay [1] |
COS1, Hepa (wild-type, CEM/LM AhR deficient and ELB1 ARNT deficient), or SH-SY5Y cells are grown in 6 cm culture dishes in Dulbecco’s Modified Medium (DMEM) containing 10% fetal bovine serum. For treatment, IO (5 μM), GSK 3 Inhibitor IX (BIO) (5 or 10 μM), MeBIO (5 or 50 μM), LiCl (20 or 40 mM), or mock solution (DMSO, 0.5% final concentration) is added to medium when cell density reaches appr 70% confluence. After 12 (SH-SY5Y) or 24 hours, the cells, while still in plate, are lysed with lysis buffer (1% SDS, 1 mM sodium orthovanadate, 10 mM Tris [pH 7.4]). The lysate is passed several times through a 26G needle, centrifuged at 10,000× g for 5 min, and adjusted to equal protein concentration. About 8 μg of each sample is loaded for immunoblotting. Enhanced chemiluminescence is used for detection. The following primary antibodies are used: mouse anti-β-catenin CT, mouse anti-phospho-β-catenin, mouse anti-GSK-3 β, mouse anti-GSK-3 phosphoTyr216, rabbit anti-AhR (Aryl hydrocarbon receptor), and rabbit anti-actin. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
---|---|
Animal Administration [4] |
BALB/c mice (at 6-8 weeks old) and immunodeficient NOD/SCID/IL2Rgamma null (NSG) mice (female at 6-8 weeks old) are used in the assay. A2058 human melanoma cells at 5×106 cells in serum free medium are inoculated subcutaneously into the dorsal area of NSG mice to create xenograft model. When tumors become palpable, 6 GSK 3 Inhibitor IX (BIO) or vehicle control is administered via oral gavage once daily at 50 mg/kg body weight. Tumor growth is monitored every other day. Tumor volumes are measured every 3 to 4 days. Tumor volumes are calculated using the formula: 0.5 × (larger diameter) × (small diameter)2. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务