Indinavir sulfate ethanolate (MK-639 ethanolate) 是一种口服有效并且具有选择性的HIV-1蛋白酶抑制剂，其对PR的Ki值为 0.54 nM。Indinavir sulfate ethanolate 可通过抑制基质金属蛋白酶-2 水解的激活，抗血管生成以及促癌细胞凋亡来发挥抗癌活性。Indinavir sulfate ethanolate 也是一种SARS-CoV 3CLpro抑制剂。
| 生物活性 | Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selectiveHIV-1proteaseinhibitor with aKiof 0.54 nM forPR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation ofMMPs-2hydrolysis, anti-angiogenesis and inducingapoptosis. Indinavir sulfate ethanolate is also aSARS-CoV3CLproinhibitor[1][2][3][4]. |
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体外研究
(In Vitro) | Indinavir sulfate ethanolate (0-50 μM; 18 h) blocks lymphocyte cell cycle in G0/G1 phase in PBMCs cells and impairs lymphoproliferative responses[1].
Indinavir sulfate ethanolate (40 μM-40 nM; 5 days) inhibits cell invasion and (40 μM-40 nM; 48 h) MMPs-2 activation of the Huh7 and SK-HEP-1 hepatocarcinoma cells in vitro[2].
Cell Viability Assay[1] | Cell Line: | PBMCs (from healthy and HIV-infected volunteers) | | Concentration: | 0-50 μM | | Incubation Time: | 18 h (pretreatment; stimulation with anti-CD3 for an additional 48 hours) | | Result: | Blocked anti-CD3-induced cell-cycle progression in a dose-dependent manner.
Resulted in dose-dependent reduction of lymphoproliferative responses. |
Cell Invasion Assay[2] | Cell Line: | Huh7 and SK-HEP-1 cells | | Concentration: | 40 μM-40 nM | | Incubation Time: | 5 days | | Result: | Reduced ability to invade an in vitro constituted extracellular matrix for both cell lines treated compared with the untreated cells. |
Western Blot Analysis[2] | Cell Line: | Huh7 and SK-HEP-1 cells | | Concentration: | 40 μM-40 nM | | Incubation Time: | 48 h | | Result: | Blocked the conversion of latent MMP-2 to its 62/64-kDa active form. |
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体内研究
(In Vivo) | Indinavir sulfate ethanolate (70 mg/kg; i.g.; once a day for 3 weeks) inhibits the growth of hepatocarcinoma cells in vivo[2].
| Animal Model: | Nude mice(s.c. into Huh7 and SK-HEP-1 cells)[2]. | | Dosage: | 70 mg/kg | | Administration: | Oral gavage; once a day for 3 weeks | | Result: | Delaied the growth of s.c. implanted hepatocarcinoma xenografts in nude mice compared with placebo. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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