2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. FRC-222

FRC-222 是一种 CHD1 抑制剂，其 Kd 值为 0.15 μM，IC50 值为 0.49 μM。FRC-222 通过芳香笼相互作用和延伸配体接触结合到 CHD1 串联染色质结构域的 H3K4me3 结合位点。FRC-222 可用于前列腺癌的研究。

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FRC-222

FRC-222 Chemical Structure

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FRC-222 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FRC-222 is a CHD1 tandem chromodomain inhibitor with a Kd of 0.15 μM and an IC50 of 0.18 μM. FRC-222 binds to the H3K4me3 binding site of CHD1 tandem chromodomain via aromatic cage interactions and extended ligand contacts. FRC-222 can be used for the research of prostate cancer[1].

体外研究
(In Vitro)

FRC-222 (Compound 2n) 以 0.15 μM 的 Kd 值与纯化的重组 CHD1 串联染色质结构域结合[1]。
FRC-222 可抑制纯化重组 CHD1 串联染色质结构域与 H3K4me3 肽段的相互作用，其 IC50 为 0.49 μM[1]。
FRC-222 (25-100 μM) 可结合 HEK293T 细胞裂解液中的内源性全长 CHD1，并以浓度依赖的方式竞争性抑制其与 LSD1-K114me3 肽的结合[1]。
FRC-222 (10 μM) 对纯化的 LSD1、KMT9、METTL21A、EHMT2 (G9a)、SET8 和 NSD2 酶表现出高选择性，对 DNMT1 的抑制作用极低[1]。
FRC-222 (16 μM) 对纯化的 TAF3、SPIN1 和 PHF8 甲基化赖氨酸阅读器结构域表现出高选择性，对 H3K4me3 肽的结合无显著抑制作用[1]。
FRC-222 (0.8-6 μM；48 小时) 以浓度依赖的方式降低 PC-3M-Luc 前列腺癌细胞的活力，在浓度 ≥1.8 μM 时可观察到显著的抑制作用[1]。
FRC-222 (0.8-6 μM；48 小时) 可强效且呈浓度依赖性地降低 22Rv1 前列腺癌细胞的活力，在浓度 ≥1.8 μM 时可观察到显著的抑制作用[1]。

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

FRC-222 相关抗体:

Cell Viability Assay[1]

Cell Line: PC-3M-Luc prostate cancer cells
Concentration: 0.8 μM; 1.2 μM; 1.8 μM; 2.7 μM; 4 μM; 6 μM
Incubation Time: 48 h
Result: Retained over 110% of control cell viability at 0.8 μM and 1.2 μM.
Reduced viability to 60% of control at 1.8 μM.
Reduced viability to 35% of control at 2.7 μM.
Reduced viability to 25% of control at 4 μM.
Reduced viability to ~5% of control at 6 μM.

Cell Viability Assay[1]

Cell Line: 22Rv1 prostate cancer cells
Concentration: 0.8 μM; 1.2 μM; 1.8 μM; 2.7 μM; 4 μM; 6 μM
Incubation Time: 48 h
Result: Retained over 110% of control cell viability at 0.8 μM.
Retained ~90% of control viability at 1.2 μM.
Reduced viability to ~10% of control at 1.8 μM.
Reduced viability to ≤10% of control at concentrations ≥2.7 μM.
分子量

579.77

Formula

C36H45N5O2
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

FRC-222 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

FRC-222FRC222FRC 222DNA/RNA Synthesisprostate cancer22Rv1 prostate cancer cellsKMT9CHD1 tandem chromodomainPC-3M-Luc prostate cancer cellsHEK293T cell lysateMETTL21AEHMT2 (G9a)H3K4me3LSD1Inhibitorinhibitorinhibit

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产品名称：
FRC-222
目录号：
HY-183603
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