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Submit ReviewTDZD 8 is a selective non-ATP competitive inhibitor of GSK 3β (IC50 = 2 μM); thiadiazolidinone deriviative. Does not inhibit Cdk-1/cyclin B, CK-II, PKA or PKC at >100 μM. Reduces severity of L-dopa-induced dyskinesia in a Parkinson's disease in vivo model.
分子量 | 222.26 |
公式 | C10H10N2O2S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 327036-89-5 |
PubChem ID | 4124851 |
InChI Key | JDSJDASOXWCHPN-UHFFFAOYSA-N |
Smiles | CN1SC(N(C1=O)CC2=CC=CC=C2)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 22.23 | 100 | |
ethanol | 22.23 | 100 |
以下数据基于产品分子量 222.26。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 4.5 mL | 22.5 mL | 44.99 mL |
5 mM | 0.9 mL | 4.5 mL | 9 mL |
10 mM | 0.45 mL | 2.25 mL | 4.5 mL |
50 mM | 0.09 mL | 0.45 mL | 0.9 mL |
参考文献是支持产品生物活性的出版物。
Xie et al (2016) Inhibition of Glycogen Synthase Kinase-3β (GSK-3 beta ) as potent therapeutic strategy to ameliorates L-dopa-induced dyskinesia in 6-OHDA parkinsonian rats. Sci.Rep. 6 23527 PMID: 26997328
Martinez et al (2002) First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. J.Med.Chem. 45 1292 PMID: 11881998
If you know of a relevant reference for TDZD 8, please let us know.
关键词: TDZD 8, TDZD 8 supplier, TDZD8, NP01139, NP_01139, Selective, non-ATP, competitive, inhibitor, GSK, 3, β, L-dopa-induced, dyskinesia, NP, 01139, Glycogen, Synthase, Kinase, 6092, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 TDZD 8 的部分引用包括:
Coleen M et al (2020) Glycogen synthase kinase-3 inhibition rescues sex-dependent contextual fear memory deficit in human immunodeficiency virus-1 transgenic mice. Br J Pharmacol 177 5658-5676 PMID: 33080056
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I have used TDZD to inhibit GSK3 in the brain of mice. After the treatment, we investigated if the NCS-1 gene would increase its expression as we have hypothesised the GSK3 protein impairs NCS-1 gene expression. We found that this happened, but only in the pre frontal cortex (PFC) as showed by the figure.
We treated mice with TDZD-8 at 30 mg/kg, i.p. for 1 h
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.