TBC1D2-IN-2
TBC1D2-IN-2 is an orally potent TBC1D2 inhibitor that binds to the TBC1D2 PH domain with a KD of 0.4 μM. TBC1D2-IN-2 induces autophagic cell death by reducing TBC1D2 protein levels, promoting RAB7A aggregation and enhancing autophagy. TBC1D2-IN-2 can be used in the research of hepatocellular carcinoma.
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- Formule: C38H46N4O2
- Masse moléculaire:590.80
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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
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
TBC1D2 0.4 μM (Kd) |
In Vitro
TBC1D2-IN-2 (1 μg/10 μL; 30 min) specifically binds to the PH domain of TBC1D2, competing with a TBC1D2 antibody for the same binding epitope[1].
TBC1D2-IN-2 (40 nM; 15 min) induces TBC1D2 degradation in HCCLM3 cells, including under starvation conditions that normally upregulate TBC1D2[1].
TBC1D2-IN-2 (0.5-32 μM; 2 days) inhibits HepG2 cell proliferation with an IC50 of 0.21 μM, as measured by 2-day MTT assay[1].
TBC1D2-IN-2 (80 nM; 8 days, medium renewed every 2 days) suppresses HCCLM3 cell colony formation by over 80%[1].
TBC1D2-IN-2 (40 nM; 48 h) induces autophagy in HCCLM3 cells, and maintains this autophagy-inducing effect even in the presence of chloroquine-mediated autophagy inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCCLM3 human hepatocellular carcinoma cells (full-nutrient and starvation conditions)
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Concentration:40 nM
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Incubation Time:15 min
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Result:Rapidly reduced TBC1D2 fluorescence intensity under both full-nutrient and starvation conditions.
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Cell Line:HCCLM3 human hepatocellular carcinoma cells
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Concentration:20-120 nM
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Incubation Time:48 h
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Result:Altered intracellular RAB7A distribution from diffuse staining to punctate aggregation foci in a concentration-dependent manner, indicating RAB7A accumulation.
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Cell Line:HCCLM3 human hepatocellular carcinoma cells (with and without chloroquine inhibition)
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Concentration:40 nM; 10 μM chloroquine (combination)
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Incubation Time:48 h
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Result:Increased Lyso-Tracker Red-positive autolysosomal signals both in the absence and presence of chloroquine, supporting enhanced autophagy.
In Vivo
G2 (TBC1D2-IN-2) (40 mg/kg; p.o.; single dose) shows pronounced hepatic retention and gradual accumulation in HCCLM3 xenograft tumors after a single oral dose of 40 mg/kg in male BALB/c nude mice[1].
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, 5 weeks old, 18-20 g, subcutaneous axillary implantation of HCCLM3 cells)[1]
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Dosage:60 mg/kg; 40 mg/kg; 20 mg/kg; 20 mg/kg (in combination with sorafenib 20 mg/kg)
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Administration:p.o.; once every 2 days; 28 days
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Result:Yielded tumor growth inhibition (TGI) values of 67.7% at 60 mg/kg, 58.2% at 40 mg/kg, and 46.6% at 20 mg/kg.
Produced a TGI of 70.9% when combined with 20 mg/kg sorafenib.
Caused no body weight loss in any treatment group.
Showed no appreciable lesions or tissue injury in the heart, liver, spleen, lung, or kidney via hematoxylin and eosin staining.
Chemical Information
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Masse moléculaire 590.80
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Formule C38H46N4O2
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SMILES
O=C(N1[C@@](CC/2)([H])[C@@]3([H])CCCN4[C@@]3([H])[C@](CCC4)([H])C1)C2=C\C5=CC=C6C=C(OCC7=CC=C(CN8CCNCC8)C=C7)C=CC6=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-2 Related Classifications
HY-187218 Related Classifications
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