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PDE2/PDE10-IN-1
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产品链接:www.medchemexpress.com/K-756.html
研究领域:Cell Cycle/DNA Damage
靶点:PARP
相关产品:BMN-673 | MK-4827 | XAV-939 | Rucaparib phosphate | Veliparib | PJ34 hydrochloride | Nicotinamide | E7449 | AZD-2461 | NVP-TNKS656 | BSI-201 | G007-LK | Saroglitazar Magnesium | A-966492 | INO-1001 |
公司介绍:MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库,总部位于美国新泽西,分别在瑞典和上海设有欧洲区子公司和亚洲区总代理,营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商, 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域,PI3K、MAPK等近千个细分靶点,超过4000个活性小分子化合物现货,以及GPCR、API、离子通道等超过20种不同类型的化合物库,同时提供从毫克到千克的专业定制合成服务。
MCE 对每批产品都进行严格的LCMS和NMR检验,其产品已被全球近万名客户广泛使用并发表大量文章、;
MCE 定期增加各领域热门抑制剂、激动剂,不断扩增已有化合物库,以满足*新的科研需求;
数千种产品在上海有充足备货,24-48小时内送达客户;
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K-756产品描述:K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively.IC50 & Target: IC50: 31 nM (TNKS1), 36 nM (TNKS2)[1]In Vitro: K-756 is a novel and selective Wnt/β-catenin pathway inhibitor targeting tankyrase (TNKS). TNKS is one of the members of the PARP family (it is also known as PARP5). K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. To study the isoform selectivity of K-756, the PARP family enzyme inhibitory activity at 10 μM is evaluated. K-756 inhibits TNKS1 and TNKS2 by 97% and 100%, respectively. In contrast, the inhibitory activity of K-756 against PARP1, PARP2, PARP3, PARP6, PARP7, and PARP11 is less than 13%. K-756 inhibits the cell growth of APC-mutant colorectal cancer COLO 320DM and SW403 cells by inhibiting the Wnt/β-catenin pathway. K-756 strongly inhibits the reporter activity in DLD-1/TCF-Luc cells with an IC50 of 110 nM, but does not inhibit DLD-1/mtTCF-Luc cells, even at 1,000 nM. APC-mutant colorectal cancer cell line COLO 320DM and SW403 cells are treated with K-756 and after 144 hours, cell growth inhibition is measured by an XTT assay. The application of K-756 inhibits the cell growth of COLO 320DM with a GI50 of 780 nM. K-756 also inhibits SW403 with a GI50 of 270 nM[1].In Vivo: DLD-1/TCF-Luc cell xenografts are created in SCID mice. Vehicle (0.5% MC400) or K-756 is administered orally once a day for 3 days at 100, 200, and 400 mg/kg. The Wnt/β-catenin signal inhibition in the tumor is detected by measuring FGF20 and LGR5 and luciferase activity. The expression of FGF20 and reporter activity are significantly decreased at doses of 100 mg/kg and above at 3-day administration. The expression of LGR5 is significantly decreased at doses of 200 mg/kg and above at 3-day administration. The maximum inhibitory activity is reached with the administration of K-756 at a dose of 400 mg/kg at 3-day administration. The Wnt/β-catenin signal inhibition at a dose of 400 mg/kg is observed from 1-day administration[1].产品链接:www.medchemexpress.com/K-756.html
研究领域:Cell Cycle/DNA Damage
靶点:PARP
相关产品:BMN-673 | MK-4827 | XAV-939 | Rucaparib phosphate | Veliparib | PJ34 hydrochloride | Nicotinamide | E7449 | AZD-2461 | NVP-TNKS656 | BSI-201 | G007-LK | Saroglitazar Magnesium | A-966492 | INO-1001 |
公司介绍:MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库,总部位于美国新泽西,分别在瑞典和上海设有欧洲区子公司和亚洲区总代理,营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商, 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域,PI3K、MAPK等近千个细分靶点,超过4000个活性小分子化合物现货,以及GPCR、API、离子通道等超过20种不同类型的化合物库,同时提供从毫克到千克的专业定制合成服务。
MCE 对每批产品都进行严格的LCMS和NMR检验,其产品已被全球近万名客户广泛使用并发表大量文章、;
MCE 定期增加各领域热门抑制剂、激动剂,不断扩增已有化合物库,以满足*新的科研需求;
数千种产品在上海有充足备货,24-48小时内送达客户;
大量产品提供免费试用装;已为全球多个知名企业、院校构建各种定制型化合物库。
电话:021-58955995 手机:13611715263 联系人:客服部 Q Q:4008203792
热门标签:PDE2/PDE10-IN-1