Proteasome inhibitor IX

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

AM 114 是 20S 蛋白酶体胰凝乳蛋白酶样活性的抑制剂 (IC50 ~1 μM)。

AM 114 is an inhibitor of chymotrypsin-like activity of the 20S proteasome (IC50 ~1 μM). AM 114 shows potent anticancer activity. AM 114 exhibits HCT116 p53+/+ cells growth inhibitory activity(IC50 = 1.49 μM).(In Vitro):AM114 exhibits potent activity against p53+/+ cells in colony formation assay, with an IC50 value of 0.6 μM. AM114 treatment inhibits the chymotrypsin-like activity of the 20S proteasome in vitro, leading to a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells. In HCT116 p53+/+ cells, AM114(0.1-10 μM) treatment causes a loss of cell survival in the p53+/+ and p53-/- cells by approximately 70 and 20%, respectively at a concentration of 1 μM.

Proteasome inhibitor IX (AM114; 0.1-10 μM; 14 days; HCT116 p53+/+ cells) treatment causes a loss of cell survival in the p53+/+ and p53-/- cells by approximately 70 and 20%, respectively at a concentration of 1 μM. Proteasome inhibitor IX (AM114) exhibits potent activity against p53+/+ cells in colony formation assay, with an IC50 value of 0.6 μM. Incubation of HCT116 p53+/+ cells with 1 μM Proteasome inhibitor IX (AM114) causes 28% of the cells to exhibit positive Annexin V staining at 48 h, and this fraction of dead cells increased to 76% at 72 h.Proteasome inhibitor IX (AM114) treatment inhibits the chymotrypsin-like activity of the 20S proteasome in vitro, leading to a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells.

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PS-IX | AM114

Proteasome/Ubiquitin

Proteasome

CRAC channel

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856849-35-9

377.01

C20H21B2NO5

>98% (HPLC)

In Vitro:?DMSO : 6.25 mg/mL (16.58 mM)

O=C(/C(CN(C)C/1)=C\C2=CC=C(B(O)O)C=C2)C1=C/C3=CC=C(B(O)O)C=C3

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(-20℃)

With Ice Pack

≥ 2 years