MC4033

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

MC4033 是一种选择性的，可逆的赖氨酸乙酰转移酶8(KAT8) 抑制剂，其 IC50 值为 12.1 μM。MC4033 具有抗癌活性。MC4033 可诱导凋亡 (apoptosisautophagy)。

MC4033 shows IC50s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively.MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells.

Cell Proliferation AssayCell Line:HT29, HCT116, HeLa, H1299, A549, H460, MCF7, U937, and U251 cellsConcentration:10, 25, 50, and 100 μMIncubation Time:72 hResult:Displayed dose-dependent antiproliferative effects in HCT116, H1299, A549, and U937 cell lines.The inhibition rate of cell proliferation was 70% at 50 μM and >80% at 100 μM in U937 cells.Cell Cycle AnalysisCell Line:HT29, HCT116, and HeLa cells Concentration:50 μM and 100 μM Incubation Time:72 h Result:Propidium iodide (PI) staining showed a slight increase in the percentage of cells with DNA hypodiploid peak, indicative of apoptosis.RT-PCR Cell Line:HCT116 cells Concentration: 100 μM Incubation Time:48h Result:Reduced the mRNA levels of oncogenes UCP2. Immunofluorescence Cell Line: HT29 cells Concentration:50 μM Incubation Time:24 h Result:Reduced H4K16Ac signal intensity by 80%.Western Blot Analysis Cell Line:HCT116 cells Concentration:0,10, 25, 50,100 μM Incubation Time:48 h Result:Showed that the altered ratio of LC3-II/-I and the regulation of p62 autophagy markers indicated the activation of autophagy in HCT116 cells.Apoptosis Analysis Cell Line:HCT116 cells Concentration:100 μM or 10 μM (MC4033/CQ) Incubation Time:72 h Result:Showed that exposure of HCT116 cells to CQ increased the apoptotic effect of KAT8i.

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Apoptosis

Apoptosis

Apoptosis | Histone Acetyltransferase

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28532-21-0

295.29

C16H13N3O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 25 mg/mL (84.66 mM; 超声助溶 )

O=C(O)C1=CC=C(C=C1)N2N=C(C(=CC3=CC=CN3)C2=O)C

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(-20℃)

With Ice Pack

≥ 2 years