
ML265
CAS No. 1221186-53-3
ML265 ( TEPP-46 )
产品货号. M20635 CAS No. 1221186-53-3
ML265 是一种有效的 PKM2 激活剂 (AC50 : 92 nM),对 PKM1、PKL 和 PKR 几乎没有影响或没有影响,在小鼠异种移植模型中诱导四聚化并减少肿瘤形成和大小。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥786 | 有现货 |
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10MG | ¥1191 | 有现货 |
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50MG | ¥3021 | 有现货 |
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100MG | 获取报价 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称ML265
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述ML265 是一种有效的 PKM2 激活剂 (AC50 : 92 nM),对 PKM1、PKL 和 PKR 几乎没有影响或没有影响,在小鼠异种移植模型中诱导四聚化并减少肿瘤形成和大小。
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产品描述ML265 is a potent PKM2 activator (AC50 : 92 nM) showing little or no effect on PKM1 PKL and PKRinduces tetramerization and reduces tumor formation and size in a mouse xenograft model.?(In Vitro):TEPP-46 and DASA-58 activate PKM2 by a mechanism similar to that of the endogenous activator FBP. Pre-treatment of cells with TEPP-46 or DASA-58 prevents pervanadate-induced inhibition of PKM2 activity. TEPP-46 also induces a decrease in the intracellular levels of acetyl-coA, lactate, ribose phosphate and serine. TEPP-46 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes. TEPP-46 treatment significantly downregulates the expression of the M1 markers Il12p40 and Cxcl-10. Activation of PKM2 using TEPP-46 significantly inhibits FSL-1 and CpG-induced Il1b mRNA expression. TEPP-46 inhibits Mtb-induced Il1b mRNA levels, boosts Mtb-induced levels of Il10 mRNA, and has no effect on levels of Tnf.(In Vivo):TEPP-46 exhibits good oral bioavailability with relatively low clearance, long half-life, and good volume of distribution-parameters that predict for drug exposure in tumor tissues. TEPP-46 at 150 mg/kg readily achieves maximal PKM2 activation measured in A549 xenograft tumors.
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体外实验TEPP-46 and DASA-58 activate PKM2 by a mechanism similar to that of the endogenous activator FBP. Pre-treatment of cells with TEPP-46 or DASA-58 prevents pervanadate-induced inhibition of PKM2 activity. TEPP-46 also induces a decrease in the intracellular levels of acetyl-coA, lactate, ribose phosphate and serine. TEPP-46 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes. TEPP-46 treatment significantly downregulates the expression of the M1 markers Il12p40 and Cxcl-10. Activation of PKM2 using TEPP-46 significantly inhibits FSL-1 and CpG-induced Il1b mRNA expression. TEPP-46 inhibits Mtb-induced Il1b mRNA levels, boosts Mtb-induced levels of Il10 mRNA, and has no effect on levels of Tnf.
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体内实验TEPP-46 exhibits good oral bioavailability with relatively low clearance, long half-life, and good volume of distribution-parameters that predict for drug exposure in tumor tissues. TEPP-46 at 150 mg/kg readily achieves maximal PKM2 activation measured in A549 xenograft tumors.
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同义词TEPP-46
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通路Others
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靶点Other Targets
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受体PKM2
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研究领域——
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适应症——
化学信息
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CAS Number1221186-53-3
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分子量372.46
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分子式C17H16N4O2S2
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纯度>98% (HPLC)
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溶解度DMSO:50 mg/mL (134.24 mM)
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SMILESCn1c2cc(sc2c2cnn(Cc3cccc(N)c3)c(=O)c12)S(C)=O
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化学全称6-(3-aminobenzyl)-4-methyl-2-(methylsulfinyl)-46-dihydro-5H-thieno[2'3':45]pyrrolo[23-d]pyridazin-5-one
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Walsh M J Brimacombe K R Anastasiou D et al. ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model[M]// Probe Reports from the NIH Molecular Libraries Program. PubMed 2009.
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