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    DASA-58
    DASA-58

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1874
    CAS #: 1203494-49-8Purity ≥98%

    Description: DASA-58 is a potent and selective activator of pyruvate kinase M2 (PKM2) with an AC90 value of 680 nM, and an AC50 value of 38 nM. 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. 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.

    References: Cell Metab. 2015 Jan 6;21(1):65-80; Oncotarget. 2015 Sep 15;6(27):24061-74.

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    Molecular Weight (MW)453.53 
    FormulaC19H23N3O6S2 
    CAS No.1203494-49-8 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 91 mg/mL (200.6 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 3-[[4-[(2,3-dihydro-1,4-benzodioxin-6-yl)sulfonyl]hexahydro-1H-1,4-diazepin-1-yl]sulfonyl]-benzenamine

    InChi Key: GMHIOMMKSMSRLY-UHFFFAOYSA-N

    InChi Code: 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 Code: O=S(N1CCN(S(C2=CC=C(OCCO3)C3=C2)(=O)=O)CCC1)(C4=CC(N)=CC=C4)=O

    SynonymsML-203; ML 203; ML203; DASA-58; DASA 58; DASA58; NCGC00185916; NCGC-00185916; NCGC 00185916


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    In Vitro

    In vitro activity: 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. 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.


    Cell Assay: In A549-PKM1/kd and A549-PKM2/kd cells, Flag-PKM1 and Flag-PKM2 were expressed, respectively. Endogenous PKM2 was knockdowned. Treatment with DMSO resulted in 233±27% more pyruvate kinase activity in lysates from A549-PKM1/kd cells than that in lysates from A549-PKM2/kd cells. Treatment with DASA-58 did not increase the pyruvate kinase activity in A549-PKM1/kd cells, but it resulted in a 248 ±21% pyruvate kinase activity increase in the lysate of A549-PKM2/kd cells. In cells, 0-100 μM of DASA-58 dose-dependently activated PKM2 with an EC50 value of 19.6 μM.

    In VivoDASA-58 (40 μM) affects EMT of prostate cancers and tumor dissemination in SCID mice. 
    Animal modelMale SCID-bg/bg mice bearing PC3 tumors 
    Formulation & DosageDissolved in DMSO; 40 μM; i.v. injection 
    References

    Cell Metab. 2015 Jan 6;21(1):65-80; Oncotarget. 2015 Sep 15;6(27):24061-74. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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