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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C38H46N4O2
- 分子量:590.80
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
TBC1D2 0.4 μM (Kd) |
体外実験
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.
体内実験
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.
化学情報
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分子量 590.80
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TBC1D2-IN-2 関連分類
HY-187218 関連分類
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