AGX51

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AGX51 是 DNA 结合 (ID) 蛋白抑制剂的拮抗剂。 AGX51 处理导致泛 Id 降解、细胞周期停滞和细胞死亡。

AGX51 is an antagonist of inhibitor of DNA binding (ID) proteins. AGX51 treatment lead to pan-Id degradation, cell cycle arrest, and cell death.(In Vitro):AGX51 inhibits the Id1-E47 interaction. AGX51 is well-tolerated in mice and phenocopies the genetic loss of Id expression in AMD and ROP models by inhibiting retinal neovascularization. AGX51 may have utility in the management of multiple diseases.

Western Blot Analysis Cell Line:4T1 cells Concentration:0, 5, 10, 20, 40 and 80 μM Incubation Time:24 hours Result:Decreased ID1 protein levels starting at a concentration of 40 μM in 4T1 cells.Western Blot Analysis Cell Line:4T1 cells Concentration:40 μM Incubation Time:0, 2, 4, 8 , 12, 24, 48 and 72 hoursResult:Decreased ID1 protein levels starting at 4 h, while until 24 h ID1 protein completely loss.Cell Viability Assay Cell Line:4T1 cells, HMLE RAS Twist, MDA-MB-157, MDA-MB-436, MDA-MB-231, MDA-MB-453, BT-474, MDA-MB-361, SK-BR-3, MCF-7, T47-D, PDX-BR7, PDX-IBT and PDX-BR11 Concentration:40 μM Incubation Time:24 hours Result:Inhibited 4T1, HMLE RAS Twist, MDA-MB-157, MDA-MB-436, SK-BR-3, MCF-7, PDX-BR7, PDX-IBT and PDX-BR11 cell lines with IC50s of 26.66, 8.7, 22.28, 30.91, 36.55, 60, 10.89, 11.97 and 18.56 μM, respectively.Cell Cycle Analysis Cell Line:4T1 cells Concentration:40 μM Incubation Time:24 and 48 hours Result:Affected cell cycle of 4T1 cells with a G0/G1 phase accumulation.Cell Viability Assay Cell Line:4T1 cells Concentration:40 μM Incubation Time:4 and 24 hours Result:Reduced phospho-histone H3 levels in 4T1 cells.Cell Viability Assay Cell Line:4T1 cells Concentration:40 μM Incubation Time:24 hours Result:Increased ROS level of 4T1 cells and indicated ROS production is a main mechanism of cell killing.

Animal Model:Balb/c mice with luciferase-labeled 4T1 cellsDosage:50 mg/kg Administration:Intraperitoneal injection; 60 mg/kg twice a day; for 4 weeks Result:Inhibited lung metastasis development.Animal Model:A/J mice with AOM colon tumor model Dosage:15 mg/kg Administration:Intraperitoneal injection; 15 mg/kg twice a day; for 3 weeks Result:Dreased the colon tumors and exhibited anti-tumor activity in AOM colon tumor mice.

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Others

Other Targets

Parasite| Sodium Channel

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330834-54-3

431.532

C27H29NO4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (231.74 mM)

CCC(=O)N(CCC(c1ccc2OCOc2c1)c1ccccc1OC)Cc1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years