1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. Deubiquitinase Aldehyde Dehydrogenase (ALDH)
  3. MT16-001

MT16-001 是一种细胞渗透性的 UCHL1 抑制剂,其 IC50 值为 580 nM。MT16-001 对 USP30 也有相当的抑制活性,且对其他 UCH 家族去泛素化酶 (DUB) 及更广范围的蛋白质组具有选择性。MT16-001 可与 UCHL1 活性位点的半胱氨酸共价结合,在完整细胞中与 ALDH2ALDH9A1GATD3A 发生共价结合,同时作为一种细胞毒剂在人胚肾细胞中呈现陡直的剂量反应曲线。MT16-001 可用于多种癌症、肝纤维化和肺纤维化的研究。

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MT16-001

MT16-001 Chemical Structure

CAS No. : 1895049-73-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MT16-001 is a cell-permeable UCHL1 inhibitor with an IC50 value of 580 nM. MT16-001 also exhibits considerable inhibitory activity against USP30, and shows selectivity for other UCH family deubiquitinases (DUBs) as well as the broader proteome. MT16-001 binds covalently to the cysteine residue at the active site of UCHL1, and forms covalent interactions with ALDH2, ALDH9A1 and GATD3A in intact cells. Meanwhile, as a cytotoxic agent, it displays a steep dose-response curve in human embryonic kidney cells. MT16-001 can be used for research on various cancers, liver fibrosis and pulmonary fibrosis[1].

IC50 & Target[1]

USP30

 

ALDH2

 

体外研究
(In Vitro)

MT16-001 (30 min) 可强效抑制重组 UCHL1 (IC50 = 580 nM),且在 1 μM 浓度下抑制 USP30,但在高达 10 μM 的浓度下对重组 UCHL3 无抑制作用[1]
MT16-001 (72 h) 对 HEK293 细胞表现出细胞毒性,EC50 为 730 nM[1]
MT16-001 (1 h) 可与稳定表达 FLAG-UCHL1 的完整 Cal51 细胞中的 UCHL1 结合,其 IC50 为 550 nM[1]
MT16-001 (2-2000 nM; 3 h) 在浓度高达 2000 nM 时不会对 HEK293 细胞的整个蛋白质组造成急性破坏[1]

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

分子量

298.36

Formula

C15H14N4OS

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
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  • 稀释计算器

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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.

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MT16-001
目录号:
HY-182636
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