1. PROTAC MAPK/ERK Pathway Stem Cell/Wnt
  2. PROTACs MEK ERK
  3. PROTAC MEK1 Degrader-1

PROTAC MEK1 Degrader-1 是靶向 MEK1PROTAC,其 pIC50 值为 7.0。PROTAC MEK1 Degrader-1 由 MEK1 抑制剂 和 von Hippel-Lindau 配体组成。PROTAC MEK1 Degrader-1 抑制 ERK1/2 的磷酸化。PROTAC MEK1 Degrader-1 对 A375 细胞具有抗增殖活性。

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PROTAC MEK1 Degrader-1 Chemical Structure

PROTAC MEK1 Degrader-1 Chemical Structure

CAS No. : 2671004-41-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells[1].

体外研究
(In Vitro)

PROTAC MEK1 Degrader-1 (Compound 3) (10 μM-100 pM; 12 h) 在 1 μM 和 10 μM 两个最高浓度下发生降解,而较低浓度则导致 MEK1 和 ERK1/2 表达增加[1]。 PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 12 h) 显著抑制 IL6 等细胞因子的分泌[1]。 PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 0-72 h) 对 A375 细胞具有抗增殖活性[1]。 PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 0-20 h) 可在 5 h 后显著降解 MEK 和 ERK1/2,8 h 后完全抑制[1]

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

Cell Proliferation Assay[1]

Cell Line: A375 cells
Concentration: 10 μM
Incubation Time: 0 h, 20 h, 40 h, 60 h, 80h
Result: Had a strong inhibitory effect on cell growth

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 10 μM
Incubation Time: 16 h
Result: It degraded MEK and inhibited phosphorylation of ERK1/2.
分子量

1201.17

Formula

C53H66FIN8O11S2

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

PROTAC MEK1 Degrader-1 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (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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PROTAC MEK1 Degrader-1
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