2. Metabolic Enzyme/Protease
  3. Glycosidase
  4. JZ-4109

JZ-4109 是一种 β-葡糖脑苷脂酶 (GCase) 调节剂，对野生型重组 GCase 的 IC50 为 8 nM。JZ-4109 结合于 GCase 二聚体界面的变构位点，可稳定野生型及 GCaseN370S 突变体 GCase，诱导 GCase 发生二聚化。JZ-4109 可提升 GCase 蛋白丰度。JZ-4109 可用于帕金森病的相关研究。

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JZ-4109

JZ-4109 Chemical Structure

CAS No. : 1997359-63-3

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JZ-4109 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

JZ-4109 is a β-Glucocerebrosidase (GCase) modulator with an IC50 of 8 nM for wild-type recombinant GCase. JZ-4109 binds to an allosteric site at the GCase dimer interface, stabilizes wild-type and GCaseN370S mutant GCase, induces GCase dimerization. JZ-4109 increases GCase protein abundance. JZ-4109 can be used for the research of Parkinson's diseas[1].

体外研究
(In Vitro)

JZ-4109 (Compound 3) (0.76 nM-1.56 μM;30 min) 可通过线性混合型抑制作用强效抑制野生型重组 GCase，其 IC50 为 8 nM[1]。
JZ-4109 (0.25-100 μM; heated from 20 °C to 95 °C at 0.1 °C/s) 可稳定野生型重组 GCase 以对抗热变性[1]。
JZ-4109 (0.2-2 μM; 3 days) 可显著提高健康对照人成纤维细胞中 GCase 蛋白丰度与酶活性，且不会改变 GBA mRNA 水平[1]。
JZ-4109 (2 μM; 3 days) 可促进健康对照人类成纤维细胞中 GCase 的成熟与转运至内质网后区室，且不会增加滞留在内质网中的 GCase[1]。
JZ-4109 (2 μM; 3 days) 可显著提高 HEK 细胞溶酶体组分中 GCase 的丰度与酶活性[1]。
JZ-4109 (0.2-2 μM; 3 days) 可显著提高 1 型戈谢病供体的纯合 GBAN370S 突变人成纤维细胞中，内质网后成熟型 GCase 蛋白的丰度与酶活性[1]。
JZ-4109 (4.12-33.0 μM, co-incubated with 16.5 μM GCase) 可在溶液中诱导野生型 GCase 呈剂量依赖性二聚化[1]。

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

JZ-4109 相关抗体:

Western Blot Analysis[1]

Cell Line: Healthy control human fibroblast cells
Concentration: 0.2 μM; 2 μM
Incubation Time: 3 days
Result: Significantly increased GCase protein abundance relative to DMSO control at 0.2 μM.
Produced a greater significant increase in GCase protein abundance relative to DMSO control at 2 μM.
Significantly increased GCase enzyme activity relative to DMSO control at both 0.2 μM and 2 μM.

Western Blot Analysis[1]

Cell Line: HEK cells
Concentration: 2 μM
Incubation Time: 3 days
Result: Significantly increased GCase levels and enzyme activity in lysosomal enrichment fractions relative to DMSO control.
Showed a significant increase in GCase relative to lysosome marker Lamp1 relative to DMSO control.

Western Blot Analysis[1]

Cell Line: Homozygous N370S mutant human fibroblast cells (type-1 Gaucher’s disease patient)
Concentration: 0.2 μM; 2 μM
Incubation Time: 3 days
Result: Significantly increased GCase protein abundance and enzyme activity relative to DMSO control at 0.2 μM.
Produced a greater significant increase in GCase protein abundance and enzyme activity relative to DMSO control at 2 μM.
Localized the increase in GCase signal to post-ER mature GCase.
分子量

338.41

Formula

C22H18N4
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

JZ-4109 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)

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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:

JZ-41091997359-63-3JZ4109JZ 4109GlycosidaseHEK cellsN370S mutant GCaseER stressβ-GlucocerebrosidaseGCaselysosomesGBA mRNAfibroblast cellsParkinson's diseaseGaucher’s diseaseInhibitorinhibitorinhibit

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