YM17
YM17 is an orally active TNIK inhibitor with an IC50 of 181.9 nM and a Kd of 1.18 μM. YM17 induces Apoptosis and cell cycle redistribution. YM17 inhibits tumor growth in hepatocellular carcinoma xenograft models. YM17 can be used for research on hepatocellular carcinoma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C31H34Cl2N4O3
- Peso molecular:581.53
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MHCC97H | IC50 |
1.16 μM
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Antiproliferative activity against human MHCC97H cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human MHCC97H cells assessed as viability reduction incubated 48 hrs by MTT assay.
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42636786 |
| Huh-7 | IC50 |
0.50 μM
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Antiproliferative activity against human HuH-7 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human HuH-7 cells assessed as viability reduction incubated 48 hrs by MTT assay.
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42636786 |
| HepG2 | IC50 |
0.64 μM
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Antiproliferative activity against human HepG2 cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human HepG2 cells assessed as viability reduction incubated 48 hrs by MTT assay.
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42636786 |
| THLE-2 | IC50 |
27.76 μM
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Cytotoxicity against human THLE-2 liver cells assessed as viability reduction incubated 48 hrs by MTT assay.
Cytotoxicity against human THLE-2 liver cells assessed as viability reduction incubated 48 hrs by MTT assay.
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42636786 |
In Vitro
YM17 (0.25-0.75 μM; 24-48 h) reduces wound closure in HuH-7 cells in a concentration-dependent manner[1].
YM17 (0.25-0.75 μM; 24 h) reduces migrated HuH-7 cells in a concentration-dependent manner after 24 h[1].
YM17 (0.25-0.75 μM) reduces clonogenic outgrowth of HuH-7 cells in a concentration-dependent manner[1].
YM17 (0.5-1.5 μM) decreases live-cell signals and increases dead-cell signals in HuH-7 3D tumor spheroids[1].
YM17 (0.25-0.75 μM; 24 h) reduces the p-TNIK/TNIK ratio and TNIK/β-catenin-associated pro-proliferative proteins while increasing Bax/Bcl-2, active caspase-3, and cleaved PARP1 in HuH-7 cells[1].
YM17 (0.078-5.00 μM) binds recombinant TNIK with a fitted KD value of 1.18 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MHCC97H, HuH-7, HepG2, and THLE-2 cells
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Concentration:Serially diluted YM17
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Incubation Time:48 h
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Result:Inhibited proliferation of MHCC97H, HuH-7, and HepG2 cells with IC50 values of 1.16, 0.50, and 0.64 μM, respectively.
Showed reduced cytotoxicity toward THLE-2 liver cells with an IC50 value of 27.76 μM.
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Cell Line:HuH-7 cells
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Concentration:0.25, 0.50, 0.75 μM YM17
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Incubation Time:24 h
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Result:Induced marked cell-cycle redistribution in HuH-7 cells, characterized by an increased G1-phase population and decreased S- and G2/M-phase populations.
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Cell Line:HuH-7 cells
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Concentration:0.50, 0.75, 1.00 μM YM17
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Incubation Time:24 h
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Result:Annexin V-FITC/PI staining showed that YM17 reduced the viable cell population and increased both early and late apoptotic populations in a concentration-dependent manner.
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Cell Line:HuH-7 cells
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Concentration:0.25, 0.50, 0.75 μM YM17
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Incubation Time:24 h
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Result:Had only a limited effect on total TNIK protein levels but markedly reduced the p-TNIK/TNIK ratio.
YM17 exposure decreased the levels of active β-catenin, MYC, and Cyclin B1.
Increased the Bax/Bcl-2 ratio, elevated active caspase-3, and increased cleaved PARP1 levels.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female)[1]
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Dosage:40 mg/kg
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Administration:p.o. (oral gavage); every other day; 28 days
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Result:Markedly delayed HuH-7 xenograft tumor progression.
At the study endpoint, the mean tumor weight in the YM17 group was 0.66 g, corresponding to a tumor growth inhibition (TGI) of 68.89%; the vehicle group mean tumor weight was 2.12 g.
No obvious body-weight loss was observed.
Immunohistochemical analysis showed increased cleaved caspase-3-positive staining and a reduced proportion of Ki-67-positive cells in YM17-treated tumors.
H&E staining showed decreased tumor cell density and more evident tissue damage/necrosis-like changes.
H&E staining of major organs showed no obvious structural damage.
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Liver Cancer Modeling
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Peso molecular 581.53
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Fòrmula C31H34Cl2N4O3
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SMILES
O=C(NC1=C2CC[C@]3([H])[C@@]4([H])CCCN5[C@@]4([H])[C@@](CCC5)([H])CN3C2=NC6=CC(OC)=C(OC)C=C16)C7=CC(Cl)=CC(Cl)=C7
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YM17 Related Classifications
HY-189665 Related Classifications
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