GSK137
GSK137 is an orally active BCL6 inhibitor. GSK137 competitively blocks the protein-protein interactions of BCL6 with the corepressors SMRT, NCOR1, and BCOR. GSK137 produces only weak cell cycle arrest in multiple BCL6-positive diffuse large B-cell lymphoma cell lines and has almost no effect on tumor cell viability. GSK137 inhibits the generation of mouse germinal center B cells and Tfh cells, and downregulates TNP-specific IgM and IgG antibody levels. GSK137 can be used for research related to diffuse large B-cell lymphoma.
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- CAS No.: 2728727-91-9
- Formule: C21H19FN6
- Masse moléculaire:374.41
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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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Chemical Information
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Activité biologique
Description
In Vitro
GSK137 binds the BCL6 BTB-POZ lateral groove with a resolution of 2.04 Å, occupying the same site as the SMRT corepressor peptide[1].
GSK137 (1 μM; 24 h) does not degrade BCL6 protein in Farage DLBCL cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Farage DLBCL cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Did not reduce BCL6 protein levels in Farage cells.
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Cell Line:Farage, Karpas422, ULA, and VAL cells
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:14 days
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Result:had little to no effect on viability or proliferation of Farage, Karpas422, ULA, and VAL cells.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 (male, 30-40 g, 8-9 weeks of age, TNP-KLH (100 μg) on day 0)[1]
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Dosage:15, 30 mg/kg
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Administration:p.o.; three times daily; day -1 to day +12
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Result:Suppressed TNP‑specific IgM and IgG responses in TNP‑KLH‑immunized mice, with significant antibody reduction occurring only at day 12: 15 mg/kg and 30 mg/kg oral three‑times‑daily doses decreased IgM by 43 % / 58 %, IgG by 58 % / 66 %.
Diminished splenic germinal‑center B‑cell absolute numbers and relative frequency at day 12 for both dosing groups.
Lowered splenic Tfh‑cell absolute counts and CD4+ T‑cell‑subset frequency; 30 mg/kg dose returned total CD4+ T‑cell levels to naive‑animal baseline.
Yielded modelled maximum target‑engagement (TE) of 89.9 %‑94.7 % under repeated oral dosing, with calculated exposure durations above IC50/IC80/IC90 thresholds.
Chemical Information
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CAS No. 2728727-91-9
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Masse moléculaire 374.41
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Formule C21H19FN6
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SMILES
FC1=C(N2N=C1)N[C@@H](C[C@@H]2C3=C(N=CC=C3)C)C4=CC=CC5=C4C=CC(N)=N5
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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)
GSK137 Related Classifications
HY-148631 Related Classifications
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Keywords
- GSK137
- 2728727-91-9
- GSK 137
- GSK-137
- BCL6
- B-cell lymphoma 6 protein
- B-cell lymphoma 5 protein (BCL-5)
- Zinc finger and BTB domain-containing protein 27
- Zinc finger protein 51
- B-cell lymphoma
- BTB-POZ domain
- CD4+ T cells
- CD69
- SOCS2
- T-dependent antibody responses
- Tfh cells
- corepressor
- germinal center
- Inhibitor
- inhibitor
- inhibit