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SB 415286,GSK3抑制剂

高效的选择性GSK3抑制剂

规格或纯度: 98%

CAS编号: 264218-23-7
分子式: C₁₆H₁₀ClN₃O₅
分子量: 359.72
MDL号: MFCD04039789
PubChem编号: 4210951

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货号 (SKU)	包装规格	是否现货	价格	数量
S129720-1mg	1mg	现货
S129720-5mg	5mg	现货
S129720-10mg	10mg	现货
S129720-50mg	50mg	现货

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glycogen synthase kinase 3 alpha Inhibitor glycogen synthase kinase 3 beta Inhibitor

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基本描述

别名	3-[(3-氯-4-羟基苯基)氨基]-4-(2-硝基苯基)-1H-吡咯-2,5-二酮
英文别名	264218-23-7\|SB 415286\|SB-415286\|SB415286\|3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione\|3-(3-chloro-4-hydroxyphenylamino)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione\|CHEMBL322970\|1H-Pyrrole-2,5-dione, 3-[(3-chloro-4-hydroxyphenyl)amin
规格或纯度	98%
英文名称	SB415286
生化机理	SB 415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM. 1 As a result of GSK3 inhibition, SB 415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 ?M. SB 415286 also protects primary neurons from death induced by the PI3-kinase pathway.Potent, selective GSK3 inhibitor (K i = 31 nM for GSK-3α); competes with ATP. Neuroprotective and antioxidant properties. Also able to stimulate glycogen synthesis and gene transcription. Cell-permeable.
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	1mg卖完停产，不再备货。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	产品介绍： SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β. 产品用途： SB 415286 was used to treat neuroblastoma cells and study the effect of GSK-3 inhibition on cell proliferation. Product Introduction SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β. Product Usage SB 415286 was used to treat neuroblastoma cells and study the effect of GSK-3 inhibition on cell proliferation.

名称和标识符

IUPAC Name	3-(3-chloro-4-hydroxyanilino)-4-(2-nitrophenyl)pyrrole-2,5-dione
INCHI	InChI=1S/C16H10ClN3O5/c17-10-7-8(5-6-12(10)21)18-14-13(15(22)19-16(14)23)9-3-1-2-4-11(9)20(24)25/h1-7,21H,(H2,18,19,22,23)
InChi Key	PQCXVIPXISBFPN-UHFFFAOYSA-N
Canonical SMILES	C1=CC=C(C(=C1)C2=C(C(=O)NC2=O)NC3=CC(=C(C=C3)O)Cl)[N+](=O)[O-]
Isomeric SMILES	C1=CC=C(C(=C1)C2=C(C(=O)NC2=O)NC3=CC(=C(C=C3)O)Cl)[N+](=O)[O-]
WGK Germany	3
PubChem CID	4210951
分子量	359.72

数据库链接

PubChem CID	4210951
CAS Registry No.	264218-23-7
ChEMBL Ligand	CHEMBL322970
Reactome Reaction	R-HSA-9687724
Reactome Drug	R-ALL-9687689

化学和物理性质

溶解性	DMSO 72 mg/mL Water <1 mg/mL Ethanol 72 mg/mL

安全和危险性（GHS）

象形图	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, 7 (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, 9 (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. Bartram J et al.. (2017) Cortical Up states induce the selective weakening of subthreshold synaptic inputs.. Nat Commun, 8 (): (665). [PMID:28939859]

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