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	48-602MAG	Buffer Detection Kit for Magnetic Beads	1 Kit

110165CBC Sigma-AldrichO-GlcNAcase Inhibitor, TMG - CAS 1009816-48-1 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

分析证书
参考
Data Sheet

同义词: (3aR,5R,6S,7R,7aR)-2-(Ethylamino)-3a,6,7,7a-tetrahydro-5-(hydroxymethyl)-5H-pyrano[3,2-d]thiazole-6,7-diol, 1,2-Dideoxy-2ʹ-ethylamino-α-D-glucopyranoso-[2,1-d]-2ʹ-thiazoline, OGA Inhibitor, Thiamet-G

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概述

Replacement Information

价格及供货情况

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Description
Overview	A cell-permeable, blood-brain barrier-permeant, orally active aminothiazoline that effectively increases O-GlcNAc level of cellular proteins both in cultures (EC₅₀ = 30 nM, EC_max = 200 nM in PC3) in vitro and in rats (50 mg/kg i.v.; 200 mg/kg via drinking water ad libitum) and mice (500 mg/kg via drinking water ad libitum) in vivo by inhibiting O-GlcNAcase/OGA-mediated O-GlcNAc cleavage in a substrate-competitive (K_i = 21 nM), time- and dose-dependent, and highly selective manner. TMG long-term treatment in murine AD model effectively prevents loss of motor neurons and reduces NFTs in brain without apparent effect on Tau hyperphosphorylation. O-GlcNAcylation is also reported to slow down heat-induced sTAB1 (TAK1-binding protein) aggregation and modulate CK2α kinase activity and substrate selectivity in vitro.
Catalogue Number	110165CBC
Brand Family	Calbiochem®
Synonyms	(3aR,5R,6S,7R,7aR)-2-(Ethylamino)-3a,6,7,7a-tetrahydro-5-(hydroxymethyl)-5H-pyrano[3,2-d]thiazole-6,7-diol, 1,2-Dideoxy-2ʹ-ethylamino-α-D-glucopyranoso-[2,1-d]-2ʹ-thiazoline, OGA Inhibitor, Thiamet-G

References
References	Yuzwa, S.A., et al. 2012. Nat. Chem. Biol. 8, 393. Tarrant, M.K., et al. 2012. Nat. Chem. Biol. 8, 262 Yuzwa, S.A., et al. 2008. Nat. Chem. Biol. 4, 483.

Product Information
CAS number	1009816-48-1
Form	Off-white solid
Hill Formula	C₉H₁₆N₂O₄S
Chemical formula	C₉H₁₆N₂O₄S
Quality Level	MQ100

Applications

Biological Information
Purity	≥98% by HPLC

Physicochemical Information

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Harmful
Storage	-20°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
110165CBC-25MGCN	04055977208009

Documentation

O-GlcNAcase Inhibitor, TMG - CAS 1009816-48-1 - Calbiochem 分析证书

标题	批号
110165CBC	输入批号

参考

参考信息概述
Yuzwa, S.A., et al. 2012. Nat. Chem. Biol. 8, 393. Tarrant, M.K., et al. 2012. Nat. Chem. Biol. 8, 262 Yuzwa, S.A., et al. 2008. Nat. Chem. Biol. 4, 483.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	04-April-2012 JSW
Synonyms	(3aR,5R,6S,7R,7aR)-2-(Ethylamino)-3a,6,7,7a-tetrahydro-5-(hydroxymethyl)-5H-pyrano[3,2-d]thiazole-6,7-diol, 1,2-Dideoxy-2ʹ-ethylamino-α-D-glucopyranoso-[2,1-d]-2ʹ-thiazoline, OGA Inhibitor, Thiamet-G
Description	A cell-permeable, stable (no degradation at room temp for 9 days in water), orally available aminothiazoline that effectively increases O-GlcNAc (O-linked β-N-acetylglucosamine) level of cellular proteins both in cultures (EC₅₀ = 30 nM, EC_max = 200 nM in PC3) in vitro and in rats (50 mg/kg i.v.; 200 mg/kg via drinking water ad libitum) and mice (500 mg/kg via drinking water ad libitum) in vivo by inhibiting O-GlcNAcase/OGA-mediated O-GlcNAc cleavage in a substrate-competitive (K_i = 21 nM against pNP-GlcNaAc hydrolysis by human OGA), time- and dose-dependent, and highly selective manner, displaying no effect toward OCT (UDP GlcNAc polypeptidyltransferase) and five other glycoside hydrolases. O-GlcNAc modification is shown to reduce both the kinetics and extent of Tau441 c-terminal fragment Tau_244-441 aggregate formation. TMG long-term treatment (36-wk; 500 mg/kg; drinking water ad libitum) of JNPL3 murine AD model bearing mutant human Tau (P301L) results in less NFTs (neurofibrillary tangles) in brain and 40% higher motor neurons in ventral horn without apparent effect on Tau hyperphosphorylation, while short-term treatment (≤24 h) in rats is reported to result in both a decrease in Tau phosphorylation and an increase of Tau O-GlcNAc modification. O-GlcNAcylation is also reported to slow down heat-induced sTAB1 (TAK1-binding protein) aggregation and modulate CK2α kinase activity and substrate selectivity in vitro.
Form	Off-white solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1009816-48-1
Chemical formula	C₉H₁₆N₂O₄S
Purity	≥98% by HPLC
Solubility	DMSO (100 mg/ml) or H₂O (100 mg/ml)
Storage	Protect from light -20°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Harmful
References	Yuzwa, S.A., et al. 2012. Nat. Chem. Biol. 8, 393. Tarrant, M.K., et al. 2012. Nat. Chem. Biol. 8, 262 Yuzwa, S.A., et al. 2008. Nat. Chem. Biol. 4, 483.

种类

Life Science Research > Inhibitors and Biochemicals

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