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5489-57-6

5489-57-6 structure
5489-57-6 structure
  • Name: Arborinine
  • Chemical Name: 1-hydroxy-2,3-dimethoxy-10-methylacridin-9-one
  • CAS Number: 5489-57-6
  • Molecular Formula: C16H15NO4
  • Molecular Weight: 285.29
  • Create Date: 2018-03-05 08:00:00
  • Modify Date: 2024-01-06 11:50:20
  • Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity [1][2].

Name 1-hydroxy-2,3-dimethoxy-10-methylacridin-9-one
Synonyms Arborinine
Arborinin
1-hydroxy-2,3-dimethoxy-10-methyl-10H-acridin-9-one
1-hydroxy-2,3-dimethoxy-10-methyl-9-acridone
1-Hydroxy-2,3-dimethoxy-10-methyl-10H-acridin-9-on
Arbornine
Description Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity [1][2].
Related Catalog
Target

LSD1

In Vitro Arborinine (0, 5, 15, 30 µM; 48 h) 增加 H3K4me1/2、H3K9me1/2、E-cad 蛋白的表达[1]。 Arborinine (20 µM) 降低 786O 细胞中 UBE2O 蛋白水平的表达[1]。 Arborinine (20 µM) 诱导细胞周期停滞在 S 期并抑制细胞凋亡[1]。 Cell Proliferation Assay[1] Cell Line: 786O, A498, 769P, Caki1, OSRC2 cells Concentration: 0-100 µM Incubation Time: 48, 72 h Result: Showed antiproliferative activity with IC50s of 30.62, 39.09, 15.67, 31.42, 30.35 µM at 48 h, 20.92, 27.01, 14.94, 30.26, 17.37 µM at 72 h for 786O, A498, 769P, Caki1, OSRC2 cells, respectively. Western Blot Analysis[1] Cell Line: 786O cells Concentration: 0, 5, 15, 30 µM Incubation Time: 48 h Result: Increased the expression of H3K4me1/2 and H3K9me1/2 protein in a dose-dependent manner. Cell Cycle Analysis[1] Cell Line: 786O and A498 cells Concentration: 20 µM Incubation Time: Result: Induced increased population in S phase and decreased population in G1 phase, significantly inhibited both early and late apoptosis of ccRCC cells
In Vivo Arborinine (40、80 mg/kg;灌胃; 21 天) 在小鼠体内显示出抗肿瘤活性[2]。 Animal Model: BALB/c nude mice (SGC-7901 cells and SGC-7901/ADR cells)[2] Dosage: 40, 80 mg/kg Administration: P.o.; for 21 days Result: Inhibited the growth of tumors while unchanged the body weights.
References

[1]. Feng C, et al. Arborinine from Glycosmis parva leaf extract inhibits clear-cell renal cell carcinoma by inhibiting KDM1A/UBE2O signaling. Food Nutr Res. 2022 Sep 16;66.  

[2]. Chu Y, et al. Arborinine, a potential LSD1 inhibitor, inhibits epithelial-mesenchymal transition of SGC-7901 cells and adriamycin-resistant gastric cancer SGC-7901/ADR cells. Invest New Drugs. 2021 Jun;39(3):627-635.  

Density 1.296g/cm3
Boiling Point 508.4ºC at 760 mmHg
Molecular Formula C16H15NO4
Molecular Weight 285.29
Flash Point 261.3ºC
Exact Mass 285.10000
PSA 60.69000
LogP 2.41450
Index of Refraction 1.621
HS Code 2933990090
HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%