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经验公式(希尔记法):
C19H12N2O2
化学文摘社编号:
分子量:
300.31
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
N(c3cc4c(cncc4)cc3)C1=CC(=O)C(=O)c2c1cccc2
InChI key
NYDMVPHEEBVAHT-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
faint brown-red to dark red
solubility
DMSO: 0.5 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Hsp90 inhibitor with anti-cancer efficacy in vitro and in vivo.
YZ129 is an ATP site-targeting Hsp90 inhibitor (IC50 = 29.5 nM against 2.5 nM geldanamycin-FITC for binding human HSP90α) that prevents thapsigargin (1 μM)-induced NFAT nuclear translocation in HeLa cells (IC50 = 820 nM) by blocking HSP90 client calcineurin-mediated NFAT dephosphorylation. YZ129 (5 μM; 24-48 hr) suppresses U87 glioblastoma (GBM) cell migration and proliferation as a result of G2/M arrest and apoptosis induction. Daily intraperitoneal administration is efficacious against U87 xenografts (s.c.; bilateral posterior limbs)-derived tumor growth in mice in vivo.
Other Notes
Product may exist in a Tautomeric Form.
存储类别
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Zhenzhen Liu et al.
Cell chemical biology, 26(3), 352-365 (2019-01-15)
Glioblastoma (GBM) is among the most common and malignant types of primary brain tumors in adults, with a dismal prognosis. Although alkylating agents such as temozolomide are widely applied as the first-line treatment for GBM, they often cause chemoresistance and
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