SML2651
Elesclomol
≥98% (HPLC), anticancer agent, powder
别名:
1,3-bis[2-Methyl-2-(phenylthioxomethyl)hydrazide]propanedioic acid, GSK842879A, N′1,N′3-Dimethyl-N′1,N′3-di(phenylcarbonothioyl)malonohydrazide, NSC 174939, NSC174939, STA 4783, STA-4783, STA4783
Product Name
Elesclomol, ≥98% (HPLC)
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
S=C(N(NC(=O)CC(=O)NN(C)C(=S)c2ccccc2)C)c1ccccc1
InChI
1S/C19H20N4O2S2/c1-22(18(26)14-9-5-3-6-10-14)20-16(24)13-17(25)21-23(2)19(27)15-11-7-4-8-12-15/h3-12H,13H2,1-2H3,(H,20,24)(H,21,25)
InChI key
BKJIXTWSNXCKJH-UHFFFAOYSA-N
相关类别
生化/生理作用
Copper (II)-chelating malonohydrazide derivative with in vitro and in vivo anticancer efficacy via reactive oxygen species (ROS) & apoptosis induction.
Elesclomol (STA-4783) is a copper (II)-chelating malonohydrazide derivative that exerts its in vitro and in vivo anticancer efficacy via reactive oxygen species (ROS)/oxidative stress & apoptosis induction in a Cu(II)-dependent manner (GI50 = 12 nM without vs. 129 nM with Cu2+ removal by TRIEN in K562 culture; typical conc. range 0.1-2 μM in cultures). Elesclomol chelates extracellular Cu(II) for mitochondria delivery, where upon Cu2+ reduction (to Cu+) & ROS generation, copper-free elesclomol then exits cells for continual Cu(II) shuttling and accumulation in mitochondria. In addition to Cu2+, elesclomol can also chelate Co2+ and Ni2+, but not Fe3+ or Zn2+.
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
Masazumi Nagai et al.
Free radical biology & medicine, 52(10), 2142-2150 (2012-05-01)
Elesclomol is an investigational drug that exerts potent anticancer activity through the elevation of reactive oxygen species (ROS) levels and is currently under clinical evaluation as a novel anticancer therapeutic. Here we report the first description of selective mitochondrial ROS
Yi-Jie Ren et al.
Frontiers in pharmacology, 8, 804-804 (2017-11-23)
In order to survive under conditions of low oxygen, cancer cells can undergo a metabolic switch to glycolysis and suppress mitochondrial respiration in order to reduce oxygen consumption and prevent excessive amounts of reactive oxygen species (ROS) production. Nucleus accumbens-1
Jia Yu Wang et al.
Cancer research, 77(22), 6226-6239 (2017-09-28)
MTH1 helps prevent misincorporation of ROS-damaged dNTPs into genomic DNA; however, there is little understanding of how MTH1 itself is regulated. Here, we report that MTH1 is regulated by polyubiquitination mediated by the E3 ligase Skp2. In melanoma cells, MTH1
Changyu Zhang et al.
Chemical communications (Cambridge, England), 54(31), 3835-3838 (2018-03-27)
A new fluorescence probe was developed for HClO detection under physiological conditions, which displayed fast response (t1/2 < 30 s) and large off-on fluorescence increase (>1000-fold) toward HClO with high sensitivity and selectivity. The probe was successfully applied for the
W Lu et al.
Oncogene, 36(33), 4719-4731 (2017-04-11)
TP53 plays essential roles in tumor initiation and progression, and is frequently mutated in cancer. However, pharmacological stabilization and reactivation of p53 have not been actively explored for targeted cancer therapies. Herein, we identify a novel Cyclophilin A (CypA) small
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