TBS6b
TBS6b is a potent and selective ACKR3 molecular glue degrader. TBS6b degrades ACKR3 via the ubiquitin-proteasome pathway. TBS6b inhibits hepatocellular carcinoma cell proliferation, migration, and invasion. TBS6b is relevant to hepatocellular carcinoma (HCC) research.
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- Formule: C29H28N2O6
- Masse moléculaire:500.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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ACKR3 |
TBS6b (0-4 μM; 48 h; HCCLM3 and HepG2 cells) reduces cell proliferation, migration, and invasion[1].
TBS6b (0-4 μM; 48 h; HCCLM3 and HepG2 cells) downregulates the expression of proliferation and mesenchymal markers (PCNA, N-cadherin, and Vimentin), while upregulating the epithelial marker E-cadherin in a dose-dependent fashion. TBS6b selectively inhibits ACKR3 protein expression without altering its mRNA levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCCLM3 and HepG2 cells
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Concentration:0 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:48 h
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Result:Significantly reduced cell proliferation in a dose-dependent manner.
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Cell Line:HCCLM3 and HepG2 cells
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Concentration:0 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:48 h
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Result:Significantly reduced cell migration in a dose-dependent manner.
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Cell Line:HCCLM3 and HepG2 cells
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Concentration:0 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:48 h
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Result:Significantly reduced cell invasion in a dose-dependent manner.
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Cell Line:HCCLM3 and HepG2 cells
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Concentration:0 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:48 h
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Result:Selectively inhibits ACKR3 protein expression without altering its mRNA levels.
TBS6b (5 mg/kg; IP; every other day; 4 weeks) reduces metastasis, and shows no significant changes in liver or kidney tissues in a mouse lung metastasis model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Balb/c-Foxn1nu mice (4-5 weeks) were subcutaneously injected with 1 × 107 cells/mL sh-NC and sh-ACKR3 (derived from HCCLM3) and NC and ACKR3 (derived from HepG2) cells[1].
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Dosage:5 mg/kg
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Administration:IP; every other day; 14 days
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Result:Suppressed tumor growth and metastasis without inducing significant toxicity, as evidenced by stable body weight, normal organ histology, and unchanged serum levels of ALT, AST, BUN, and CRE.
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Animal Model:Male Balb/c-Foxn1nu mice (4-5 weeks) were intravenously injected with 1 × 107 cells/mL sh-NC and sh-ACKR3 (derived from HCCLM3) and NC and ACKR3 (derived from HepG2) cells[1].
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Dosage:5 mg/kg
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Administration:IP; every other day; 4 weeks
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Result:Reduced metastasis. Decreased levels of Ki67, N-cadherin, and Vimentin, and increased E-cadherin in HCCLM3 cells, with no marked difference between combined and single-agent treatments.
Chemical Information
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Masse moléculaire 500.54
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Formule C29H28N2O6
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SMILES
COC1=C(C(OC)=C2C(C=C(OC2=C1)C3=CC=C(C=C3)OCCCN4C(C)=NC5=C4C=CC=C5)=O)OC
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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)
TBS6b Related Classifications
HY-179035 Related Classifications
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