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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
storage temp.
2-8°C
Quality Level
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
Disclaimer
毒性:有害(C)
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。
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.
Packaging
用惰性气体包装
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
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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