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
MDL编号:
UNSPSC代码:
41106300
PubChem化学物质编号:
NACRES:
NA.77
生物来源
synthetic (organic)
质量水平
方案
≥97% (HPLC)
表单
solid
颜色
pale yellow
mp
228-230 °C
溶解性
0.1 M HCl: slightly soluble
0.1 M NaOH: slightly soluble
DMSO: soluble
H2O: insoluble
ethanol: soluble
ethyl acetate: soluble
储存温度
−20°C
SMILES字符串
Fc1ccc(cc1)\C(=C2\CCN(CCN3C(=S)Nc4ccccc4C3=O)CC2)c5ccc(F)cc5
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)
InChI key
ZCNBZFRECRPCKU-UHFFFAOYSA-N
相关类别
应用
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。
生化/生理作用
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。
特点和优势
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。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
Marylana Saadeh et al.
PloS one, 7(1), e30200-e30200 (2012-01-25)
Chronic exposure (24-72 hrs) of pancreatic islets to elevated glucose and fatty acid leads to glucolipoxicity characterized by basal insulin hypersecretion and impaired glucose-stimulated insulin secretion (GSIS). Our aim was to determine the mechanism for basal hypersecretion of insulin. We
R W Erickson et al.
The Journal of biological chemistry, 274(32), 22243-22250 (1999-07-31)
The superoxide-generating neutrophil NADPH oxidase can be activated in cell-free reconstitution systems by several agonists, most notably arachidonic acid and the detergent sodium dodecyl sulfate. In this study, we show that both phosphatidic acids and diacylglycerols can serve separately as
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