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Tankyrase 1/2 Inhibitor VI, G007-LK-Calbiochem

品牌
Sigma-Aldrich
CAS
1380672-07-0
货号
5.04907
规格纯度
Tankyrase 1/2 Inhibitor VI, G007-LK, CAS 1380672-07-0, is a cell-permeable, potent and highly selective inhibitor of tankyrase (IC50 = 33 &26 nM for TNKS1 and TNKS2, respectively).
价格
3379.01 *本价格含增值税费
促销
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数量
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半岛bd体育手机客户端 名称:
1380672-07-0
Tankyrase 1/2 Inhibitor VI, G007-LK-Calbiochem
TNKS1/2 Inhibitor VI, G007LK, Wnt Pathway Inhibitor XXI, 4-(5-(( E)-2-(4-(2-Chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)ethenyl)-1,3,4-oxadiazol-2-yl)benzonitrile
TNKS1/2 Inhibitor VI, G007LK, Wnt Pathway Inhibitor XXI, 4-(5-(( E)-2-(4-(2-Chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)ethenyl)-1,3,4-oxadiazol-2-yl)benzonitrile
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

A cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD+pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC50= 33 and 26 nM, respectively, against TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 in auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (ICmax~300 and 600 nM, respectively). Shown to display little or no inhibitory potency (IC50>10 ?M) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50>10 ?M). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formationin vitro(200 nM) and tumor expansion in micein vivo(20 mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD+pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC50= 33 and 26 nM, respectively, in TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (ICmax~300 and 600 nM, respectively). In addition to being more selective over PARP1/2 (IC50>10 ?M vs 116 nM/47 nM with XAV939) than the nicotinamide site-targeting XAV939 (Cat. No. 575545), G007-LK is also shown to display little or no inhibitory potency (IC50>10 ?M) toward 5 other PARP enzymes (PARP3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50>10 ?M). Wnt signaling inhibition upon G007-LK treatment in 11 APC (Adenomatous polyposis coli/deleted in polyposis 2.5/DP2.5) mutatant CRC (colorectal cancer) lines ranges from no effect to varying degrees of partial blockages that do not correlate with the observed CRC colony formation inhibitions.Two CRC lines, COLO-320DM & SW403, whose colony formation are affected by G007-LKin vitro(by 70% and 27%, respectively, at 200 nM in 7 to 13 d) are also inhibited by G007-LK for their tumor expansion in micein vivo(by 47% and 42%, respectively, on d21; 20 mg/kg per daily i.p.), while G007-LK toxicity is observed at high dosages in mice (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.) due to small intestine damage as a result of on-target wnt signaling inhibition in normal tissue. Exhibits favorable pharmacokinetic properties in mice when administered via i.p. ( Plasmat1/2≥2.73 h;Cmax≥2.358 ?g/mL; 5 mg/kg) or p.o. ( Plasmat1/2≥2.8 h;Cmax≥871 ng/mL; 5 mg/kg).

生化/生理作用

Cell permeable: yes
Primary Target
Tankyrase 1/2
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Lau, T., et al. 2013.Cancer Res.73,3132.
Voronkov, A., et al. 2013.J. Med. Chem.56,3012.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式 C25H16ClN7O3S
分子量 529.96

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥98% (HPLC)
形式 powder
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
protect from light
颜色 white
溶解性 DMSO: 25 mg/mL
储存温度 2-8℃

安全信息

储存分类代码 11 - Combustible Solids
WGK WGK 2
闪点(F) Not applicable
闪点(C) Not applicable

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