甲异靛
中文名称:
甲异靛
中文同义词:
N-甲基-(3,3-双-二氢吲哚)-2,2-二酮;甲异靛;异甲靛;甲异靛, >96%
英文名称:
Meisoindigo
英文同义词:
1-METHYL-3,3-BIINDOLE-2,2(1H,1H)-DIONE;3-(1,2-dihydro-2-oxo-3h-indol-3-ylidene)-1,3-dihydro-1-methyl-2h-indol-2-one;MEISOINDIGO;N-methylisoindigotin;Dian III;Methylisoindigotin;Natura-α;Meisoindigo 3-(1,2-Dihydro-2-oxo-3H-indol-3-ylidene)-1,3-dihydro-1-methyl-2H-indol-2-one
CAS号:
97207-47-1
分子式:
C17H12N2O2
分子量:
276.29
EINECS号:
200-256-5
相关类别:
小分子抑制剂;小分子抑制剂，天然产物;医药化工中间体;标准品;中药对照品;Inhibitors
Mol文件:
97207-47-1.mol
熔点
236-237°C
储存条件
Sealed in dry,Room Temperature
生物活性
Meisoindigo (Dian III) 是 Indirubin (HY-N0117) 的衍生物，可以造成急性髓细胞性白血病 (AML) 细胞周期在 G0/G1 期停滞，并诱导凋亡。Meisoindigo 具有很高的抗肿瘤活性。
体外研究
Meisoindigo (Dian III; 5-20 μM; for 24 hours) inhibits growth of the AML cell lines.
Meisoindigo (10 μM; for 24 hours) induces apoptosis of acute myeloid leukemia.
Meisoindigo (5-10 μM; for 24 hours) causes cell-cycle arrest.
Meisoindigo (5-10 μM; for 24 hours) increases the cleaved caspase-3 and pro-apoptotic Bak, and decreases Bcl-2 and Bcl-xL levels in HL-60 cells.
Meisoindigo (10, 30, 50, 100, 150 μM; 24 hours) interdicts LPS-induced (1 μg/mL) NLRP3 inflammasome activation and M1/M2 polarization through down-regulation of TLR4 pathways after OGD/R in HT-22 and BV2 cells.
Cell Viability Assay
Cell Line: HL-60, NB4, U937 leukemic cell lines
Concentration: 5, 10, 15, 20 μM
Incubation Time: For 24 hours
Result: Inhibited growth of the AML cell lines in a dose- and time-dependent manner.
Apoptosis Analysis
Cell Line: HL-60 cells
Concentration: 10 μM
Incubation Time: For 24 hours
Result: Induced apoptosis of acute myeloid leukemia.
Cell Cycle Analysis
Cell Line: HL-60 cells
Concentration: 5, 10 μM
Incubation Time: For 24 hours
Result: Caused cell-cycle arrest, with more cells in sub-G1 and G0/G1 phases and fewer cells in the S phase, in a dose-dependent manner.
Western Blot Analysis
Cell Line: HL-60 cells
Concentration: 5, 10 μM
Incubation Time: For 24 hours
Result: Increased the cleaved caspase-3 and pro-apoptotic Bak, and decreased Bcl-2 and Bcl-xL levels in HL-60 cells.
Cell Line:
HL-60, NB4, U937 leukemic cell lines
Concentration:
5, 10, 15, 20 μM
Incubation Time:
For 24 hours
Result:
Inhibited growth of the AML cell lines in a dose- and time-dependent manner.
Cell Line:
HL-60 cells
Concentration:
10 μM
Incubation Time:
For 24 hours
Result:
Induced apoptosis of acute myeloid leukemia.
Cell Line:
HL-60 cells
Concentration:
5, 10 μM
Incubation Time:
For 24 hours
Result:
Caused cell-cycle arrest, with more cells in sub-G1 and G0/G1 phases and fewer cells in the S phase, in a dose-dependent manner.
Cell Line:
HL-60 cells
Concentration:
5, 10 μM
Incubation Time:
For 24 hours
Result:
Increased the cleaved caspase-3 and pro-apoptotic Bak, and decreased Bcl-2 and Bcl-xL levels in HL-60 cells.
体内研究
Meisoindigo (Dian III; 50-150 mg/kg; IP; daily; for 14 days) has anti-leukemic activity in vivo.
Meisoindigo (2, 4, 8, 12 mg/kg; IP; before MCAO and 2 h after reperfusion) significantly reduces infarct volume, ameliorates neurological deficits 3 days after middle cerebral artery occlusion (MCAO) in Wild-type C57BL/6J mice (25-30 g). Meisoindigo reduces edema and lowers AQP4 expression in the brain.
Animal Model: NOD/SCID mice, 6-8 weeks old, with HL-60 leukemic cells
Dosage: 50, 100, 150 mg/kg
Administration: IP; daily; for 14 days
Result: Had anti-leukemic activity in vivo.
Animal Model:
NOD/SCID mice, 6-8 weeks old, with HL-60 leukemic cells
Dosage:
50, 100, 150 mg/kg
Administration:
IP; daily; for 14 days
Result:
Had anti-leukemic activity in vivo.
