|3-((4-((2,3-二氢苯并[b][1,4]二恶英-6-基)磺酰基)-1,4-二氮杂卓-1-基)磺酰基)苯胺|CsnPharm

CAS No.: 1203494-49-8

DASA-58 Catalog No. CSN17555

Synonyms: ML-203;NCGC00185916

DASA-58 is a selective activator of pyruvate kinase M2 (PKM2).

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技术信息

生物活性

描述Pyruvate kinase M2 (PKM2) interacts with phosphotyrosine-containing proteins to regulate glucose metabolism in cells. DASA-58 is a potent activator of recombinant PKM2 with an AC₉₀ value of 680 nM and an AC₅₀ value of 38 nM. In A549-PKM2/kd cell lysates, treatment with 40 μM DASA-58 for 3 hours caused 248% increase of pyruvate kinase activity. Incubation of A549 cells with 0 – 100 μM DASA-58 dose-dependently activated PKM2 with an EC₅₀ value of 19.6 μM. Also in A549 cells, pretreatment with 1 μM DASA-58 prevented pervanadate-induced PKM2 activity inhibition. DASA-58 at 50 μM decreased lactate production in H1299 cells compared to DMSO-treated group. In H1299 cells incubated with [6-¹⁴C]-glucose, DASA-58 at 30 μM led to a significant reduction of glucose-derived carbon incorporation into lipids. A549 cells treated with 100 μM DASA-58 showed diminished incorporation of glucose carbons into acetyl-CoA and decreased de novo lipogenesis^[3]. Injection of SCID mice with DASA-58-treated PC3 cells (40 μM, 48h incubation) significantly downregulated CAFs-induced lung metastases formation^[4].
作用机制DASA-58 increases PKM2 activity by an allosteric mechanism similar to fructose-1,6-bisphosphate, a glycolytic metabolite fructose that binds to PKM2, inducing a conformational conversion of the enzyme into its most active form^[3].
参考文献

[1] Palsson-McDermott EM, Curtis AM, et al. 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.
[2] Giannoni E, Taddei ML, et al. Targeting stromal-induced pyruvate kinase M2 nuclear translocation impairs oxphos and prostate cancer metastatic spread. Oncotarget. 2015 Sep 15;6(27):24061-74.
[3] Anastasiou D, Yu Y, Israelsen WJ, Jiang JK, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A, Yang H, Mattaini KR, Metallo CM, Fiske BP, Courtney KD, Malstrom S, Khan TM, Kung C, Skoumbourdis AP, Veith H, Southall N, Walsh MJ, Brimacombe KR, Leister W, Lunt SY, Johnson ZR, Yen KE, Kunii K, Davidson SM, Christofk HR, Austin CP, Inglese J, Harris MH, Asara JM, Stephanopoulos G, Salituro FG, Jin S, Dang L, Auld DS, Park HW, Cantley LC, Thomas CJ, Vander Heiden MG. Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat Chem Biol. 2012 Oct;8(10):839-47.
[4] 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2049 mL
- 11.0246 mL
- 22.0493 mL
- 5 mM
- 0.4410 mL
- 2.2049 mL
- 4.4099 mL
- 10 mM
- 0.2205 mL
- 1.1025 mL
- 2.2049 mL

技术信息

CAS号

1203494-49-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H23N3O6S2

运输

蓝冰

分子量

453.53

别名

ML-203;NCGC00185916

溶解度

DMSO	91.0 mg/mL (200.6 mM)
Water	Insoluble
Ethanol	Insoluble

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