TBC1D2-IN-1
TBC1D2-IN-1 is a potent orally active and selective TBC1D2 inhibitor with a Kd of 1.1 μM. TBC1D2-IN-1 selectively inhibits TBC1D2-mediated GTP hydrolysis on RAB7A-GTP, promotes RAB7A accumulation on lysosomal membranes, and induces apoptosis and autophagy. TBC1D2-IN-1 exerts selective antiproliferative activity cancer cells. TBC1D2-IN-1 can be used for the research of cervical carcinoma.
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- Formule: C34H35F3N2O3
- Masse moléculaire:576.65
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
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Caspase-3 |
Bax |
Bcl-2 |
TBC1D2-IN-1 (compound A1) (0.1-20 μM) binds selectively to the PH domain of TBC1D2, showing weaker binding to Top 1 and no binding to Hsp90[1].
TBC1D2-IN-1 (2 days) potently and selectively inhibits proliferation of HeLa cells with an IC50 of 0.43 μM and inhibits proliferation of A549, HepG2, and BEAS-2B cells with IC50 values of 0.56, 0.79, and 1.5 μM, respectively[1].
TBC1D2-IN-1 (0.5-1.5 μM; 24 h) induces dose-dependent accumulation of RAB7A on the lysosomal membrane of HeLa cells[1].
TBC1D2-IN-1 (0.5-2 μM; 48 h) induces concentration-dependent upregulation of RAB7A protein levels in HeLa cells[1].
TBC1D2-IN-1 (0.5-2 μM; 48 h) induces concentration-dependent decreases in TBC1D2 and VEGFR2 protein levels in HeLa cells after 48 h of treatment, with no significant effects on Top 1 or Hsp90 levels[1].
TBC1D2-IN-1 (0.5-2.5 μM; 24 h) induces potent autophagy in HeLa cells[1].
TBC1D2-IN-1 (0.1-10 μM; 1 h) induces a biphasic change in TBC1D2 protein levels in HeLa cells[1].
TBC1D2-IN-1 (0.5-2.5 μM; 24 h) induces a triphasic apoptotic response in HeLa cells[1].
TBC1D2-IN-1 (0.5-2.5 μM; 24 h) induces a non-monotonic change in the G2/M phase fraction of HeLa cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0.5; 1.5 μM
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Incubation Time:24 h
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Result:Induced dose-dependent accumulation of RAB7A on the lysosomal membrane, visible as distinct punctate staining in treated cells compared to the diffuse cytoplasmic staining in control cells.
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Cell Line:HeLa cells
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Concentration:0.5; 1; 1.5; 2 μM
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Incubation Time:48 h
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Result:Induced a concentration-dependent increase in RAB7A protein levels.
Caused a statistically significant 2.2-fold increase in RAB7A protein levels at 2 μM compared to control.\n
Induced a concentration-dependent decrease in TBC1D2 and VEGFR2 protein levels.
Caused no significant changes in Top 1 or Hsp90 protein levels.\n
Induced dynamic changes in apoptotic regulators: p53 levels showed a modest initial increase followed by a decrease, caspase-3 and Bcl-2 levels progressively declined, and Bax levels initially decreased then markedly increased at 2 μM.
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Cell Line:HeLa cells
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Concentration:0.5; 1; 1.5; 2; 2.5 μM
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Incubation Time:24 h
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Result:Induced a biphasic response in lysosomal fluorescence intensity: fluorescence increased in a concentration-dependent manner up to 1.5 μM, with a 40-fold increase relative to control, then decreased at 2.5 μM due to lysosomal impairment from apoptosis.
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Cell Line:HeLa cells
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Concentration:0.1; 0.5; 1; 3; 10 μM
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Incubation Time:1 h
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Result:Induced a biphasic change in TBC1D2 fluorescence intensity within 1 h: levels decreased at 0.1 μM, rebounded to a 1.6-fold increase at 1 μM, then decreased again at 10 μM compared to control.
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Cell Line:HeLa cells
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Concentration:0.5; 1; 1.5; 2; 2.5 μM
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Incubation Time:24 h
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Result:Induced a triphasic apoptotic response: the percentage of apoptotic cells increased from 4% (control) to 26% at 1.5 μM, decreased to 16% at 2 μM, then sharply rose to 94% at 2.5 μM.
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Cell Line:HeLa cells
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Concentration:0.5; 1; 1.5; 2; 2.5 μM
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Incubation Time:24 h
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Result:Induced a non-monotonic change in the G2/M phase fraction: the proportion increased from 11% (control) to 34% at 0.5 μM, decreased to 4% at 1 μM, then gradually rose to 54% at 2.5 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude subcutaneously injected with HeLa cells[1]
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Dosage:40 mg/kg
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Administration:p.o.; every other day; 28 days
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Result:Achieved a 49% tumor growth inhibition rate.
Induced extensive areas of tumor necrosis via H&E staining.
Exhibited no significant body weight loss relative to controls.
Caused only mild, gefitinib-comparable histopathological alterations in major organs, including mild capillary wall thickening in lungs and occasional tubular swelling and edema in kidneys.
Chemical Information
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Masse moléculaire 576.65
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Formule C34H35F3N2O3
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SMILES
O=C1N(C[C@@]2([H])[C@@]3([H])[C@]4([H])CCCN3CCC2)[C@]4([H])CC/C1=C\C5=CC(C=CC(OCC6=CC=C(OC(F)(F)F)C=C6)=C7)=C7C=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TBC1D2-IN-1 Related Classifications
HY-183772 Related Classifications
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