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Cat. No.: HY-148631

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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.

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

CAS No.: 2728727-91-9
Formula: C₂₁H₁₉FN₆
Molecular Weight:374.41

Storage:

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

Data Sheet (296 KB)

GSK137 Chemical Structure

CAS No.: 2728727-91-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

In Vitro

Anti-cancerCell Cycle RegulationOthers

Anti-cancer

GSK137 (0.01-10 μM; 14 days) has little effect on the viability or proliferation of Farage, Karpas422, ULA, and VAL cells^[1].
GSK137 moderately relieves the repression of BCL6 target genes in Farage cells, among which SOCS2 increases markedly and CD69 also increases^[1].

Anti-cancer

Cell Cycle Regulation

GSK137 induces a moderate G1 phase arrest in ULA, but only slight cell cycle changes in Farage, Karpas422, and VAL^[1].

Others

GSK137 is a potent cell-free inhibitor that inhibits the binding of corepressor peptide to the human BCL6 BTB-POZ domain, with a pIC₅₀ of 8 for SMRT; it inhibits the intracellular BCL6-SMRT corepressor interaction in live cells with a pIC₅₀ of 7.3^[1].
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.

Western Blot Analysis^[1]

Cell Line:

Farage DLBCL cells
Concentration:

1 μM
Incubation Time:

24 h
Result:

Did not reduce BCL6 protein levels in Farage cells.

Cell Viability Assay^[1]

Cell Line:

Farage, Karpas422, ULA, and VAL cells
Concentration:

0.01, 0.1, 1, 10 μM
Incubation Time:

14 days
Result:

had little to no effect on viability or proliferation of Farage, Karpas422, ULA, and VAL cells.

Parmacokinetics

Species	Dose	Route	C_max	T_max
Mice^[1]	15 mg/kg	p.o.	471 ng/mL	0.5 h
Mice^[1]	30 mg/kg	p.o.	1340 ng/mL	0.5 h

In Vivo

Adaptive ImmunityImmune Tolerance & Immunosuppression

Adaptive Immunity

GSK137 (15 mg/kg; p.o.; three times daily; Day -1 to Day +12) reduces the number of germinal centers in immunized C57BL/6J mice^[1].

Adaptive Immunity

Immune Tolerance & Immunosuppression

GSK137 (15-30 mg/kg; p.o.; three times daily; day -1 to day +12) inhibits T-dependent antigen-specific IgM and IgG responses in immunized CD1 mice and reduces the frequencies of splenic germinal center B cells and Tfh cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CD1 (male, 30-40 g, 8-9 weeks of age, TNP-KLH (100 μg) on day 0)^[1]
Dosage:

15, 30 mg/kg
Administration:

p.o.; three times daily; day -1 to day +12
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.

Related Protocols :

Chemical Information

CAS No. 2728727-91-9
Molecular Weight 374.41
Formula C₂₁H₁₉FN₆
SMILES

FC1=C(N2N=C1)N[C@@H](C[C@@H]2C3=C(N=CC=C3)C)C4=CC=CC5=C4C=CC(N)=N5
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (296 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Pearce AC, et al. GSK137, a potent small-molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice. The Journal of biological chemistry. 2021 Aug;297(2):100928. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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