AZ-33 is a selective lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 0.5 μM and a Kd of 0.093 μM[1].
分子量
497.56
Formula
C25H27N3O6S
CAS 号
1370290-34-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Ward RA,et al. Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation. J Med Chem. 2012 Apr 12;55(7):3285-306.
AZ-33 is a selective lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 0.5 μM and a Kd of 0.093 μM[1].
分子量
497.56
Formula
C25H27N3O6S
CAS 号
1370290-34-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Ward RA,et al. Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation. J Med Chem. 2012 Apr 12;55(7):3285-306.
AZ-33 is a selective lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 0.5 μM and a Kd of 0.093 μM[1].
分子量
497.56
Formula
C25H27N3O6S
CAS 号
1370290-34-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Ward RA,et al. Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation. J Med Chem. 2012 Apr 12;55(7):3285-306.
LDHA/PDKs-IN-1 (compound 20e) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 0.8 and 0.15 μM, respectively. LDHA/PDKs-IN-1 reduces A549 cell proliferation with an EC50 of 13.2 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-1 has the potential for the research of cancer diseases[1].
分子量
360.38
Formula
C19H21FN2O4
CAS 号
2490699-40-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Xiang S, et al. Development of dual inhibitors targeting pyruvate dehydrogenase kinases and human lactate dehydrogenase A: High-throughput virtual screening, synthesis and biological validation. Eur J Med Chem. 2020;203:112579.
LDHA/PDKs-IN-2 (compound 20k) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 1.6 and 0.7 μM, respectively. LDHA/PDKs-IN-2 reduces A549 cell proliferation with an EC50 of 15.7 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-2 has the potential for the research of cancer diseases[1].
分子量
332.35
Formula
C17H20N2O5
CAS 号
2490699-44-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Xiang S, et al. Development of dual inhibitors targeting pyruvate dehydrogenase kinases and human lactate dehydrogenase A: High-throughput virtual screening, synthesis and biological validation. Eur J Med Chem. 2020;203:112579.
LDHA-IN-3, as a selenobenzene compound, is a potent, noncompetitive lactate dehydrogenase (LDHA) inhibitor (IC50=145.2 nM). LDHA-IN-3 can be used for the research of cancer[1].
IC50 & Target
IC50: 145.2 nM (LDHA)[1]
体外研究 (In Vitro)
PSTMB (0~500 μM; 48 hours; MCF-7 cells) shows cytotoxic effect[1]. PSTMB (0.01~1 μM) shows dose-dependent inhibition of LDHA activity. PSTMB (0~0.5 μM) inhibits LDHA activity in Michaelis-Menten and Lineweaver-Burk plots. PSTMB (30 and 50 μM; HT29 cells) induces ROS production and mitochondrial damage[1]. PSTMB can bind to LDHA protein efficiently. PSTMB induces the intrinsic pathway-mediated apoptosis of cancer cells via production of mitochondrial ROS[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.
Cell Viability Assay[1]
Cell Line:
MCF-7 cells
Concentration:
0~500 μM
Incubation Time:
48 hours
Result:
Showed cytotoxic effect.
分子量
301.17
Formula
C13H9F3Se
CAS 号
227010-33-5
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Kim EY, et al. A Novel Lactate Dehydrogenase Inhibitor, 1-(Phenylseleno)-4-(Trifluoromethyl) Benzene, Suppresses Tumor Growth through Apoptotic Cell Death. Sci Rep. 2019;9(1):3969. Published 2019 Mar 8.