91高清自产国产拍,无码免费A级毛片大全,日本欧美国产中文字幕,99re热视频这里只有精品视频首页

首页

400-620-6333

提交您使用阿拉丁产品的研究文章，就得100元奖励！立即访问我们的提交页面.

跳到内容

语言

切换导航

我的购物车

搜索

菜单

账号

设置

语言

首页
应用
药物靶标
激酶
CMGC：包含CDK，MAPK，GSK3，CLK家族
Tideglusib,非ATP竞争性GSK-3β抑制剂

Tideglusib,非ATP竞争性GSK-3β抑制剂

规格或纯度: ≥98%

CAS编号: 865854-05-3
分子式: C₁₉H₁₄N₂O₂S
分子量: 334.39
MDL号: MFCD18633296
PubChem编号: 11313622

有货

库存信息

关闭

库存信息

关闭

库存信息

关闭

货号 (SKU)	包装规格	是否现货
T127039-5mg	5mg	现货
T127039-25mg	25mg	现货
T127039-100mg	100mg	现货

查看相关系列

glycogen synthase kinase 3 beta Inhibitor

Skip to the end of the images gallery

Skip to the beginning of the images gallery

基本描述

规格或纯度	≥98%
英文名称	Tideglusib
别名	NP-12;NP031112
英文别名	NP 031112;NP-031112;4-Benzyl-2-(naphthalen-1-yl)-[1,2,4]thiadiazolidine-3,5-dione
生化机理	Tideglusib, also known as NP031112 or NP-12, is a potent non ATP-competitive inhibitor of glycogen synthase kinase-3 (GSK3), an important kinase studied in stem cell research and neurodegenerative diseases. It is currently in clinical trials for Alzheimer′s disease and Progressive Supranuclear Palsy (PSP). Tideglusib reduces phosphorylation of the tau protein and the accumulation of amyloid plaques, reduces hippocampal and entorhinal cortex neuron loss and improves spatial memory deficits. It has also shown neuroprotective and anti-inflammatory activity in a variety of animal models.
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	5mg、100mg卖完停产，不再备货
产品介绍	Tideglusib(NP-031112)是不可逆的非ATP竞争性GSK-3β抑制剂，IC50为60 nM。 Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site.

名称和标识符

IUPAC Name	4-benzyl-2-naphthalen-1-yl-1,2,4-thiadiazolidine-3,5-dione
INCHI	InChI=1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2
InChi Key	PMJIHLSCWIDGMD-UHFFFAOYSA-N
Canonical SMILES	C1=CC=C(C=C1)CN2C(=O)N(SC2=O)C3=CC=CC4=CC=CC=C43
分子式	C₁₉H₁₄N₂O₂S
PubChem CID	11313622
分子量	334.39

数据库链接

PubChem CID	11313622
Wikipedia	Tideglusib
CAS Registry No.	865854-05-3

化学和物理性质

溶解性	DMSO 1 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

安全信息

WGK Germany	3

靶标

Target ID

2030

名称

glycogen synthase kinase 3 beta

缩写名

GSK3B

家族

GSK subfamily

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	420	3q13.33	GSK3B	glycogen synthase kinase 3 beta
Mouse	2	420	16 B3	Gsk3b	glycogen synthase kinase 3 beta
Rat	2	420	11q21	Gsk3b	glycogen synthase kinase 3 beta

Ensembl Gene

ENSG00000082701 (Hs) , ENSMUSG00000022812 (Mm) , ENSRNOG00000002833 (Rn)

Entrez Gene

2932 (Hs) , 56637 (Mm) , 84027 (Rn)

OMIM

605004 (Hs)

UniProtKB

P18266 (Rn) , P49841 (Hs) , Q9WV60 (Mm)

RefSeq Nucleotide

NM_001146156 (Hs) , NM_019827 (Mm) , NM_032080 (Rn)

RefSeq Protein

NP_001139628 (Hs) , NP_062801 (Mm) , NP_114469 (Rn)

Protein GI

225903437 (Hs) , 9790077 (Mm) , 14091770 (Rn)

ChEMBL Target

CHEMBL3669 (Rn) , CHEMBL1075321 (Mm) , CHEMBL262 (Hs)

关联配体

Ligand ID	6929
名称	tideglusib
别名	NP031112
类别	Synthetic organic
学名	4-benzyl-2-(naphthalen-1-yl)-1,2,4-thiadiazolidine-3,5-dione
生物活性评价	Tideglusib is an irreversible inhibitor of GSK-3 with non-competitive inhibition pattern with respect to ATP but no covalent modification has been demonstrated
评价	Tideglusib is a small molecule non-ATP-competitive, irreversible glycogen synthase kinase 3 (GSK-3β) inhibitor that has been investigated as a potential treatment for Alzheimer's disease and paralysis supranuclear palsy . Low-dose tideglusib has been reported to induce natural reparative dentine formation, as a novel approach to treating tooth decay . In vitro and in vivo, tideglusib (and analogues) has shown anti-staphylococcal activity, via inhibition of Staphylococcus aureus sortase A (SrtA; a virulence factor of Gram-positive pathogens) .
临床描述	The main purpose of this study is to evaluate the cognitive changes after administration of tideglusib versus placebo at two oral doses and two treatment regimes for 26 weeks in patients with mild to moderate Alzheimer's disease. After the 26 week core treatment period, the patients may continue in the study under blinded conditions for an optional extension period up to a maximum of 39 additional weeks (total study duration up to 65 weeks), until the last patient in the study has completed the 26 week of treatment. This study will examine the safety and efficacy of tideglusib vs. placebo for the treatment of core symptom domains in adolescents with Autism Spectrum Disorders The purpose of this study is to determine whether Tideglusib is safe and efficacious in the treatment of adolescents and adults with congenital and juvenile-onset Myotonic Dystrophy. The pharmacokinetics of tideglusib and its primary metabolite will also be investigated.
来源公司	Noscira SA Anagnostou, Evdokia, M.D. AMO Pharma Limited

参考文献

1. Luna-Medina R, Cortes-Canteli M, Sanchez-Galiano S, Morales-Garcia JA, Martinez A, Santos A, Perez-Castillo A. (2007) NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders.. J Neurosci, 27 (21): (5766-76). [PMID:17522320]
2. Martinez A, Gil C, Perez DI. (2011) Glycogen synthase kinase 3 inhibitors in the next horizon for Alzheimer's disease treatment.. Int J Alzheimers Dis, 2011 (13): (280502). [PMID:21760986]
3. Domínguez JM, Fuertes A, Orozco L, del Monte-Millán M, Delgado E, Medina M. (2012) Evidence for irreversible inhibition of glycogen synthase kinase-3β by tideglusib.. J Biol Chem, 287 (2): (893-904). [PMID:22102280]
4. del Ser T, Steinwachs KC, Gertz HJ, Andrés MV, Gómez-Carrillo B, Medina M, Vericat JA, Redondo P, Fleet D, León T. (2013) Treatment of Alzheimer's disease with the GSK-3 inhibitor tideglusib: a pilot study.. J Alzheimers Dis, 33 (1): (205-15). [PMID:22936007]
5. Neves VC, Babb R, Chandrasekaran D, Sharpe PT. (2017) Promotion of natural tooth repair by small molecule GSK3 antagonists.. Sci Rep, 7 (13): (39654). [PMID:28067250]
6. Yang T, Zhang T, Guan XN, Dong Z, Lan L, Yang S, Yang CG. (2020) Tideglusib and Its Analogues As Inhibitors of Staphylococcus aureus SrtA.. J Med Chem, 63 (15): (8442-8457). [PMID:32639734]