2. Autophagy Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Cell Cycle/DNA Damage
  3. Autophagy Beclin1 Reactive Oxygen Species (ROS) p97
  4. ATI-1

ATI-1 是一种自噬 (autophagy) 起始抑制剂。ATI-1 可靶向含缬酪肽蛋白 (VCP/p97)，破坏其与 UFL1 的相互作用，损害 VCP 相关的 UFM 化稳态，促进 Beclin1 的多泛素化与降解，阻断早期自噬体的形成。ATI-1 可在营养缺乏条件下诱导自噬依赖性恶性肿瘤细胞发生协同性死亡，线粒体膜电位降低、ROS 水平下降以及溶酶体应激。ATI-1 在胰腺腺癌异种移植小鼠模型中展现出抗肿瘤功效。ATI-1 可用于胰腺腺癌、肺癌的研究。

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ATI-1

ATI-1 Chemical Structure

CAS No. : 1242983-93-2

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ATI-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATI-1 is an autophagy initiation inhibitor. ATI-1 targets valosin-containing protein (VCP/p97, disrupts its interaction with UFL1, impairs UFMylation homeostasis associated with VCP, promotes polyubiquitination and degradation of Beclin1, and blocks the formation of early autophagosomes. ATI-1 induces synergistic death of autophagy-dependent malignant tumor cells under nutrient deprivation conditions, accompanied by decreased mitochondrial membrane potential, reduced ROS levels and lysosomal stress. ATI-1 exhibits anti-tumor efficacy in a pancreatic adenocarcinoma xenograft mouse model. ATI-1 can be used for the research of pancreatic adenocarcinoma and lung cancer[1].

体外研究
(In Vitro)

ATI-1 (10 μM; 20 h, plus 20 μM Chloroquine (CQ) (HY-17589A) final 4 h) 可强效抑制 HeLa 细胞中自噬体的形成[1]。
ATI-1 (5-20 μM; 24 h, plus 10 μM for 2 h under EBSS starvation) 可通过降低 Beclin1 蛋白水平并抑制自噬体形成，从而抑制 HeLa 细胞中的自噬起始；可呈剂量依赖性降低 LC3II 水平，而在饥饿条件下则会出现反常的 LC3II 积累[1]。
ATI-1 (5-20 μM; 48 h, plus CQ co-treatment) 可通过降低 Beclin1 蛋白水平，强效抑制自噬依赖型 NCI-H1299 和 MIA PaCa-2 细胞的自噬起始；可呈剂量依赖性降低 LC3II 水平；与 CQ 联用时，还可抑制 MIA PaCa-2 细胞的自噬体形成[1]。
ATI-1 (20 μM; 48-72 h) 可选择性抑制自噬依赖型 NCI-H1299 和 MIA PaCa-2 细胞的增殖、克隆形成能力、迁移及侵袭能力，其效力高于对自噬依赖性较弱的 HeLa 细胞的作用[1]。
ATI-1 (30 μM; 24 h) 可破坏 VCP-UFL1 相互作用，降低 VCP 的 UFMylation 修饰，减弱 VCP-Beclin1 相互作用，并在 HeLa 细胞中选择性损伤特定 VCP 辅因子的相互作用 (VCP-ATXN3、VCP-NPLOC4)[1]。
ATI-1 (3.13-50 μM) 以可测量的亲和力直接结合纯化的全长 VCP (Kd = 25.1 μM) 和纯化的 VCP N 端结构域 (Kd = 32.5 μM)[1]。
ATI-1 (20 μM; 48 h) 在自噬依赖型 NCI-H1299 和 MIA PaCa-2 细胞中诱导 G1 期阻滞，但不会引发显著的细胞凋亡[1]。
ATI-1 (5-10 μM; 2-24 h) 会加剧自噬依赖型 NCI-H1299 和 MIA PaCa-2 细胞在 EBSS 诱导的营养剥夺条件下的代谢脆弱性，进而引发非凋亡性细胞死亡、线粒体膜电位降低、ROS 水平下降以及溶酶体应激；当与饥饿处理联用时，5 μM ATI-1 可在 24 h 内使细胞活力降低约 50%-70%[1]。

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

ATI-1 相关抗体:

Cell Autophagy Assay[1]

Cell Line: HeLa cells
Concentration: 10 μM; 20 μM CQ (final 4 h)
Incubation Time: 20 h; 4 h (CQ)
Result: Markedly reduced the number of autophagosomes per cell.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 10 μM (with 10 μM CQ final 2 h); 5, 10, 20 μM; 20 μM; 10 μM (EBSS starvation)
Incubation Time: 24 h; 24 h; 24 h; 2 h (EBSS starvation)
Result: Prevented LC3II accumulation seen in the CQ-only group at 10 μM for 24 h with 10 μM CQ for the final 2 h.
Induced a dose-dependent reduction in LC3II levels at 5, 10, 20 μM for 24 h.
Reduced Beclin1 protein levels at 20 μM for 24 h.
Caused a paradoxical accumulation of LC3II under EBSS starvation at 10 μM for 2 h, but autophagic flux analysis confirmed reduced LC3 puncta.

Western Blot Analysis[1]

Cell Line: NCI-H1299 cells, MIA PaCa-2 cells
Concentration: 5, 10, 20 μM (NCI-H1299); 10 μM (NCI-H1299, with 10 μM CQ final 2 h); 5, 10, 20 μM (MIA PaCa-2); 10 μM (MIA PaCa-2, with 10 μM CQ final 2 h); 10 μM (MIA PaCa-2, with 20 μM CQ final 6 h); 20 μM (NCI-H1299, MIA PaCa-2)
Incubation Time: 48 h (NCI-H1299); 48 h (NCI-H1299, plus 2 h CQ); 48 h (MIA PaCa-2); 48 h (MIA PaCa-2, plus 2 h CQ); 48 h (MIA PaCa-2, plus 6 h CQ); 48 h (NCI-H1299, MIA PaCa-2)
Result: Induced a dose-dependent reduction in LC3II levels in both NCI-H1299 and MIA PaCa-2 cells over 48 h.
Significantly reduced LC3II levels in MIA PaCa-2 cells at 10 μM for 48 h with 10 μM CQ for the final 2 h, with less pronounced effect in NCI-H1299 cells.
Reduced yellow autophagosome/autolysosome puncta in MIA PaCa-2 cells at 10 μM for 48 h with 20 μM CQ for the final 6 h compared to CQ alone.
Markedly decreased Beclin1 protein levels in both cell lines at 20 μM for 48 h.

Cell Proliferation Assay[1]

Cell Line: NCI-H1299 cells, MIA PaCa-2 cells, HeLa cells
Concentration: 20 μM
Incubation Time: 72 h (CCK-8); 48 h (colony formation, wound healing, Transwell assays)
Result: Showed more pronounced growth-inhibitory effects in NCI-H1299 and MIA PaCa-2 cells than in HeLa cells, with lower IC50 values across time points.
Significantly inhibited proliferation of NCI-H1299 and MIA PaCa-2 cells at 20 μM for 48 h, while HeLa cells remained relatively resistant.
Markedly abrogated long-term clonogenic capacity and significantly impaired migratory and invasive potential of NCI-H1299 and MIA PaCa-2 cells.

Cell Cycle Analysis[1]

Cell Line: NCI-H1299 cells, MIA PaCa-2 cells
Concentration: 20 μM
Incubation Time: 48 h
Result: Led to G1-phase arrest in both cell lines.
Did not induce obvious apoptosis, with no significant increase in apoptotic populations compared to controls.

Western Blot Analysis[1]

Cell Line: NCI-H1299 cells, MIA PaCa-2 cells
Concentration: 20 μM
Incubation Time: 12 h, 24 h, 48 h
Result: Did not increase γH2AX levels at any time point.
Had little effect on ATXN3 abundance, unlike the canonical VCP inhibitor NMS-873 which induced robust γH2AX and reduced ATXN3 levels.

Western Blot Analysis[1]

Cell Line: NCI-H1299 cells, MIA PaCa-2 cells
Concentration: 10 μM (LC3, ROS, lysosomal, mitochondrial assays); 5 μM (cell viability, apoptosis assays)
Incubation Time: 2 h (LC3, ROS, lysosomal, mitochondrial assays); 24 h (cell viability, apoptosis assays)
Result: Enhanced LC3II accumulation compared to EBSS alone when co-treated with ATI-1 and EBSS.
Reduced cell viability by ~50% within 24 h at 5 μM, and up to ~70% in MIA PaCa-2 cells.
No significant increase in apoptotic populations was observed.
Decreased mitochondrial membrane potential, reduced ROS levels, and caused lysosomal stress with impaired membrane integrity and reduced acidic staining when combined with EBSS.
体内研究
(In Vivo)

ATI-1 (50 mg/kg；腹腔注射；每日一次；连续 14 天) 在 MIA PaCa-2 胰腺腺癌异种移植小鼠模型中展现出强效抗肿瘤功效，可显著降低肿瘤生长水平以及瘤内增殖和自噬标志物水平，且全身毒性极低[1]。

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

Animal Model: Nude mice[1]
Dosage: 50 mg/kg
Administration: i.p.; daily; 14 days
Result: Significantly suppressed tumor growth, resulting in reduced final tumor weights and volumes compared to controls.
Markedly reduced intratumoral LC3 and Ki-67 expression.
Caused no significant body weight loss or pathological abnormalities in major organs (heart, liver, spleen, lungs, kidneys).
分子量

400.49

Formula

C16H14F2N2O2S3
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

ATI-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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.

Keywords:

ATI-11242983-93-2ATI1ATI 1AutophagyBeclin1Reactive Oxygen Species (ROS)p97Atg6VCPCdc48autophagy initiationHeLa cellsMIA PaCa-2 cellsNCI-H1299 cellsVCP/p97pancreatic adenocarcinomaValosin-containing proteinUFL1UFMylationInhibitorinhibitorinhibit

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