上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
TEPP-46 (Synonyms: ML-265) 纯度: 99.71%
TEPP-46 (ML-265) 是一种有效,选择性的丙酮酸激酶 M2 (pyruvate kinase M2; PKM2) 激活剂,AC50 值为 92 nM,对 PKM1,PKL 和 PKR 作用较小或没有作用。
TEPP-46 Chemical Structure
CAS No. : 1221186-53-3
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
10 mM * 1 mL in DMSO | ¥1210 | In-stock | |
5 mg | ¥1100 | In-stock | |
10 mg | ¥1650 | In-stock | |
50 mg | ¥5400 | In-stock | |
100 mg | ¥7150 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
TEPP-46 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Kinase Inhibitor Library
- Metabolism/Protease Compound Library
- Anti-Cancer Compound Library
- Glycolysis Compound Library
- Pyroptosis Compound Library
- Anti-Cancer Metabolism Compound Library
- Glucose Metabolism Compound Library
- Targeted Diversity Library
生物活性 |
TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR[1]. |
||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
体外研究 (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[1]. 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[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
体内研究 (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[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||||||
分子量 |
372.46 |
||||||||||||||||
Formula |
C17H16N4O2S2 |
||||||||||||||||
CAS 号 |
1221186-53-3 |
||||||||||||||||
运输条件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
储存方式 |
|
||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (134.24 mM; Need ultrasonic) 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
|
||||||||||||||||
参考文献 |
|
Cell Assay [1] |
2,000 cells are seeded in 96-well plates 24 h prior to treatment start. CellTiter96® AQueous is used to assess cell viability following oxidant and PKM2 activator combination treatments. MTS: (3-(4,5-dimethylthiazol-2-yl)-5- (3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium). 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
---|---|
Animal Administration [1] |
H1299 parental and H1299 cells with constitutive expression of a mouse PKM1 cDNA (H1299-PKM1 cells) are propagated in RPMI supplemented with 10% fetal bovine serum, 2 mM glutamine, and hygromycin for transgene selection. Cells are harvested, resuspended in sterile PBS, and 5×105 cells are injected subcutaneously into nu/nu mice. Tumor growth is monitored by caliper measurement, the mice are sacrificed and tumors harvested after the time indicated. Tumors are weighed, divided and either flash-frozen in liquid nitrogen or fixed in formalin for later analysis. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务