2. Membrane Transporter/Ion Channel Immunology/Inflammation Metabolic Enzyme/Protease PI3K/Akt/mTOR Epigenetics
  3. ATP Synthase COX Oxidative Phosphorylation AMPK
  4. ATP Synthesis-IN-4

ATP Synthesis-IN-4 是一种线粒体靶向小分子配体，可以抑制 ATP 合成。ATP Synthesis-IN-4 能在黑色素瘤细胞中与 mtDNA G4s 结合，从而引起线粒体代谢改变，抑制细胞增殖。ATP Synthesis-IN-4 抑制黑色素瘤细胞关键线粒体呼吸链蛋白 (CYTB、ATP8、COX1、COX3、ND2) 的翻译，并下调 OXPHOS 复合物的表达，同时激活 AMPK 的磷酸化，诱导代谢重编程以上调糖酵解。ATP Synthesis-IN-4 可用于黑色素瘤的相关研究。

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ATP Synthesis-IN-4

ATP Synthesis-IN-4 Chemical Structure

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ATP Synthesis-IN-4 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATP Synthesis-IN-4 is a mitochondria-targeted small-molecule ligand that inhibits ATP synthesis. ATP Synthesis-IN-4 binds to mtDNA G4s in melanoma cells, thereby inducing changes in mitochondrial metabolism and inhibiting cell proliferation. ATP Synthesis-IN-4 suppresses the translation of key mitochondrial respiratory chain proteins (CYTB, ATP8, COX1, COX3, ND2) in melanoma cells, downregulates the expression of OXPHOS complexes, activates the phosphorylation of AMPK, and induces metabolic reprogramming to upregulate glycolysis. ATP Synthesis-IN-4 is applicable to relevant research on melanoma[1].

IC50 & Target[1]

COX-1

 

COX-3

 

体外研究
(In Vitro)

ATP Synthesis-IN-4 (B1N) (48 h) 可强效抑制恶性黑色素瘤细胞系 A375、SK-MEL-2 和 A2058 的增殖，IC50 值分别为 7.0 μM、8.0 μM 和 16.8 μM，且对非癌性 BJ 皮肤成纤维细胞的毒性较低 (IC50 >50 μM)[1]。
ATP Synthesis-IN-4 (0-7 μM; 20-60 min) 可选择性定位至活 A375 细胞的线粒体中，[1]。
ATP Synthesis-IN-4 (0-7 μM; 60 min) 浓度依赖的方式破坏 A375 细胞的线粒体膜电位[1]。
ATP Synthesis-IN-4 (1 μM; 20 min) 递送至 A375 细胞线粒体的过程主要依赖线粒体膜电位，因为 FCCP (HY-100410) 诱导的 MMP 降低会抑制其摄取，而 CsA (HY-B0579) 介导的 mPTP 阻断则无此作用[1]。
ATP Synthesis-IN-4 (5 μM; 1 min shaking, RT incubation) 可在体外以高亲和力选择性结合 mtDNA G4 结构，其顶级靶点的 Kd 为 0.65−1.28 μM[1]。
ATP Synthesis-IN-4 (0-7 μM; 48 h) 以浓度依赖的方式下调 A375 细胞中线粒体呼吸链相关基因的表达 (ND1, ND2, COX1, COX2, CYTB, ATP6 等)[1]。
ATP Synthesis-IN-4 (0-7 μM; 48 h) 可抑制 A375 细胞中关键线粒体呼吸链蛋白 (CYTB、ATP8、COX1、COX3、ND2) 的翻译，并下调 OXPHOS 复合物的表达，同时激活 AMPK 的磷酸化[1]。
ATP Synthesis-IN-4 (0-7 μM; 2 h) 会损伤 A375 细胞中的线粒体氧化磷酸化，处理 2 h 后可使 ATP 生成量在 3.5 μM 浓度下降低约 83%、在 7 μM 浓度下降低约 98%，同时以浓度依赖的方式上调糖酵解[1]。
ATP Synthesis-IN-4 (0-7 μM; 48 h) 可将 A375 黑色素瘤细胞阻滞于细胞周期的 S 期[1]。
ATP Synthesis-IN-4 (1.75 μM; 48 h) 与 0.2 μM Vemurafenib (HY-12057) 联用对 A375 细胞表现出协同抗增殖活性 (CI=0.67)，在处理 48 h 后将 ATP Synthesis-IN-4 对 A375 细胞的 IC50 降至 0.63 μM[1]。
ATP Synthesis-IN-4 (1.75 μM; 72 h) 与 0.2 μM Vemurafenib 联合作用 72 h 后，可诱导 A375 黑色素瘤细胞发生急性细胞衰老[1]。

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

ATP Synthesis-IN-4 相关抗体:

Immunofluorescence[1]

Cell Line: A375 cells
Concentration: 0, 1, 3.5, 7 μM
Incubation Time: 20, 60 min
Result: Was selectively localized to the mitochondria.
Decreased the fluorescence intensity of rhodamine 123.
Decreased the fluorescent foci of
B1N with FCCP pretreatment.

Real Time qPCR[1]

Cell Line: A375 cells
Concentration: 0, 3.5, 7 μM
Incubation Time: 48 h
Result: Downregulated expression of most mitochondrial respiratory chain-related mRNAs by at least 75% at 7 μM in a concentration-dependent manner; showed no significant downregulation of nuclear KRAS and VEGF mRNAs.

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 0, 3.5, 7 μM
Incubation Time: 48 h
Result: Markedly repressed expression of mitochondrial proteins CYTB, ATP8, COX1, COX3, and ND2.
Downregulated four of five mitochondrial respiratory chain complexes (I, II, III, IV) in the total OXPHOS profile.
Upregulated phosphorylated AMPKα (Thr172) in a concentration-dependent manner.

Cell Cycle Analysis[1]

Cell Line: A375 cells
Concentration: 3.5-7 μM
Incubation Time: 48 h
Result: Caused significant cell cycle arrest in the S phase; increased S phase population to ~22% and ~30% at 3.5 μM and 7 μM respectively, with corresponding decreases in G0/G1 phase, compared to ~18% in control cells.

Cell Proliferation Assay[1]

Cell Line: A375 cells
Concentration: 1.75 μM (combined with 0.2 μM Vemurafenib)
Incubation Time: 48 h
Result: Showed a synergistic effect with a combination index (CI) value of 0.67 when combined with 0.2 μM Vemurafenib; reduced the IC50 of ATP Synthesis-IN-4 to 0.63 μM in combination with 0.2 μM Vemurafenib.
分子量

419.38

Formula

C20H23BrN2OS
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

ATP Synthesis-IN-4 相关分类

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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:

ATP Synthesis-IN-4ATP SynthaseCOXOxidative PhosphorylationAMPKCyclooxygenaseAMP-activated protein kinasemitochondria-targeted small-molecule ligandATP synthesisA375 cellsSK-MEL-2 cellsA2058 cellsmelanoma
Inhibitorinhibitorinhibit

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