2. Metabolic Enzyme/Protease Apoptosis
  3. NAMPT Apoptosis
  4. Nampt-IN-17

Nampt-IN-17 是一种具有口服活性的 NAMPT 选择性抑制剂，对人源 NAMPT 的 IC50 为 17 nM，Ki 为 25.9 nM。Nampt-IN-17 可耗竭细胞内 NAD+ 和 ATP，破坏线粒体膜电位，抑制细胞增殖、自我更新、侵袭及迁移，诱导细胞周期阻滞和凋亡 (apoptosis)。Nampt-IN-17 对 NAPRT 缺陷型胃癌细胞表现出选择性活性。Nampt-IN-17 可用于 NAPRT 缺陷型胃癌的相关研究。

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Nampt-IN-17

Nampt-IN-17 Chemical Structure

CAS No. : 3077970-78-3

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Nampt-IN-17 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

Nampt-IN-17 is an selective orally active NAMPT inhibitor with a human NAMPT IC50 of 17 nM and Ki of 25.9 nM. Nampt-IN-17 depletes intracellular NAD+ and ATP, disrupts mitochondrial membrane potential, suppresses cell proliferation, self-renewal, invasion, and migration, induces cell-cycle arrest and apoptosis. Nampt-IN-17 exhibits selective activity against NAPRT-deficient gastric cancer cells. Nampt-IN-17 can be used for the research of NAPRT-deficient gastric cancer[1].

体外研究
(In Vitro)

Nampt-IN-17 (N16) (varying concentrations; 30 min) 可通过非竞争性机制强效抑制重组人源 NAMPT 酶，其 IC50 为 17 nM；且相对于 HDACs 和大多数激酶，该化合物对 NAMPT 具有高选择性，对部分 CYP450 亚型 (尤其是 CYP3A4/5) 仅表现出中等抑制活性[1]。
Nampt-IN-17 (3.1-100 μM) 可直接与重组人源 NAMPT 结合，其 Kd 值为 9.17 μM[1]。
Nampt-IN-17 (72 h) 可选择性强效抑制 NAPRT 缺陷型胃癌细胞 (HGC-27、MKN-74、MKN-45) 的活力，其 IC50 值为 0.0013 至 0.017 μM，而对表达 NAPRT 的正常细胞和癌细胞无明显抑制作用[1]。
Nampt-IN-17 (0.1-6 nM; 24-48 h) 可强效且呈剂量依赖性地抑制 NAPRT 缺陷型 HGC-27 和 MKN-74 胃癌细胞的增殖与克隆形成能力[1]。
Nampt-IN-17 (0.1-1.6 nM; 24 h) 呈剂量依赖性抑制 NAPRT 缺陷型 HGC-27 胃癌细胞的迁移和侵袭[1]。
Nampt-IN-17 (1.6-6.4 nM; 48 h) 可在 NAPRT 缺陷型 HGC-27 胃癌细胞中诱导剂量依赖性的 S 期和 G2/M 期细胞周期阻滞及细胞凋亡[1]。
Nampt-IN-17 (1.6-6.4 nM; 24-48 h) 可呈剂量依赖性地消耗 NAPRT 缺陷型 HGC-27 胃癌细胞内的 NAD+ 和 ATP 水平，并破坏其线粒体膜电位；该效应可被 NMN 逆转，但无法被烟酸逆转[1]。

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

Nampt-IN-17 相关抗体:

Cell Proliferation Assay[1]

Cell Line: NAPRT-deficient gastric cancer cell lines (HGC-27, MKN-74)
Concentration: 0.1, 0.4, 1.6 nM
Incubation Time: 24-48 h (EdU assay)
Result: Dose-dependently suppressed EdU-positive proliferating cells in HGC-27 and MKN-74 cells.
Reduced colony formation in both cell lines.

Cell Migration Assay[1]

Cell Line: NAPRT-deficient gastric cancer cell line (HGC-27)
Concentration: 0.03 nM, 0.1 nM, 0.32 nM, 1 nM, 3.2 nM, 10 nM, 32 nM
Incubation Time: 24, 48, 72 h
Result: Dose-dependently inhibited migration and invasion of HGC-27 cells, with greater activity than lead compound 1 and apatinib at equivalent concentrations.

Cell Cycle Analysis[1]

Cell Line: NAPRT-deficient gastric cancer cell line (HGC-27)
Concentration: 1.6, 3.2, 6.4 nM
Incubation Time: 48 h
Result: Induced concentration-dependent S-phase and G2/M-phase arrest in HGC-27 cells, with 6.4 nM N16 causing 44.3% S-phase and 35.8% G2/M-phase arrest.
Dose-dependently induced apoptosis, with 6.4 nM N16 resulting in 54.6% apoptotic cells, predominantly late apoptosis.

Cell Migration Assay [1]

Cell Line: HGC-27 cells
Concentration: 0.1, 0.4, 1.6 nM
Incubation Time: 24 h
Result: Suppressed the clonogenic potential of gastric cancer cells, reflecting its ability to inhibit long-term cell growth and tumorigenicity.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-∞ MRT0-∞ CL
Rat[1] 2 mg/kg i.v. 0.91 h 0.03 h 14400 μg/L 4155.7 0.33 h 0.48 L/h/kg
Rat[1] 10 mg/kg i.g. 6.32 h 0.67 h 84.07 μg/L 282.9 6.42 h 39.0 L/h/kg
体内研究
(In Vivo)

N16 (7.5-15 mg/kg; i.g.; twice daily; 12 days) 对 NAPRT 缺陷型 HGC-27 胃癌异种移植物表现出剂量依赖性的体内抗肿瘤功效，在 15 mg/kg 每日两次的剂量下达到最高 78.9% 的 TGI[1]。

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

Animal Model: BALB/c nude (male; 4-5 weeks old for efficacy study; 6 weeks old for short-term toxicity study; subcutaneous xenograft of NAPRT-deficient HGC-27 cells)[1]
Dosage: 7.5 mg/kg
Administration: i.g.; twice daily; 12 days
Result: Achieved a tumor growth inhibition (TGI) rate of 65.3%, reduced final tumor weight compared to vehicle, and caused no significant body weight loss or organ toxicity (no histological abnormalities in heart, liver, lung, spleen, or kidney).
Animal Model: BALB/c nude (male; 4-5 weeks old for efficacy study; 6 weeks old for short-term toxicity study; subcutaneous xenograft of NAPRT-deficient HGC-27 cells)[1]
Dosage: 15 mg/kg
Administration: i.g.; twice daily; 12 days
Result: Achieved a TGI rate of 78.9%, reduced final tumor weight compared to vehicle, but caused gradual body weight loss starting on day 5 and splenic histological abnormalities (reduced blue-purple-stained nuclei indicating lymphocyte depletion).
分子量

461.53

Formula

C26H28FN5O2
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

Nampt-IN-17 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

Nampt-IN-173077970-78-3NAMPTApoptosisNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factororally active NAMPT inhibitordeplete intracellular NAD+ and ATPdisrupt mitochondrial membrane potentialinduce cell cycle arrest and apoptosissuppress cell proliferation invasion and migrationNAPRT-deficient gastric cancerHGC-27 cellsMKN-74 cellsMKN-45 cellsAGS cellsGES-1 cellsBALB/c nude miceSD ratsKM miceInhibitorinhibitorinhibit

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