DASa-58, also known as ML-203 and NCGC00185916, is a selective activator of pyruvate kinase M2 (PKM2; AC50 = 38 nM in vitro, EC50 = 19.6 µM in cells).
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Name | DASA-58 |
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Iupac Chemical Name | 3-[[4-[(2,3-dihydro-1,4-benzodioxin-6-yl)sulfonyl]hexahydro-1H-1,4-diazepin-1-yl]sulfonyl]-benzenamine |
Synonyms | DASA-58; DASA 58; DASA58; ML-203; ML 203; ML203; NCGC00185916; NCGC-00185916; NCGC 00185916; |
Molecular Formula | C19H23N3O6S2 |
Molecular Weight | 453.53 |
Smile | O=S(N1CCN(S(C2=CC=C(OCCO3)C3=C2)(=O)=O)CCC1)(C4=CC(N)=CC=C4)=O |
InChiKey | 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 |
CAS Number | 1203494-49-8 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Bulk | Enquiry | Enquiry | Enquiry |
Formulation | Solid powder |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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Clinical study |
1: Giannoni E, Taddei ML, Morandi A, Comito G, Calvani M, Bianchini F, Richichi
B, Raugei G, Wong N, Tang D, Chiarugi P. Targeting stromal-induced pyruvate
kinase M2 nuclear translocation impairs oxphos and prostate cancer metastatic
spread. Oncotarget. 2015 Sep 15;6(27):24061-74. PubMed PMID: 26183399; PubMed
Central PMCID: PMC4695170.
2: Palsson-McDermott EM, Curtis AM, Goel G, Lauterbach MA, Sheedy FJ, Gleeson LE,
van den Bosch MW, Quinn SR, Domingo-Fernandez R, Johnston DG, Jiang JK, Israelsen
WJ, Keane J, Thomas C, Clish C, Vander Heiden M, Xavier RJ, O'Neill LA. Pyruvate
kinase M2 regulates Hif-1α activity and IL-1β induction and is a critical
determinant of the warburg effect in LPS-activated macrophages. Cell Metab. 2015
Jan 6;21(1):65-80. doi: 10.1016/j.cmet.2014.12.005. Erratum in: Cell Metab. 2015
Feb 3;21(2):347. Jiang, Jain-Kang [corrected to Jiang, Jian-Kang]; Vanden Heiden,
Matthew [corrected to Vander Heiden, Matthew]. Cell Metab. 2015 Feb 3;21(2):347.
PubMed PMID: 25565206; PubMed Central PMCID: PMC5198835.