1. PROTAC Immunology/Inflammation GPCR/G Protein
  2. Molecular Glues CXCR
  3. 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.

For research use only. We do not sell to patients.

TBS6b

TBS6b Chemical Structure

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Description

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[1].

IC50 & Target[1]

ACKR3

 

In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: HCCLM3 and HepG2 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 48 h
Result: Significantly reduced cell proliferation in a dose-dependent manner.

Cell Migration Assay [1]

Cell Line: HCCLM3 and HepG2 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 48 h
Result: Significantly reduced cell migration in a dose-dependent manner.

Cell Invasion Assay[1]

Cell Line: HCCLM3 and HepG2 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 48 h
Result: Significantly reduced cell invasion in a dose-dependent manner.

Western Blot Analysis[0]

Cell Line: HCCLM3 and HepG2 cells
Concentration: 0 μM, 1 μM, 2 μM, 4 μM
Incubation Time: 48 h
Result: Selectively inhibits ACKR3 protein expression without altering its mRNA levels.
In Vivo

TBS6b (5 mg/kg; IP; every other day; 14 days) suppresses mouse hepatocellular carcinoma tumor growth and metastasis without significant toxicity[1][1].
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.

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]
Dosage: 5 mg/kg
Administration: IP; every other day; 14 days
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.
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]
Dosage: 5 mg/kg
Administration: IP; every other day; 4 weeks
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.
Molecular Weight

500.54

Formula

C29H28N2O6

SMILES

COC1=C(C(OC)=C2C(C=C(OC2=C1)C3=CC=C(C=C3)OCCCN4C(C)=NC5=C4C=CC=C5)=O)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TBS6b
Cat. No.:
HY-179035
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