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SB216763,GSK3抑制剂

高效选择性GSK3抑制剂
规格或纯度: ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
S129716-5mg
5mg 现货 Stock Image
S129716-10mg
10mg 现货 Stock Image
S129716-25mg
25mg 现货 Stock Image
S129716-50mg
50mg 现货 Stock Image
S129716-100mg
100mg 期货 Stock Image

基本描述

别名 3-(2,4-二氯苯基)-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮
英文别名 280744-09-4|SB 216763|3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione|SB216763|SB-216763|3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dione|1H-Pyrrole-2,5-dione, 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-|CHEMBL1
规格或纯度 ≥98%
英文名称 SB216763
生化机理 SB 216763 is potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (Ki = 9 nM for GSK-3α); competes with ATP. SB 216763 has minimal activity against 24 other protein kinases (IC50 > 10 μ M). Stimulates glycogen synthesis, gene transcription and is neuroprotective. SB 216763 also reduces pulmonary inflammation and fibrosis in a mouse model.Potent and selective GSK3 inhibitor (K i = 9 nM for GSK-3α). Has little activity against 24 other protein kinases (IC 50 > 10 μM). Stimulates glycogen synthesis, gene transcription and is cardio- and neuroprotective.
法律信息 Sold for only research purposes
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

SB 216763


产品介绍:

SB 216763是有效,选择性和ATP竞争性的 GSK-3 抑制剂,抑制GSK-3α和GSK-3β的 IC50 为34.3 nM。

SB 216763
SB-216763 was used to inhibit GSK-3β in human brain microvascular endothelial cell line6and colorectal cancer cells.7

SB-216763 was used to inhibit GSK-3β in human brain microvascular endothelial cell line and colorectal cancer cells.

名称和标识符

IUPAC Name 3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dione
INCHI InChI=1S/C19H12Cl2N2O2/c1-23-9-13(11-4-2-3-5-15(11)23)17-16(18(24)22-19(17)25)12-7-6-10(20)8-14(12)21/h2-9H,1H3,(H,22,24,25)
InChi Key JCSGFHVFHSKIJH-UHFFFAOYSA-N
Canonical SMILES CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl
Isomeric SMILES CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl
WGK Germany 3
PubChem CID 176158
分子量 371.22

化学和物理性质

溶解性 DMSO 23 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
敏感性 对热敏感
熔点 104 °C

安全和危险性(GHS)

象形图
ghs07

Harmful

信号词 Warning
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
预防措施声明 P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P271,P304+P340,P403+P233,P362+P364,P264+P265,P337+P317,P332+P317,P319
WGK Germany 3
个人防护装备 dust mask type N95 (US), Eyeshields, Gloves

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参考文献

1. Eldar-Finkelman H, Schreyer SA, Shinohara MM, LeBoeuf RC, Krebs EG.  (1999)  Increased glycogen synthase kinase-3 activity in diabetes- and obesity-prone C57BL/6J mice..  Diabetes,  48  (8):  (1662-6).  [PMID:10426388]
2. Nikoulina SE, Ciaraldi TP, Mudaliar S, Mohideen P, Carter L, Henry RR.  (2000)  Potential role of glycogen synthase kinase-3 in skeletal muscle insulin resistance of type 2 diabetes..  Diabetes,  49  (2):  (263-71).  [PMID:10868943]
3. Coghlan MP, Culbert AA, Cross DA, Corcoran SL, Yates JW, Pearce NJ, Rausch OL, Murphy GJ, Carter PS, Roxbee Cox L et al..  (2000)  Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription..  Chem Biol,  (10):  (793-803).  [PMID:11033082]
4. Cai Z, Zhao Y, Zhao B.  (2012)  Roles of glycogen synthase kinase 3 in Alzheimer's disease..  Curr Alzheimer Res,  (7):  (864-79).  [PMID:22272620]
5. Hurtado DE, Molina-Porcel L, Carroll JC, Macdonald C, Aboagye AK, Trojanowski JQ, Lee VM.  (2012)  Selectively silencing GSK-3 isoforms reduces plaques and tangles in mouse models of Alzheimer's disease..  J Neurosci,  32  (21):  (7392-402).  [PMID:22623685]
6. Takashima A, Noguchi K, Sato K, Hoshino T, Imahori K.  (1993)  Tau protein kinase I is essential for amyloid beta-protein-induced neurotoxicity..  Proc Natl Acad Sci USA,  90  (16):  (7789-93).  [PMID:8356085]
7. Dey D et al..  (2022)  Diffusion of small molecule drugs is affected by surface interactions and crowder proteins..  iScience,  25  (10):  (105088).  [PMID:36157590]
8. Collu GM et al..  (2012)  Dishevelled limits Notch signalling through inhibition of CSL..  Development,  139  (23):  (4405-15).  [PMID:23132247]
9. Cao S et al..  (2022)  Effects of cGMP/Akt/GSK-3β signaling pathway on atrial natriuretic peptide secretion in rabbits with rapid atrial pacing..  Front Physiol,  13  ():  (861981).  [PMID:36060704]
10. Ahmed T et al..  (2015)  Rescue of impaired late-phase long-term depression in a tau transgenic mouse model..  Neurobiol Aging,  36  (2):  (730-9).  [PMID:25443285]
11. Foertsch F et al..  (2013)  S100A11 is involved in the regulation of the stability of cell cycle regulator p21(CIP1/WAF1) in human keratinocyte HaCaT cells..  FEBS J,  280  (16):  (3840-53).  [PMID:23745637]
12. Zhang Y et al..  (2016)  The anti-hyperglycemic efficacy of a lipid-lowering drug Daming capsule and the underlying signaling mechanisms in a rat model of diabetes mellitus..  Sci Rep,  ():  (34284).  [PMID:27721485]
13. Macdougall CE et al..  (2018)  Visceral Adipose Tissue Immune Homeostasis Is Regulated by the Crosstalk between Adipocytes and Dendritic Cell Subsets..  Cell Metab,  27  (3):  (588-601.e4).  [PMID:29514067]