5489-57-6
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 |
| 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 |
|---|
| Precursor 7 | |
|---|---|
| DownStream 0 | |
| 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% |