| Description | DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator. |
| In vitro | DASA-58 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes in primary BMDMs, and also inhibits glycolysis and the accumulation of succinate in LPS-activated macrophages. [1] In PC3 cells, DASA-58 impairs stromal-induced EMT program by restoring PK activity and abrogating the nuclear translocation of PKM2, as well as its association with HIF-1α. DASA-58 also dramatically reduces (~6-fold) CAFs-induced lung metastases formation in PC3 cells. [2] |
| In vivo | DASA-58 (40 μM) affects EMT of prostate cancers and tumor dissemination in SCID mice. [2] |
| molecular weight | 453.53 |
| Molecular formula | C19H23N3O6S2 |
| CAS | 1203494-49-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 84 mg/mL (185.2 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Palsson-McDermott EM, et al. Cell Metab. 2015, 21(1), 65-80. 2. Giannoni E, et al. Oncotarget. 2015, 6(27), 24061-24074. |
| Citations | 1. Yang L, Zhang J, Hu C, et al.Nuclear translocation of PKM2 mediates keratinocyte metabolic reprogramming in psoriasis.Experimental Dermatology.2023 |