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SML2640

Sigma-Aldrich

YZ129

≥98% (HPLC)

Synonym(s):

4-(6-Isoquinolinylamino)-1,2-naphthalenedione, 4-(Isoquinolin-6-ylamino)naphthalene-1,2-dione, YZ-129, YZ129

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About This Item

Empirical Formula (Hill Notation):
C19H12N2O2
CAS Number:
1643120-60-8
Molecular Weight:
300.31
MDL number:
MFCD31813767
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

faint brown-red to dark red

solubility

DMSO: 0.5 mg/mL, clear

storage temp.

2-8°C

SMILES string

N(c3cc4c(cncc4)cc3)C1=CC(=O)C(=O)c2c1cccc2

InChI key

NYDMVPHEEBVAHT-UHFFFAOYSA-N

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.

Storage Class

13 - Non Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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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