1. Anti-infection
  2. HIV
  3. ITI-367

ITI-367 是一种 HIV-1 抑制剂,靶向 HIV-1 基质蛋白核定位信号 1 (NLS-1) 以及 HIV-1 整合前复合物 (PIC) 与 importin-β 的相互作用。ITI-367 在整合前阶段抑制 HIV-1 复制,减少 2-LTR 环的形成,并将病毒 DNA 滞留于细胞质中。ITI-367 可用于 HIV 感染的研究。

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ITI-367

ITI-367 Chemical Structure

CAS No. : 288246-59-3

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生物活性

ITI-367 is a HIV-1 inhibitor that targets the nuclear localization signal 1 (NLS-1) of HIV-1 matrix protein and the interaction between HIV-1 pre-integration complex (PIC) and importin-β. ITI-367 inhibits HIV-1 replication at the pre-integration stage, reduces the formation of 2-LTR circles, and sequesters viral DNA in the cytoplasm. ITI-367 can be used for the research of HIV infection[1].

体外研究
(In Vitro)

ITI-367 (10 μM) 可特异性抑制 CEM CD4+ T 淋巴细胞中 HIV-1 的复制,且不影响 HTLV-I 的复制[1]
ITI-367 (0-10 μM) 可剂量依赖性地抑制原代单核细胞来源巨噬细胞中 HIV-1 ADA 的复制,其 IC50 为 0.05 μM[1]
ITI-367 (0-10 μM) 可呈剂量依赖性抑制扁桃体来源原代 T 淋巴细胞中 HIV-1 M1 的复制,其 IC50 为 0.7 μM[1]
ITI-367 (0-1 μM; 3 h pre-infection, 12 days post-infection) 可在不产生细胞毒性的情况下,以剂量依赖的方式抑制 HIV-1 LAI 和 HIV-1 SF-162 在体外培养的人扁桃体淋巴组织中的复制[1]
ITI-367 (0-10 μM; 8 days post-infection) 靶向 MA NLS-1 以抑制原代单核细胞来源巨噬细胞中的病毒复制[1]
ITI-367 (0-10 μM; 2 h) 可剂量依赖性地抑制 HIV-1 PICs 与 Jurkat 细胞来源胞质组分中人类 importin α 的结合[1]
ITI-367 (1 μM; 72 h) 可特异性抑制原代单核细胞来源巨噬细胞中 HIV-1 的核转运[1]
ITI-367 (10 μM; 2 h pre-incubation, 72 h post-infection) 可抑制 HIV-1 DNA 在原代单核细胞来源巨噬细胞中的核转位[1]

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

Real Time qPCR[1]

Cell Line: primary monocyte-derived macrophages
Concentration: 1 μM
Incubation Time: 72 h post-infection
Result: Dramatically reduced the amount of 2-LTR circle forms (a marker of nuclear import).
Did not affect the amount of late reverse transcripts (a marker of reverse transcription).

Immunofluorescence[1]

Cell Line: primary monocyte-derived macrophages
Concentration: 10 μM
Incubation Time: 2 h pre-incubation; 72 h post-infection
Result: Resulted in substantially less nuclei-localized fluorescent HIV-1 DNA compared to untreated cells, with viral DNA retained in the cytoplasm.
分子量

336.27

Formula

C16H11F3N2O3

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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产品名称:
ITI-367
目录号:
HY-182566
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