DASA-58 (ML203), Pyruvate Kinase M2 (PKM2) Activator

Overview
Catalog #	bs-60305c-2-mg-solid
Product Name	DASA-58 (ML203), Pyruvate Kinase M2 (PKM2) Activator
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 453.53 Formula: C19 H23 N3 O6 S2 CAS Number: 1203494-49-8 InChi Key: GMHIOMMKSMSRLY-UHFFFAOYSA-N InChi: InChI=1S/C19H23N3O6S2/c20-15-3-1-4-16(13-15)29(23,24)21-7-2-8-22(10-9-21)30(25,26)17-5-6-18-19(14-17)28-12-11-27-18/h1,3-6,13-14H,2,7-12,20H2 Smiles: NC1=CC(=CC=C1)S(=O)(=O)N1CCCN(CC1)S(=O)(=O)C1=CC2OCCOC=2C=C1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	DASA-58 (ML203) is a potent and selective Pyruvate kinase M2 (PKM2) activator with EC50 ~38 nM. It can stabilize pyruvate kinase subunit interactions, promote PKM2 tetramer formation and prevent inhibition by phosphotyrosine signaling. It can alter metabolism in cultured cells, and inhibit xenograft tumor growth in vivo. 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 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. It also dramatically reduces (~6-fold) CAFs-induced lung metastases formation in PC3 cells.