2. Immunology/Inflammation
  3. Kallikrein
  4. DKFZ-251

DKFZ-251 是一种激肽释放酶相关肽酶 KLK6 抑制剂 (IC50=0.47 μM)，对 KLK5 和 KLK7 也有一定抑制活性 (IC50 分别为 1.1 nM 和 73 nM)。DKFZ-251 可短暂酰化 KLK6 的催化性丝氨酸，形成能抑制酶功能的长寿命酰基-酶复合物。DKFZ-251 是一种表型调节剂，可改变细胞增殖能力并调控上皮间质转化 (EMT)。DKFZ-251 可用于头颈癌的相关研究。

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DKFZ-251

DKFZ-251 Chemical Structure

CAS No. : 2222059-70-1

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DKFZ-251 相关抗体

Top Publications Citing Use of Products

查看 Kallikrein 亚型特异性产品:

查看所有亚型
KLK1 KLK5 KLK8 KLK14 KLKB1 KLK10

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DKFZ-251 is a kininogenase-related peptidase KLK6 inhibitor (IC50 = 0.47 μM), and also exhibits certain inhibitory activity against KLK5 and KLK7 (IC50 values are 1.1 nM and 73 nM, respectively). DKFZ-251 transiently acylates the catalytic serine of KLK6 to form a long-lived acyl-enzyme complex that inhibits enzyme function. DKFZ-251 is a phenotypic modulator that alters cell proliferation capacity and regulates epithelial-mesenchymal transition (EMT). DKFZ-251 can be used in research related to head and neck cancer[1].

IC50 & Target

KLK5

1.1 nM (IC50)

体外研究
(In Vitro)

DKFZ-251 (compound 11) (200 μM; 1 h) 可与重组三重突变体 KLK6 形成长寿命的酰基-酶复合物，其半衰期为 6.43 h[1]。
DKFZ-251 (100-500 nM; 48 h) 可在 FaDu 细胞中诱导 BrdU 掺入呈剂量依赖性增加，并引发表型改变，这与内源性 KLK6 的靶向抑制作用一致[1]。
DKFZ-251 (2.5-10 μM; 30 min) 可特异性抑制基于活性的探针 DKFZ-633 对重组 KLK6 的标记[1]。

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

DKFZ-251 相关抗体:

Cell Proliferation Assay[1]

Cell Line: FaDu head and neck squamous cell carcinoma cells
Concentration: 100, 300, 500 nM
Incubation Time: 48 h (daily treatment)
Result: Increased BrdU-positive FaDu cells in a dose-dependent manner: ~45% (100 nM), ~50% (300 nM), ~60% (500 nM), compared to ~45% in vehicle control.
Induced a dose-dependent phenotypic change in FaDu cells, mimicking the effect of KLK6 shRNA silencing.
分子量

416.48

Formula

C24H24N4O3
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

DKFZ-251 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

DKFZ-2512222059-70-1DKFZ251DKFZ 251KallikreinKLKKallikrein-related peptidaseKLK6EMThead and neck cancerepithelial to mesenchymal transitioncatalytic serineacyl-enzyme complexFaDu cellskallikrein-related peptidaseskallikrein-related peptidase 6triple-mutant KLK6Inhibitorinhibitorinhibit

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产品名称：
DKFZ-251
目录号：
HY-124714
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