| Description | LDH-IN-1 is a pyrazole-based human lactate dehydrogenase (LDH) inhibitor(IC50s of 32 and 27 nM for LDHA and LDHB, respectively). |
| In vitro | LDH-IN-1在LDHA和LDHB上展现出低纳摩尔级别的抑制作用，对乳酸生成的抑制处于亚微摩尔水平，并能抑制MiaPaCa2胰腺癌细胞和A673肉瘤细胞中的糖酵解过程。 |
| In vivo | LDH-IN-1 在小鼠实验中展示了远超肝脏血流量(90 mL/min/kg)的清除值，其体内清除率达到227 mL/min/kg[1]。 |
| Target activity | LDHB:27 nM (IC50), LDHA:32 nM (IC50) |
| molecular weight | 570.68 |
| Molecular formula | C30H26N4O4S2 |
| CAS | 1964515-43-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (87.61 mM), Sonication is recommended. |
| References | 1. Rai G, et al. Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH). J Med Chem. 2017 Nov 22;60(22):9184-9204. |
| Citations | 1. He J, Dong C, Zhang H, et al.The oncogenic role of TFAP2A in bladder urothelial carcinoma via a novel long noncoding RNA TPRG1-AS1/DNMT3A/CRTAC1 axis.Cellular Signalling.2023, 102: 110527. |