2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Phosphodiesterase (PDE) STING
  4. Enpp-1-IN-27

Enpp-1-IN-27 是一种选择性 ENPP1 抑制剂，其 IC50 为 14.68 nM，对 ENPP2 的选择性约为 410 倍，对 ENPP3 的选择性约为 10 倍。Enpp-1-IN-27 可稳定 cGAMP 水平并激活 STING 通路，从而促进细胞因子释放并增强先天免疫反应。Enpp-1-IN-27 可激活 ISRE 并增强 cGAMP 介导的免疫反应，并在 4T1 和 CT26 同基因小鼠模型中显示出显著的抗肿瘤效果。Enpp-1-IN-27 可用于乳腺癌和结肠癌的研究。

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Enpp-1-IN-27

Enpp-1-IN-27 Chemical Structure

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Enpp-1-IN-27 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Enpp-1-IN-27 is a selective ENPP1 inhibitor with an IC50 of 14.68 nM, exhibiting approximately 410-fold selectivity against ENPP2 and 10-fold selectivity against ENPP3. Enpp-1-IN-27 stabilizes cGAMP levels and activates the STING pathway, promoting cytokine release and enhancing innate immune responses. Enpp-1-IN-27 induces ISRE activation and amplified cGAMP-mediated immune responses and shows the desired antitumor efficacy in the 4T1 and CT26 syngeneic mouse models. Enpp-1-IN-27 can used for the studies of breast cancer and colon cancer[1].

体外研究
(In Vitro)

Enpp-1-IN-27 (Compound 31) (0-50 μM, 25 h) 在 THP-1 细胞 (EC50 = 16.5 μM) 和 HCT116 细胞中均比单独使用 cGAMP 更有效地增强 cGAMP 介导的 STING 活性[1]。
Enpp-1-IN-27 (25-50 μM，4-25 h) 通过激活 THP-1 和 HCT116 细胞中的 STING 信号通路来刺激 I 型干扰素反应[1]。
Enpp-1-IN-27 (10 μM) 对五种主要 CYP 酶亚型 (CYP1A2、CYP2C9、CYP2C19、CYP2D6 和 CYP3A4) 的抑制作用可忽略不计，并表现出优异的代谢稳定性，在人、小鼠和大鼠肝微粒体中，微粒体稳定性超过 95%[1]。
Enpp-1-IN-27 表现出良好的动力学溶解度 (191 μM)，并且对人类 Ether-à-go-go 相关基因 (hERG) 通道没有显著抑制 (IC50 > 100 μM)[1]。

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

Enpp-1-IN-27 相关抗体:

ELISA Assay[1]

Cell Line: THP-1 cells and HFF cells
Concentration: 25 and 50 μM
Incubation Time: Pretreat for 1 h and treated with 5 μM of cGAMP for 24 h
Result: Significantly increased extracellular cytokine secretion compared to cGAMP treatment alone and demonstrated stronger innate immune activation than MV-658 in both THP-1 cells and HFF cells.

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 25 and 50 μM
Incubation Time: Pretreat for 1 h and treated with 5 μM of cGAMP for 6 h
Result: Enhanced the phosphorylation of STING, TBK1, and IRF3, indicating robust activation of the STING signaling cascade.

RT-PCR[1]

Cell Line: THP-1 cells
Concentration: 25 and 50 μM
Incubation Time: Pretreat for 1 h and treated with 5 μM of cGAMP for 3 h
Result: Increased the expression levels of representative interferon-stimulated genes (ISGs), including IFNB, ISG15 and IFIT3.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. T1/2 0.50 h
Mice 10 mg/kg p.o. T1/2 1.20 h
Mice 1 mg/kg i.v. Tmax 0.08 h
Mice 10 mg/kg p.o. Tmax 1.17 h
Mice 1 mg/kg i.v. Cmax 424.56 ng/mL
Mice 10 mg/kg p.o. Cmax 164.53 ng/mL
Mice 1 mg/kg i.v. AUClast 220.36 ng·h/mL
Mice 10 mg/kg p.o. AUClast 527.27 ng·h/mL
Mice 1 mg/kg i.v. AUCINF_obs 225.36 ng·h/mL
Mice 10 mg/kg p.o. AUCINF_obs 534.10 ng·h/mL
Mice 1 mg/kg i.v. MRTlast 0.45 h
Mice 10 mg/kg p.o. MRTlast 2.11 h
Mice 1 mg/kg i.v. MRTINF_obs 0.52 h
Mice 10 mg/kg p.o. MRTINF_obs 2.21 h
Mice 1 mg/kg i.v. Vss 2287.18 mL/kg
Mice 10 mg/kg p.o. F 23.93 %
Mice 1 mg/kg i.v. CL 75.61 mL/min/kg
体内研究
(In Vivo)

Enpp-1-IN-27(Compound 31) (50 mg/kg，腹腔注射，每日一次，连续 15-20 天) 在 4T1 和 CT26 同基因小鼠模型中显示出理想的抗肿瘤功效，且未观察到明显的毒性或副作用[1]。
Enpp-1-IN-27 (50 mg/kg，腹腔注射，单剂量) 具有高安全性，其肝毒性关键生物标志物 (包括天冬氨酸转氨酶 (AST) 和丙氨酸转氨酶 (ALT)) 以及肾毒性标志物 (例如血尿素氮 (BUN) 和血清肌酐) 均保持在正常范围内[1]。

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

Animal Model: 4T1 induced xenograft model established in female BALB/c mice (8 weeks old) [1]
Dosage: 50 mg/kg with or without anti-CTLA-4 antibodies (αCTLA-4)
Administration: Intraperitoneal injection (i.p.), once daily for 15 days
Result: Significantly inhibited tumor growth (47%) and the combination-treated group worked better (92%).
No significant toxicity was observed during the administration period, as indicated by stable body weight and the absence ofhair loss.
Animal Model: CT26 induced xenograft model established in female BALB/c mice (8 weeks old) [1]
Dosage: 50 mg/kg with or without anti-PD-L1
Administration: Intraperitoneal injection (i.p.), once daily for 20 days
Result: Showed significantly stronger anticancer effects in the combination therapy with PD-L1 blockade than ICIs monotherapy.
No significant toxicity was observed during the administration period, as indicated by stable body weight and the absence ofhair loss.
Promoted T cell-mediated immune activation and facilitates the conversion of cold tumor into hot tumor.
Significantly increased CD80 expression (M1 marker) and decreased CD206 levels (M2 marker).
Enhanced infiltration ofDiD-labeled PBMCs into tumor spheroids, as visualized by fluorescence imaging.
分子量

374.85

Formula

C13H19ClN6O3S
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

Enpp-1-IN-27 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:

Enpp-1-IN-27Phosphodiesterase (PDE)STINGStimulator of Interferon GenesTMEM173MITAERISMPYS4T1 cellsCT26 cellsTHP-1 cellsHCT116 cellsxenograft mice modelsInhibitorinhibitorinhibit

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目录号：
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