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

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.

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FJ9

FJ9 Chemical Structure

CAS No. : 873841-43-1

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Based on 1 publication(s) in Google Scholar

FJ9 Related Antibodies

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Description

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].

In Vitro

FJ9 (Compound 1) inhibits the interaction between GST-fused human NHERF1 PDZ1 domain and biotinylated β2AR carboxy-terminal peptide with an IC50 of 1540 μM[1].
FJ9 inhibits the interaction between GST-fused human NHERF1 PDZ2 domain and biotinylated CFTR carboxy-terminal peptide with an IC50 of 160 μM[1].
FJ9 (0.1-1000 μM) competitively inhibits Frz7 peptide binding to purified human DVL1 PDZ domain with a Ki of 63 μM and to purified human DVL3 PDZ domain with a Ki of 29 μM[2].
FJ9 (100-300 μM; 24 hours) penetrates HEK293T cells and disrupts the intracellular interaction between HA-tagged mouse DVL1 and myc-tagged human Frz7 at concentrations of 100 μM and 300 μM[2].
FJ9 (100-300 μM; 48 hours) dose-dependently down-regulates cytosolic β-catenin levels in hTERT-immortalized LP9 mesothelial cells stably expressing full-length mouse DVL1, but not in control LP9 cells or LP9 cells expressing PDZ domain-deleted mouse DVL1[2].
FJ9 (100-300 μM; 24 hours) dose-dependently inhibits constitutive Tcf transcriptional activity in HCT116 p53-/- colon cancer cells, reducing TOPflash reporter activity while minimally affecting FOPflash reporter activity[2].
FJ9 (30-100 μM; 1-2 days) down-regulates canonical Wnt signaling target proteins (cyclin D1, c-myc, survivin) and mRNA (cyclin D1, survivin) in HCT116 p53-/- colon cancer cells, and down-regulates survivin protein in NCI-H1703 non-small cell lung cancer cells[2].
FJ9 (30-100 μM; 24 hours) does not affect JNK activation in mDVL1-transfected HeLa cells after 24 hours of treatment at 30 μM and 100 μM[2].
FJ9 (86-100 μM; 3 to 6 days) induces significant apoptosis in LOX melanoma, NCI-H460 non-small cell lung cancer, and NCI-H1703 non-small cell lung cancer cells, but has no apoptotic effect on NCI-H28 mesothelioma cells or normal NHBE and SAEC cells, after 3 to 6 days of treatment at 86 to 100 μM[2].

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

FJ9 Related Antibodies

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.
In Vivo

FJ9 (50 mg/kg; i.p.; daily; 14 days) significantly inhibits H460 non-small cell lung cancer xenograft growth in nude mice without causing significant weight loss[2].

MedChemExpress (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%).
Molecular Weight

365.47

Formula

C23H27NO3
CAS No.
SMILES

O=C(C1=CC2=C(NC(C(CCCC)O)=C2CCC3=CC=CC=C3)C=C1C)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FJ9 Related Classifications

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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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