DVL1/P-gp-IN-1
DVL1/P-gp-IN-1 is a DVL1 inhibitor (lC50 of 0.97 μM) and a P-glycoprptein (P-gp) inhibitor. DVL1/P-gp-IN-1 specific binds to the PDZ domain of the DVL1 protein of the Wnt/β-catenin pathway and inhibition of the P-gp. DVL1/P-gp-IN-1 reduces β-catenin expression, suppresses colon cancer cells proliferation, and induces apoptosis both in vitro and in xenograft models. DVL1/P-gp-IN-1 can be used in colorectal cancer research.
For research use only. We do not sell to patients.
- Formula: C27H27ClN4O4S
- Molecular Weight:539.05
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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DVL1 0.97 μM (IC50) |
P-gp |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW-620 | IC50 |
14.21 μM
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Inhibits SW-620 cell growth for 72 hours.
Inhibits SW-620 cell growth for 72 hours.
|
42283820 |
| DLD-1 | IC50 |
15.69 μM
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Inhibits DLD-1 cells growth for 72 hours.
Inhibits DLD-1 cells growth for 72 hours.
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42283820 |
| HCT-116 | IC50 |
17.45 μM
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Inhibits HCT-116 cell growth for 72 hours.
Inhibits HCT-116 cell growth for 72 hours.
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42283820 |
| SW480 | IC50 |
16.4 μM
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Inhibits SW480 cells growth for 72 hours.
Inhibits SW480 cells growth for 72 hours.
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42283820 |
DVL1/P-gp-IN-1 (Compound (S,S)-15) (5-10 μM) exhibits concentration-dependent inhibition of the binding between DVL1 PDZ and the TMEM88 peptide[1].
DVL1/P-gp-IN-1 (1-500 μM; 72 h) inhibits the growth of SW620, SW480, HCT116, and DLD-1 colon cancer cells[1].
DVL1/P-gp-IN-1 (50 μM; 24 h) induces increased apoptosis in SW620, SW480, HCT116, and DLD-1 colon cancer cells[1].
DVL1/P-gp-IN-1 (23 μM, 24 h) suppresses mRNA expression and total protein levels of β-catenin in HCT116 cells[1].
DVL1/P-gp-IN-1 (0.1 nM-10 μM; 72 h) shows dose-dependent cytotoxicity that becomes significant at concentrations >1 μM in HT29 cells and with no significant differences in HT29/HT29/DX cells[1].
DVL1/P-gp-IN-1 (1-100 nM; 3 h) dose-dependently restores intracellular Doxorubicin (DOX) (HY-15142A) accumulation in resistant HT29/DX cells without affecting sensitive HT29 cells[1].
DVL1/P-gp-IN-1 (1-100 nM; 3 h) suppresses P-gp ATP hydrolysis activity in a dose-dependent fashion[1].
DVL1/P-gp-IN-1 (1-100 nM; 72 h) dose-dependently reverses DOX resistance in HT29/DX cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620, SW480, HCT116, and DLD-1 colon cancer cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Induced accumulation of histone-bound DNA fragments during apoptosis in all tested cell lines.
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Cell Line:HCT116 cells
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Concentration:23 μM
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Incubation Time:24 h
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Result:Reduced the expression of the CTNNB1 gene, which encodes the β-catenin protein.
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Cell Line:HCT116 cells
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Concentration:23 μM
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Incubation Time:24 h
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Result:Reduced total β-catenin protein levels in HCT116 cells.
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Cell Line:HT29 and HT29/DX cells
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Concentration:1 nM, 10 nM, 100 nM
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Incubation Time:72 h
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Result:Barely strengthened DOX cytotoxicity in sensitive HT29 cells except at 100 nM.
Reduced cell viability dose-dependently in resistant HT29/DX cells when combined with DOX.
Restored DOX chemosensitivity in HT29/DX cells.
DVL1/P-gp-IN-1 (DVL1/P-gp-IN-1 at 14 mg/kg and 5-FU at 12 mg/kg; i.p.; every 2 days; for 40 days) combined with 5-FU reduces tumor size and CTNNB1 mRNA expression, strongly represses β-catenin protein, and achieves more prominent suppression of Ki-67 proliferation marker in colorectal cancer tumor tissues of BALB/Cnu/nu mice, displaying superior antitumor efficacy relative to 5-FU monotherapy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:10-week-old male BALB/Cnu/nu nude mice received subcutaneous inoculation of HCT116 cell suspension (1 × 108 cells/mL)[1]
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Dosage:25 mg/kg
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Administration:i.p., every 2 days, for 40 days
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Result:Reduced tumor size and weight in mice compared to the control group.
Caused a more substantial reduction in mRNA expression versus 5-FU.
Reduced the expression of β-catenin at the protein level.
Markedly suppressed Ki-67 levels within tumor tissues.
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Animal Model:10-week-old male BALB/Cnu/nu nude mice received subcutaneous inoculation of HCT116 cell suspension (1 × 108 cells/mL)[1]
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Dosage:14 mg/kg combined with 5-FU at 12 mg/kg
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Administration:i.p., every 2 days, for 40 days
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Result:Reduced tumor size and weight in mice and exhibited a slightly superior efficacy over 5-FU administered as a single agent.
Paired with 5-FU inhibited CTNNB1 mRNA expression in tumor tissue.
Combined with 5-FU significantly reduced β-catenin protein levels.
Combined with 5-FU displayed stronger suppression of Ki-67 expression in tumor tissue.
Chemical Information
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Molecular Weight 539.05
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Formula C27H27ClN4O4S
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SMILES
O=C(C(N1)=C(S(=O)(C2=CC(C)=CC(C)=C2)=O)C3=C1C=CC(Cl)=C3)N[C@@H](C)C(N[C@H](C4=CC=NC=C4)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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