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关于此项目
经验公式(希尔记法):
C19H17NO3
化学文摘社编号:
分子量:
307.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
PTP CD45 抑制剂, The PTP CD45 Inhibitor, also referenced under CAS 345630-40-2, controls the biological activity of PTP CD45. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
SMILES string
N(c1cc2c(cc1)c3c(cccc3)C(=O)C2=O)C(=O)C(C)(C)C
InChI
1S/C19H17NO3/c1-19(2,3)18(23)20-11-8-9-13-12-6-4-5-7-14(12)16(21)17(22)15(13)10-11/h4-10H,1-3H3,(H,20,23)
InChI key
VZQDDSYKVYARDW-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
red-violet
solubility
DMSO: 5 mg/mL, ethanol: 5 mg/mL
shipped in
wet ice
Quality Level
General description
一种具有细胞渗透性、有效、选择性、竞争性和可逆的CD45抑制剂(以pNPP为底物,IC50=200 nM,CD45 lck为3.8 µM,PTP1B lck为>30 µM),具有抗增殖特性。据报道,还可阻断有效阻断T细胞受体介导的增殖(IC50 = 100 nM)。与其他 1,2-萘二酮类似物相比,细胞毒性较低(CC50 = 3.5 µM)。菲二酮基团不用作硫醇氧化剂。10号染色体上缺失的磷酸酶张力蛋白同源物(PTEN)最有效的抑制剂之一,可增强多种细胞中的PIP3信号,并改善中性粒细胞减少相关肺炎小鼠模型中粒细胞输注的效果。
Biochem/physiol Actions
主靶
CD45,使用pNPP作为底物
CD45,使用pNPP作为底物
产物不与ATP竞争。
可逆性:是
细胞可渗透性:是
靶标IC50:使用pNPP或磷酸化Ick505肽作为底物,对于CD45分别为200 nM或3.8 µM
Packaging
用惰性气体包装
Other Notes
Li, Y., et al. 2011.Blood117, 6702.
Urbanek, R.A., et al. 2001.J. Med. Chem.44, 1777.
Urbanek, R.A., et al. 2001.J. Med. Chem.44, 1777.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性:有害(C)
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
Xiaorong Hu et al.
Aging, 13(2), 2768-2779 (2021-01-08)
Atherosclerosis is the main cause of cardiovascular disease. Systemic inflammation is one important characteristic in atherosclerosis. Pro-inflammatory macrophages can secrete inflammatory factors and promote the inflammation of atherosclerosis. It has a great value for the treatment of atherosclerosis by inhibiting
Peter Szodoray et al.
Cell reports, 36(6), 109525-109525 (2021-08-12)
Humoral immunity relies on the efficient differentiation of memory B cells (MBCs) into antibody-secreting cells (ASCs). T helper (Th) signals upregulate B cell receptor (BCR) signaling by potentiating Src family kinases through increasing CD45 phosphatase activity (CD45 PA). In this
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