甲异靛

生物活性体外研究体内研究甲异靛试剂级价格

甲异靛

CAS号:97207-47-1
英文名:Meisoindigo
中文名:甲异靛
CBNumber:CB8394558
分子式:C17H12N2O2
分子量:276.29
MOL File:97207-47-1.mol

甲异靛化学性质

熔点 :236-237°C
沸点 :482.0±45.0 °C(Predicted)
密度 :1.381±0.06 g/cm3(Predicted)
储存条件 :Sealed in dry,Room Temperature
溶解度 :insoluble in H2O; insoluble in EtOH; ≥25.85 mg/mL in DMSO with ultrasonic
形态 :powder to crystal
酸度系数(pKa) :11.62±0.20(Predicted)
颜色 :Orange to Brown to Dark red

安全信息

海关编码 :2933.79.1500

甲异靛化学药品说明书

异甲靛片
甲异靛片

甲异靛性质、用途与生产工艺

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.

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.