D5794
二酰甘油激酶抑制剂II
solid
别名:
3-[2-[4-(双(4-氟苯基)亚甲基)-1-哌啶基]乙基]-2,3-二氢-2-硫代-4(1H)-喹唑啉酮, R59949
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关于此项目
经验公式（希尔记法）:
C28H25F2N3OS
化学文摘社编号:
分子量:
489.58
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
41106300
MDL number:
InChI
1S/C28H25F2N3OS/c29-22-9-5-19(6-10-22)26(20-7-11-23(30)12-8-20)21-13-15-32(16-14-21)17-18-33-27(34)24-3-1-2-4-25(24)31-28(33)35/h1-12H,13-18H2,(H,31,35)
SMILES string
Fc1ccc(cc1)\C(=C2\CCN(CCN3C(=S)Nc4ccccc4C3=O)CC2)c5ccc(F)cc5
InChI key
ZCNBZFRECRPCKU-UHFFFAOYSA-N
biological source
synthetic (organic)
assay
≥97% (HPLC)
form
solid
color
pale yellow
mp
228-230 °C
solubility
0.1 M HCl: slightly soluble, 0.1 M NaOH: slightly soluble, DMSO: soluble, H2O: insoluble, ethanol: soluble, ethyl acetate: soluble
storage temp.
−20°C
Quality Level
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相关类别
Application
甘油二酯激酶抑制剂II可用于确定嵌合抗原受体 (CAR) 改造的细胞毒性T细胞的肿瘤诱导抑制。它还用于诱导T细胞急性淋巴细胞白血病中的pAkt和PKR样细胞外信号调节激酶 (pErk) 信号。
Biochem/physiol Actions
二酰基甘油激酶抑制剂。抑制红细胞膜中[38P]1-油酰基-2-乙酰甘油基-3-磷酸（OAPA）的形成：IC50 = 3.3 μM。
Features and Benefits
这种化合物是激酶磷酸酶生物学研究的特色产品。点击此处发现更多特色激酶磷酸酶生物产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。
存储类别
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Gloves
Costin N Antonescu et al.
Molecular biology of the cell, 21(16), 2944-2952 (2010-06-25)
Clathrin-mediated endocytosis (CME) is the main route of internalization of receptor-ligand complexes. Relatively little is known about the role of specific lipids in CME, in particular that of phosphatidic acid (PA). We examined the effect of altering cellular PA levels
D L Nunn et al.
The Biochemical journal, 243(3), 809-813 (1987-05-01)
The diacylglycerol kinase inhibitor R59022 (10 microM) potentiates secretion and aggregation responses in human platelets challenged with sub-maximal concentrations of thrombin. Potentiation correlates closely with increased formation of diacylglycerol, increased phosphorylation of a 40 kDa protein, a known substrate for
RasGRP1 overexpression in T-ALL increases basal nucleotide exchange on Ras rendering the Ras/PI3K/Akt pathway responsive to protumorigenic cytokines
Ksionda O, et al.
Oncogene, 35(28), 3658-3658 (2016)
Elisa Temes et al.
The Journal of biological chemistry, 280(25), 24238-24244 (2005-04-26)
Hypoxia-inducible factors (HIF) are heterodimeric (alpha/beta) transcription factors that play a fundamental role in cellular adaptation to low oxygen tension. In the presence of oxygen, the HIF-alpha subunit becomes hydroxylated at specific prolyl residues by prolyl hydroxylases. This post-translational modification
X Du et al.
The Biochemical journal, 357(Pt 1), 275-282 (2001-06-21)
We have previously shown that unsaturated fatty acids amplify platelet-derived-growth-factor (PDGF)-induced protein kinase C (PKC) activation in vascular smooth-muscle cells (VSMCs). Diacylglycerol-induced PKC activation is normally terminated by diacylglycerol kinases (DGKs). We thus hypothesized that fatty acids act by inhibiting
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