2. Cytoskeleton Metabolic Enzyme/Protease Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. Exosomes MAGL Interleukin Related VEGFR
  4. AM9928

AM9928 是一种单酰基甘油脂肪酶 (MAGL) 抑制剂，其 IC50 和 Ki 值分别为 8.9 和 7.3 nM。AM9928 可阻断三阴性乳腺癌 (TNBC) 细胞的黏附和迁移，抑制 TNBC 分泌 IL-6、IL-8 和 VEGF-A。AM9928 可抑制 TNBC 来源外泌体诱导的人脑微血管内皮细胞 (HBMECs) 激活，减少 HBMECs 分泌 IL-8 和 VEGF-A。AM9928 可减轻血脑屏障通透性变化，抑制乳腺脂肪垫肿瘤生长，并减少 TNBC 的脑定植。AM9928 可用于三阴性乳腺癌的相关研究。

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AM9928

AM9928 Chemical Structure

CAS No. : 1869033-49-7

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AM9928 相关抗体

Top Publications Citing Use of Products

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AM9928 is a monoacylglycerol lipase (MAGL) inhibitor with IC50 and Ki values of 8.9 nM and 7.3 nM, respectively. AM9928 blocks the adhesion and migration of triple-negative breast cancer (TNBC) cells, and inhibits the secretion of IL-6, IL-8 and VEGF-A by TNBC cells. AM9928 suppresses the activation of human brain microvascular endothelial cells (HBMECs) induced by TNBC-derived exosomes, and reduces the secretion of IL-8 and VEGF-A by HBMECs. AM9928 attenuates changes in blood-brain barrier permeability, inhibits tumor growth in the mammary fat pad, and reduces brain colonization of TNBC. AM9928 can be used in studies related to triple-negative breast cancer[1][2][3].

IC50 & Target[1]

IL-6

 

IL-8

 

体外研究
(In Vitro)

AM9928 (100 ng/mL; 10-30 min) 可在 10 分钟和 30 分钟时阻断 MDA-MB-BrM2 三阴性乳腺癌 (TNBC) 细胞与 HBMEC 单层细胞的黏附[1]。
AM9928 (100 ng/mL; 5 h) 可显著抑制 MDA-MB-231 和 MDA-MB-BrM2 三阴性乳腺癌 (TNBC) 细胞穿过人脑微血管内皮细胞 (HBMEC) 单层的迁移能力[1]。
AM9928 (250 nM; 72 h) 可显著抑制 MDA-MB-231 和 MDA-MB-BrM2 三阴性乳腺癌 (TNBC) 细胞分泌 IL-6、IL-8 和 VEGF-A[1]。
AM9928 (250 nM; 24 h) 可改变 MDA-MB-231 和 MDA-MB-BrM2 三阴性乳腺癌 (TNBC) 细胞的外泌体生成，所产生的外泌体可显著抑制活化人脑微血管内皮细胞 (HBMECs) 分泌 IL-8 和 VEGF-A[1]。
AM9928 可抑制截短型大鼠脂肪酸酰胺水解酶 (ΔTM rFAAH)，其 IC50 值为 23 nM 和 27 nM[3]。

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

AM9928 相关抗体:

Cell Migration Assay [1]

Cell Line: MDA-MB-231, MDA-MB-BrM2 (human TNBC cell lines)
Concentration: 100 ng/mL
Incubation Time: 5 h
Result: Significantly inhibited transmigration of MDA-MB-231 and MDA-MB-BrM2 TNBC cells across HBMEC monolayers by approximately 50%.

ELISA Assay[1]

Cell Line: MDA-MB-231, MDA-MB-BrM2 (human TNBC cell lines)
Concentration: 250 nM
Incubation Time: 72 h
Result: Reduced IL-6, IL-8 and VEGF-A secretion.

ELISA Assay[1]

Cell Line: MDA-MB-231, MDA-MB-BrM2 (human TNBC cell lines), human brain microvascular endothelial cells (HBMECs)
Concentration: 250 nM (TNBC cell treatment)
Incubation Time: 24 h (TNBC cell treatment); 6 h (exosome-HBMEC incubation)
Result: Reduced HBMEC IL-8 and VEGF-A secretion.
体内研究
(In Vivo)

AM9928 (10 mg/kg；静脉注射；每周 2 次；持续 3 周) 可显著抑制 BALB/c 小鼠乳腺脂肪垫中三阴性乳腺癌的肿瘤生长，降低血脑屏障 (BBB) 通透性，并减少脑转移定植[1]。

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

Animal Model: BALB/c (female, 6 weeks old, triple negative breast cancer model via GFP-4T1-BrM5 mammary tumor cell injection into mammary fat pads)[1]
Dosage: 10 mg/kg
Administration: i.v.; twice weekly; 3 weeks
Result: Significantly reduced mammary fat pad tumor growth compared to vehicle controls.
Significantly lowered average sum of GFP intensity (measure of brain tumor colonization) compared to vehicle controls.
Significantly decreased BBB permeability (measured by Evans blue dye content in brain tissue) compared to tumor-bearing vehicle controls.
Increased average sum of intensity for ZO-1 tight junction protein expression to 610,920 (vs. 582,096 in vehicle controls).
Increased average sum of intensity for Claudin-5 expression to 681,457 (vs. 518,599 in vehicle controls).
Reduced the number of mice with mammary tumors and brain tumors compared to vehicle controls.
Increased the number of mice alive at day 28 compared to vehicle controls.
分子量

396.44

Formula

C24H20N4O2
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

AM9928 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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:

AM99281869033-49-7AM 9928AM-9928ExosomesMAGLInterleukin RelatedVEGFRMonoacylglycerol lipaseILVascular endothelial growth factor receptortriple negative breast cancermonoacylglycerol lipaseMDA-MB-BrM2IL-6TNBCHBMECsIL-8VEGF-Ahuman MAGLMDA-MB-231Inhibitorinhibitorinhibit

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