2. PROTAC Epigenetics Metabolic Enzyme/Protease Immunology/Inflammation PI3K/Akt/mTOR
  3. PROTACs Histone Acetyltransferase HIF/HIF Prolyl-Hydroxylase PD-1/PD-L1 PTEN
  4. NP1192

NP1192 是一种高效、选择性的 PROTAC NAT10 降解剂，可降低癌细胞中 NAT10 蛋白的表达并抑制 ac4C 修饰。NP1192 通过破坏 NAT10/HIF-1α/PD-L1 轴，实现对缺氧驱动的糖酵解和免疫抑制的双重抑制，在体外和体内均展现出卓越的抗肿瘤功效，并与抗 PD-L1 联合产生协同作用。NP1192 可用于卵巢癌、宫颈癌、胶质母细胞瘤相关研究。(蓝色: CRBN 配体 (HY-148834); 黑色: 连接子; 粉色: NAT10 配体 (HY-16706))。

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NP1192

NP1192 Chemical Structure

CAS No. : 2966791-41-1

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NP1192 相关抗体

Top Publications Citing Use of Products

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

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HIF-1α HIF

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NP1192 is a potent, selective PROTAC NAT10 degrader that depletes NAT10 protein and inhibits ac4C modification in cancer cells. NP1192 demonstrates dual inhibition of hypoxia-driven glycolysis and immunosuppression via NAT10/HIF-1α/PD-L1 axis disruption, achieving superior antitumor efficacy and synergizing with anti-PD-L1 both in vitro and in vivo. NP1192 can be used for ovarian, cervical, and glioblastoma cancer research. (Blue: CRBN ligand (HY-148834); Black: linker; Pink: NAT10 ligand (HY-16706))[1].

IC50 & Target[1]

NAT10

 

体外研究
(In Vitro)

NP1192 (0-20 μM，24-48 小时) 以剂量和时间依赖的方式诱导 SiHa (人) 和 U14 (鼠) 宫颈癌细胞系中 NAT10 的降解，该过程通过泛素-蛋白酶体系统 (UPS) 而非溶酶体途径进行[1]。
NP1192 (36 小时) 抑制宫颈癌 (SiHa) 细胞的生长，IC50 值为 7.814 μM (耐药细胞中为 76.2 μM)，并且在类器官中也显示出剂量依赖性疗效，卵巢癌 (OV)、宫颈癌 (CESC) 和胶质母细胞瘤 (GBM) 类器官的 IC50 值分别为 9.947、3.048 和 13.76 μM[1]。
NP1192 (20 μM，0-72 小时和 2 周) 显著降低宫颈细胞的活力，诱导细胞周期阻滞，并抑制其侵袭和克隆形成能力[1]。
NP1192 (0.195-50 μM，1-8 天) 可显著减少肿瘤模型 (卵巢癌、宫颈癌和胶质母细胞瘤) 类器官的大小和数量，而相应的正常类器官则未受影响，表明其对非恶性组织的细胞毒性极低[1]。
NP1192 (20 μM，36 小时) 通过降解 NAT10 进而损害 HIF-1α 的表达，重编程宫颈癌细胞的缺氧肿瘤微环境与代谢，其表现为葡萄糖摄取和乳酸生成减少以及 ATP 水平升高，从而破坏糖酵解过程[1]。

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

NP1192 相关抗体:

Western Blot Analysis[1]

Cell Line: SiHa, U14, and HFF-1 cells
Concentration: 0, 1.25, 2.5, 5, 10 and 20 μM
Incubation Time: 24, 36 and 48 h
Result: Led to a substantial depletion of total NAT10 protein in SiHa (human) and U14 (murine) CCa cell lines in a a dose-and time-dependent manner.
Induced degradation rates of 28%, 32%, 40%, and 43% in SiHa cells at concentrations of 1.25, 2.5, 5, and 10 μM, respectively, with a maximum of 69% degradation at 20 μM after 36 h and only 20% degradation after 24 h.
Led to a nearly 70% reduction in the NAT10 protein content in murine U14 cervical cells after 36 h.
Did not exhibit the classical hook effect even at concentrations as high as 20 μM.
Failed to degrade NAT10 significantly when co-treated with MG132 (HY-13259), whereas Bafilomycin A1 (HY-100558) exerted no discernible effect on its degradation efficacy.
Substantially induced minimal cytotoxicity in nonmalignant HFF-1 cells with low NAT10 expression.
Decreased HIF-1α protein levels.
Reversed the induction of hypoxia-related genes under hypoxic conditions, such as HIF1A and PD-L1, at both mRNA and protein levels.

Cell Proliferation Assay[1]

Cell Line: SiHa cells and NAT10-KD SiHa cells
Concentration: 20 μM
Incubation Time: 2 weeks
Result: Led to a substantial decrease in colony formation capacity, with the magnitude of inhibition being only second to that in NAT10-knockdown cells.

Cell Invasion Assay[1]

Cell Line: SiHa cells and NAT10-KD SiHa cells
Concentration: 20 μM
Incubation Time: 36 h
Result: Substantially hindered cell invasion with a significant decrease in the number of cells crossing the basement membrane.
体内研究
(In Vivo)

NP1192 (25 mg/kg，腹腔注射，每 2 天一次，持续一周) 可与抗 PD-L1 抗体协同作用，在 U14-luc 异种移植小鼠模型中抑制肿瘤生长、抑制糖酵解并增强 CD8+ T 效应细胞免疫功能[1]。

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

Animal Model: Female C57BL/6J mice (6-8 weeks old) subcutaneously injected with U14-luc cells[1]
Dosage: 25 mg/kg
Administration: i.p., every 2 days for a week
Result: Significantly reduced tumor volume and tumor burden compared to DMSO at 25 mg/kg.
Significantly inhibited tumor growth when combined with anti-PD-L1 antibody (2.5 mg/kg).
Showed the most pronounced reduction (>80%) in tumor lactate levels when combined with anti-PD-L1 antibody (2.5 mg/kg).
¹⁸F-FDG PET–CT imaging revealed minimal metabolic uptake when combined with anti-PD-L1 antibody, suggesting effective suppresses tumor metabolic activity.
Enhanced the CD8+ Teff cell population, reprograms the TME, and potentiates antitumor immunity when combined with anti-PD-L1 blockade.
Did not cause significant weight loss or systemic toxicity both alone and in combination.
分子量

734.87

Formula

C39H42N8O5S
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

NP1192 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:

NP11922966791-41-1NP 1192NP-1192PROTACsHistone AcetyltransferaseHIF/HIF Prolyl-HydroxylasePD-1/PD-L1PTENHATsHATHypoxia-inducible factorsHIFsHIF-PHPD-1/Programmed death-ligand 1Phosphatase and tensin homologMMAC1NAT10PROTACac4C modificationhypoxia-driven glycolysisimmunosuppressionHIF-1αPD-L1cervicalCCa cellsovarianglioblastomaTMEInhibitorinhibitorinhibit

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