2. Membrane Transporter/Ion Channel Stem Cell/Wnt Apoptosis
  3. Na+/H+ Exchanger (NHE) Wnt Apoptosis
  4. FJ9

FJ9 是一种 NHERF1/PDZ 抑制剂，针对人源 NHERF1 PDZ1 的 IC50 为 1540 μM，针对 NHERF1 PDZ2 的 IC50 为 160 μM，针对 Frizzled-7-Dishevelled PDZ 复合物的 Ki 为 10 μM。FJ9 结合 NHERF1 PDZ 结构域的配体结合口袋，从而阻断同源配体的相互作用，破坏 Frizzled-7 与 Dishevelled 的相互作用，并下调经典 Wnt 信号通路。FJ9 可诱导具有完整 β-连环蛋白信号通路的癌细胞发生凋亡 (apoptosis)。FJ9 可用于非小细胞肺癌、黑色素瘤的相关研究。

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FJ9

FJ9 Chemical Structure

CAS No. : 873841-43-1

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FJ9 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

FJ9 is a NHERF1/PDZ inhibitor with human NHERF1 PDZ1 IC50 1540 μM, NHERF1 PDZ2 IC50 160 μM, and Frizzled-7-Dishevelled PDZ complex Ki 10 μM. FJ9 binds ligand-binding pockets of NHERF1 PDZ domains to block cognate ligand interactions, disrupts Frizzled-7-Dishevelled interactions, and down-regulates canonical Wnt signaling. FJ9 induces apoptosis in cancer cells with intact β-catenin signaling. FJ9 can be used for the research of non-small cell lung cancer, melanoma[1][2].

体外研究
(In Vitro)

FJ9 (Compound 1) 可抑制 GST 融合人源 NHERF1 PDZ1 结构域与生物素化 β2AR 羧基末端肽之间的相互作用，其 IC50 为 1540 μM[1]。
FJ9 可抑制 GST 融合的人源 NHERF1 PDZ2 结构域与生物素化 CFTR 羧基末端肽之间的相互作用，其 IC50 为 160 μM[1]。
FJ9 (0.1-1000 μM) 可竞争性抑制 Frz7 肽与纯化的人源 DVL1 PDZ 结构域的结合，其 Ki 值为 63 μM；同时可竞争性抑制 Frz7 肽与纯化的人源 DVL3 PDZ 结构域的结合，其 Ki 值为 29 μM[2]。
FJ9 (100-300 μM；24 小时) 可穿透 HEK293T 细胞，并在 100 μM 和 300 μM 浓度下破坏 HA 标签化小鼠 DVL1 与 myc 标签化人类 Frz7 之间的细胞内相互作用[2]。
FJ9 (100-300 μM；48 小时) 可呈剂量依赖性下调稳定表达全长小鼠 DVL1 的 hTERT 永生化 LP9 间皮细胞中的胞质 β-catenin 水平，但对对照 LP9 细胞或表达 PDZ 结构域缺失型小鼠 DVL1 的 LP9 细胞无此作用[2]。
FJ9 (100-300 μM；24 小时) 可剂量依赖性地抑制 HCT116 p53-/- 结肠癌细胞中组成型 Tcf 转录活性并可降低 TOPflash 报告基因的活性，而对 FOPflash 报告基因的活性影响极小[2]。
FJ9 (30-100 μM；1-2 天) 可下调 HCT116 p53-/- 结肠癌细胞中经典 Wnt 信号通路的靶蛋白 (cyclin D1、c-myc、survivin) 及 mRNA (cyclin D1、survivin)，并下调 NCI-H1703 非小细胞肺癌细胞中的 survivin 蛋白[2]。
FJ9 (30-100 μM；24 小时) 在 30 μM 和 100 μM 浓度下处理 24 小时后，不会影响转染 mDVL1 的 HeLa 细胞中 JNK 的激活[2]。
FJ9 (86-100 μM；3-6 天) 在 86~100 μM 浓度处理 3~6 天后，可在 LOX 黑色素瘤细胞、NCI-H460 非小细胞肺癌细胞和 NCI-H1703 非小细胞肺癌细胞中诱导显著凋亡，但对 NCI-H28 间皮瘤细胞以及正常 NHBE 和 SAEC 细胞无凋亡作用[2]。

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

FJ9 相关抗体:

Western Blot Analysis[2]

Cell Line: HEK293T cells transiently expressing HA-tagged mouse DVL1 and myc-tagged human Frz7
Concentration: 100 μM; 300 μM
Incubation Time: 24 h
Result: Diminished the formation of the intracellular DVL1-Frz7 complex at concentrations above the in vitro Ki value, as shown by reduced detection of myc-tagged Frz7 in anti-HA immunoprecipitates.
Left whole lysate myc-hFrz7 levels consistent.

Western Blot Analysis[2]

Cell Line: hTERT-immortalized LP9 mesothelial cells stably expressing empty vector, full-length mouse DVL1, or PDZ domain-deleted mouse DVL1 (ΔPDZ-DVL1)
Concentration: 100 μM; 300 μM
Incubation Time: 48 hours
Result: Causes a dose-dependent down-regulation of cytosolic β-catenin exclusively in LP9 cells stably expressing full-length DVL1.
Causes no significant change in cytosolic β-catenin levels in control empty vector-expressing cells or ΔPDZ-DVL1-expressing cells.
Causes no significant cell death or morphologic changes in any cell line.

Western Blot Analysis[2]

Cell Line: HCT116 p53-/- colon cancer cells; NCI-H1703 non-small cell lung cancer cells
Concentration: 30 μM; 100 μM
Incubation Time: 2 days
Result: Down-regulated canonical Wnt signaling target proteins (cyclin D1, c-myc, survivin) in HCT116 p53-/- colon cancer cells, and down-regulated survivin protein in NCI-H1703 non-small cell lung cancer cells

Real Time qPCR[2]

Cell Line: HCT116 p53-/- colon cancer cells; NCI-H1703 non-small cell lung cancer cells
Concentration: 30 μM; 100 μM
Incubation Time: 1 day
Result: Down-regulated cyclin D1 and survivin in HCT116 p53-/- colon cancer cells.

Western Blot Analysis[2]

Cell Line: HeLa cells transiently transfected with mouse DVL1
Concentration: 30 μM; 100 μM
Incubation Time: 24 hours
Result: Has no effect on the dual phosphorylation (activation) of JNK in mDVL1-transfected HeLa cells, indicating no impact on non-canonical Wnt signaling mediated by JNK.

Apoptosis Analysis[2]

Cell Line: LOX melanoma cells, NCI-H460 non-small cell lung cancer cells, NCI-H1703 non-small cell lung cancer cells, NCI-H28 mesothelioma cells, normal human bronchial epithelial (NHBE) cells, normal human small airway epithelial (SAEC) cells
Concentration: 86 μM; 100 μM
Incubation Time: 3 days; 4 days
Result: Induces significant apoptosis in LOX, H460, and H1703 tumor cells with intact β-catenin signaling.
Neither suppresses growth nor induces apoptosis in H28 mesothelioma cells with a homozygous β-catenin gene deletion.
Has minimal effect on normal NHBE and SAEC cells which do not express Wnt-1.
体内研究
(In Vivo)

FJ9 (50 mg/kg；腹腔注射；每日一次；连续 14 天) 可显著抑制裸鼠体内 H460 非小细胞肺癌异种移植物的生长，且未导致显著的体重下降[2]。

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

Animal Model: NSWNU-M (6-week-old female, injected s.c. with 4 million H460 tumor cells)[2]
Dosage: 50 mg/kg
Administration: i.p.; daily; 14 days
Result: Significantly inhibited growth of H460 tumor xenografts.
Reduced mean tumor volume to ~300 mm3 on day 12 (vs ~400 mm3 for vehicle control).
Reduced mean tumor volume to ~275 mm3 on day 14 (vs ~475 mm3 for vehicle control).
Reduced mean tumor volume to ~325 mm3 on day 16 (vs ~700 mm3 for vehicle control).
Caused no significant mouse weight loss (<5%).
分子量

365.47

Formula

C23H27NO3
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

FJ9 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

FJ9873841-43-1FJ 9FJ-9Na+/H+ Exchanger (NHE)WntApoptosisSodium/hydrogen ExchangerSodium-hydrogen ExchangerFrizzled-7-Dishevelled PDZ complexhuman NHERF1 PDZ1mouse xenograft modelshuman NHERF1 PDZ2canonical Wnt signalingmelanomanon-small cell lung cancerHCT116 p53-/- colon cancer cellsapoptosisHEK293T cellsInhibitorinhibitorinhibit

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