SMILES string
S(CC2=C(C(=O)c3c(cccc3)C2=O)C)C(=S)N1CCCCC1
InChI
1S/C18H19NO2S2/c1-12-15(11-23-18(22)19-9-5-2-6-10-19)17(21)14-8-4-3-7-13(14)16(12)20/h3-4,7-8H,2,5-6,9-11H2,1H3
InChI key
STAFOGVMELKGRI-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Pyruvate kinase M2 (PKM2) inhibitor superior to shikonin.
Compound 3k (C3k) is a pyruvate kinase M2 (PKM2) inhibitor with 3-fold higher potency than shikonin (IC50 = 2.95 and 8.82 μM, respectively, by in vitro PKM2 LDH coupled assay). C3k exhibits potent cancer cell-selective antiproliferative activity in high PKM2-expressing cancer cultures (HCT116/HeLA/H1299 IC50 = 0.18/0.29/1.56 μM with C3k, 1.84/2.45/1.88 μM with shikonin) with much less cytotoxicity toward normal BEAS-2B human bronchial epithelial cells (IC50 = 18.46 μM; IC50 = 5.36 μM with shikonin).
Compound 3k (C3k) is a pyruvate kinase M2 (PKM2) inhibitor with 3-fold higher potency than shikonin (IC50 = 2.95 and 8.82 μM, respectively, by in vitro PKM2 LDH coupled assay). C3k exhibits potent cancer cell-selective antiproliferative activity in high PKM2-expressing cancer cultures (HCT116/HeLA/H1299 IC50 = 0.18/0.29/1.56 μM with C3k, 1.84/2.45/1.88 μM with shikonin) with much less cytotoxicity toward normal BEAS-2B human bronchial epithelial cells (IC50 = 18.46 μM; IC50 = 5.36 μM with shikonin).
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Xianling Ning et al.
European journal of medicinal chemistry, 138, 343-352 (2017-07-09)
Pyruvate kinase M2 (PKM2) is a rate-limiting enzyme of the glycolytic pathway which is highly expressed in cancer cells. Cancer cells rely heavily on PKM2 for anabolic and energy requirements, and specific targeting of PKM2 therefore has potential as strategy
Rui-Yuan Pan et al.
Cell metabolism, 34(4), 634-648 (2022-03-19)
The pro-inflammatory activation of microglia is a hallmark of Alzheimer's disease (AD), and this process involves a switch from oxidative phosphorylation (OXPHOS) toward glycolysis. Here, we show how a positive feedback loop in microglia drives AD pathogenesis, and we demonstrate
Jae Hyeon Park et al.
In vivo (Athens, Greece), 36(2), 694-703 (2022-03-05)
Pyruvate kinase M2 (PKM2) functions as an important rate-limiting enzyme in aerobic glycolysis and is involved in tumor initiation and progression. However, there are few studies on the correlation between PKM2 expression and its role in glioma. PKM2 expression was
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