2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. GRI918013

GRI918013 (compound 1) 是选择性和竞争型的自分泌运动因子 (ATX/NPP2) 抑制剂，具有抗侵袭和抗转移活性。GRI918013 通过竞争性结合 ATX，阻断溶血磷脂酰胆碱 (LPC) 等脂质底物进入 ATX 活性位点，抑制 ATX 介导的 LPC 水解生成溶血磷脂酸 (LPA)，从而抑制 ATX-LPA 轴相关的肿瘤细胞侵袭和转移。GRI918013 抑制 ATX 介导的 LPL 底物 FS-3 水解 (IC50=31.42 nM、Ki=12.98 nM)。GRI918013 可用于黑色素瘤等癌症侵袭与转移的研究，也可作为纤维化疾病、神经性疼痛、胆汁淤积性瘙痒等 ATX-LPA 轴相关疾病的工具化合物。

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GRI918013

GRI918013 Chemical Structure

CAS No. : 313685-55-1

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GRI918013 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
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

GRI918013 (compound 1) is a selective and competitive autotaxin (ATX/NPP2) inhibitor with anti-invasive and anti-metastatic activity. GRI918013 competitively binds to ATX, blocking lipid substrates such as lysophosphatidylcholine (LPC) from entering the ATX active site, thereby inhibiting ATX-mediated hydrolysis of LPC to lysophosphatidic acid (LPA), and consequently inhibiting ATX-LPA axis-related tumor cell invasion and metastasis. GRI918013 inhibits ATX-mediated hydrolysis of the LPL substrate FS-3 (IC50=31.42 nM, Ki=12.98 nM). GRI918013 can be used in research on cancer invasion and metastasis, such as melanoma, and can also serve as a tool compound for ATX-LPA axis-related diseases such as fibrotic diseases, neuropathic pain, and cholestatic pruritus[1].

IC50 & Target

Autotaxin

 

体外研究
(In Vitro)

GRI918013 (10 µM；3 h) 可竞争性抑制 ATX 介导的 FS-3 水解 (IC50=31.42 nM；Ki=12.98 nM)，且不抑制磷酸二酯酶（PDE）底物 pNP-TMP 水解，对 NPP6、NPP7 及 LPA、S1P 受体无作用[1]。
GRI918013 (10 µM；2 h) 对 ATX 介导的 LPC 14:0、LPC 16:0、LPC 18:0、LPC 18:1 四种底物的水解抑制率分别为 41.0%、55.4%、43.6%、51.8%[1]。
GRI918013 可剂量依赖性抑制 ATX 依赖的 A2058 细胞侵袭 (IC50=118.79 nM，16 h) [1]。
GRI918013 对 ATXF275A 突变体的抑制活性降低 (IC50 >10 μM，而 ATX 野生型为 3.0 μM)，但对 ATXY83A 突变体仍保持活性 (IC50=0.15 μM) [1]。
GRI918013 (10 µM；4 h) 可抑制 ATX 介导的 ADMAN-LPC 水解，抑制率为 89.0%[1]。

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

GRI918013 相关抗体:

Cell Invasion Assay[1]

Cell Line: A2058 human melanoma cells
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 16 hours
Result: Dose-dependently inhibited ATX-dependent A2058 cell invasion with an IC50 of 118.79 nM.
体内研究
(In Vivo)

GRI918013 (30 µg/小鼠；腹腔注射；每日；10 天) 可减少携带 B16-F10 黑色素瘤的雌性 C57BL/6 小鼠的肺转移 [1]。

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

Animal Model: C57BL/6 mice (female, 8–12 weeks old)[1]
Dosage: 30 µg/mouse
Administration: i.p.; daily; 10 days
Result: Significantly reduced the number of lung metastatic nodules when administered 1 day before or 1 day after tumor cell inoculation compared to vehicle-treated controls.
分子量

433.28

Formula

C17H15Cl2FN2O4S
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

GRI918013 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:

GRI918013313685-55-1GRI 918013GRI-918013Phosphodiesterase (PDE)A2058 cellATXmicefemale C57BL/6 miceLPA receptorsADMAN-LPC hydrolysisB16-F10 melanomaY83A mutantNPP6sphingosine 1-phosphate receptorsFS-3 hydrolysisF275A ATX mutantcancer cellsNPP7melanomaAutotaxinInhibitorinhibitorinhibit

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产品名称：
GRI918013
目录号：
HY-119601
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