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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
NC1=CC=CC(S(N2CCN(S(C3=CC=C(OCCO4)C4=C3)(=O)=O)CCC2)(=O)=O)=C1
生化/生理作用
DASA-58 is a potent and selective activator of cancer-specific pyruvate kinase isoform PKM2 (hPKM2 AC50 = 38 nM, Emax = 82%), but not PKM1, PKR or PKL, that stabilizes PKM2 tetrameric conformation by targeting a site distinct from that of fructose-1,6-bis-phosphate (FBP). DASA-58 exhibits good aqueous solubility (51.2 μg/mL), decreases cellular lactate production and suppresses cell proliferation selectively under hypoxic conditions (30 μM; H1299, 1% O2). When administered in mice, DASA-58 is reported to exhibit anti-thrombotic efficacy in vivo (40 mg/kg via iv).
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Mucosal immunology, 12(6), 1280-1290 (2019-08-30)
The pyruvate kinase M2 (PKM2)-mediated aerobic glycolysis has been shown to play a critical role in promoting cell survival and proliferation. However, little is known about the function of intestinal epithelial PKM2 in intestine homeostasis. Here we investigate whether and
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