SML2853
DASA-58
≥98% (HPLC)
别名:
3-(4-(2,3-Dihydrobenzo[b][1,4]dioxin-6-ylsulfonyl)-1,4-diazepan-1-ylsulfonyl)aniline, CID-44543605, DASA 58, DASA58, ML 203, ML-203, ML203, N,N′-DiArylSulfonAmide 58, NCGC00185916
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
NC1=CC=CC(S(N2CCN(S(C3=CC=C(OCCO4)C4=C3)(=O)=O)CCC2)(=O)=O)=C1
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
InChI key
GMHIOMMKSMSRLY-UHFFFAOYSA-N
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).
Potent and selective activator of cancer-specific pyruvate kinase PKM2 in vitro and in vivo, but not PKM1, PKR or PKL.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Xinxing Ouyang et al.
Journal of molecular cell biology, 11(2), 93-106 (2018-11-15)
Glucose metabolism plays a key role in thymocyte development. The mammalian target of rapamycin complex 2 (mTORC2) is a critical regulator of cell growth and metabolism, but its role in early thymocyte development and metabolism has not been fully studied.
Matthew B Boxer et al.
Journal of medicinal chemistry, 53(3), 1048-1055 (2009-12-19)
The metabolism of cancer cells is altered to support rapid proliferation. Pharmacological activators of a tumor cell specific pyruvate kinase isozyme (PKM2) may be an approach for altering the classic Warburg effect characteristic of aberrant metabolism in cancer cells yielding
Qiuyue Kong et al.
Diabetes, 68(2), 361-376 (2018-11-21)
Nonalcoholic steatohepatitis (NASH) is the most prevalent cause of chronic liver disease worldwide. Macrophage-mediated inflammation plays a critical role in NASH pathogenesis; however, optimum therapies for macrophage activation and NASH remain elusive. HSPA12A encodes a novel member of the HSP70
Paresh P Kulkarni et al.
Haematologica, 104(4), 806-818 (2018-11-02)
Platelets are critical to arterial thrombosis, which underlies myocardial infarction and stroke. Activated platelets, regardless of the nature of their stimulus, initiate energy-intensive processes that sustain thrombus, while adapting to potential adversities of hypoxia and nutrient deprivation within the densely
Jiao Feng et al.
Journal of experimental & clinical cancer research : CR, 38(1), 204-204 (2019-05-19)
The treatment for advanced primary hepatocellular carcinoma (HCC) is sorafenib (SORA), while HCC has become increasingly drug resistant with enhanced aerobic glycolysis. The present study aimed to examine the chemotherapeutic effects of a flavonoid proanthocyanidin B2 (PB2) on HCC. Five
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