1. Anti-infection Metabolic Enzyme/Protease
  2. HIV Protease HIV
  3. HIV-1 protease-IN-6

HIV-1 protease-IN-6 (compound 17d) 是一种有效的 HIV-1 蛋白酶 (HIV-1 protease) 抑制剂,其 IC50 为 21 pM,Ki 为 4.7 pM。HIV-1 protease-IN-6 对 DRV (darunavir) 耐药病毒突变体表现出强大的抗病毒活性 (antiviral activity),抑制强度甚至超过对野生型病毒。

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HIV-1 protease-IN-6 Chemical Structure

HIV-1 protease-IN-6 Chemical Structure

CAS No. : 2892016-32-7

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生物活性

HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus[1].

IC50 & Target

HIV-1

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK-293T CC50
> 100 μM
Compound: 17d
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
[PMID: 35483138]
SUP-T1 EC50
0.74 μM
Compound: 17d
Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by
Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by
[PMID: 35483138]
体外研究
(In Vitro)

HIV-1 protease-IN-6 (compound 17d) (10 μM; 48 h) exhibits full inhibition against the late stage of HIV-1 replication cycle while the inhibition rate is 2.6% on early stage at the cellular level[1].
HIV-1 protease-IN-6 (10 μM; 24 h) displays antiviral activity against HIV-1NL4-3 with an EC50 value of 0.74 μM, and exhibits anti-DRV-resistant tendency with an EC50 value of 0.61 μM towards DRV-resistant variant[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

530.61

Formula

C27H31FN2O6S

CAS 号
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.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
HIV-1 protease-IN-6
目录号:
HY-150549
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