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Acetazolamide

CAS No. : 59-66-5

MCE 站：Acetazolamide

产品活性：Acetazolamide 是一种碳酸酐酶 (carbonic anhydrase，CA) IX 抑制剂，抑制 hCA IX，IC₅₀ 为 30 nM。利尿剂。

研究领域：Metabolic Enzyme/Protease  |  Autophagy

作用靶点：Carbonic Anhydrase  |  Autophagy

In Vitro: Acetazolamide also inhibits hCA II with an IC₅₀ of 130 nM.
Acetazolamide (Ace) is a small heteroaromatic sulfonamide that binds to various carbonic anhydrases with high affinity, acting as a carbonic anhydrase (CA) inhibitor.
Compared with the control group, the high Acetazolamide concentration (AceH, 50 nM), Cisplatin (Cis; 1 µg/mL) ａnd Cis combined with the low Acetazolamide concentration (AceL, 10 nM) treatments significantly reduces viability of Hep-2 cells.
Treatment with the Acetazolamide/Cis combination significantly increases the expression levels of P53, as both AceL+Cis ａnd AceH+Cis treatments result in significantly increased P53 protein expression levels compared with the control group. The Ace/Cis combination treatment significantly reduces the bcl-2/bax expression ratio, ａnd increases the expression of caspase-3 protein, compared with the control group. AceL, AceH, Cis ａnd AceL+Cis treatments significantly reduce the bcl-2/bax ratio compared with the control group.
Combined Ace ａnd Cis treatment effectively promotes apoptosis in Hep-2 cells.
Combined treatment with Ace/Cis markedly decreases the expression of AQP1 mRNA in Hep-2 cells. Both AceH ａnd AceL+Cis treatments decrease the expression of aquaporin-1 (AQP1) mRNA in Hep-2 cells compared with the control group.

In Vivo: Acetazolamide (40 mg/kg) significantly potentiates the inhibitory effect of MS-275 on tumorigenesis in neuroblastoma (NB) SH-SY5Y xenografts.
Acetazolamide (40 mg/kg) and/or MS-275 treatment reduce expression of HIF1-α ａnd CAIX in NB SH-SY5Y xenograft.
Acetazolamide (40 mg/kg), MS-275 ａnd Acetazolamide+MS-275 reduce expression of mitotic ａnd proliferative markers in NB SH-SY5Y xenografts.

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