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经验公式(希尔记法):
C18H29N3O6
化学文摘社编号:
分子量:
383.44
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
CA-074, ≥98% (HPLC)
SMILES string
CCCNC(=O)[C@H]1O[C@@H]1C(=O)N[C@@H]([C@H](C)CC)C(=O)N2CCC[C@H]2C(O)=O
InChI key
ZEZGJKSEBRELAS-NSIINPIOSA-N
InChI
1S/C18H29N3O6/c1-4-8-19-15(22)13-14(27-13)16(23)20-12(10(3)5-2)17(24)21-9-6-7-11(21)18(25)26/h10-14H,4-9H2,1-3H3,(H,19,22)(H,20,23)(H,25,26)/t10?,11-,12-,13-,14-/m0/s1
biological source
synthetic (organic)
assay
≥98% (HPLC)
form
powder
solubility
methanol: 1 mg/mL, clear, colorless
storage temp.
−20°C
Quality Level
Application
CA-074 已被用作组织蛋白酶 B 抑制剂:
- 利用 HeLa 细胞研究其对携带 R642M 和 N714K 的 S 蛋白的假型病毒的影响
- 确定自噬在葡萄糖缺乏(GD)诱导的损伤中的作用
- 研究其暴露于组织蛋白酶 B(CATB)对神经元功能的影响
Biochem/physiol Actions
CA-074 是组织蛋白酶 B 的有效和选择性抑制剂。它有助于研究组织蛋白酶 B 在体内的生物学功能。研究表明,CA-074 在还原条件下也能抑制组织蛋白酶 L。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
M Murata et al.
FEBS letters, 280(2), 307-310 (1991-03-25)
A series of new epoxysuccinyl peptides were designed and synthesized to develop a specific inhibitor of cathepsin B. Of these compounds, N-(L-3-trans-ethoxycarbonyloxirane-2-carbonyl)-L-isoleucyl-L-proli ne (compound CA-030) and N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-prol ine (compound CA-074) were the most potent and specific inhibitors of cathepsin B
Igor Stern et al.
The Biochemical journal, 381(Pt 2), 511-517 (2004-04-16)
The crystal structure of the inhibitor NS-134 in complex with bovine cathepsin B reveals that functional groups attached to both sides of the epoxysuccinyl reactive group bind to the part of active-site cleft as predicted. The -Leu-Pro-OH side binds to
The cathepsin B-selective inhibitors CA-074 and CA-074Me inactivate cathepsin L under reducing conditions
Steverding D
Open enzyme inhibition Journal, 4, 11-16 (2011)
Giuseppe Nicastro et al.
Proceedings of the National Academy of Sciences of the United States of America, 102(30), 10493-10498 (2005-07-16)
The Josephin domain plays an important role in the cellular functions of ataxin-3, the protein responsible for the neurodegenerative Machado-Joseph disease. We have determined the solution structure of Josephin and shown that it belongs to the family of papain-like cysteine
Masashi Asai et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 25(10), 3720-3730 (2011-07-13)
γ-Secretase catalyzes the cleavage of the intramembrane region of the Alzheimer amyloid precursor protein (APP), generating p3, amyloid-β peptide (Aβ), and the APP intracellular domain (AICD). Although a γ-secretase inhibitor has been shown to cause an accumulation of the APP
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