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Chemical Structure| 901245-65-6 Chemical Structure| 901245-65-6

Structure of GSK-5959
CAS No.: 901245-65-6

Chemical Structure| 901245-65-6

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GSK5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM.

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Product Details of GSK-5959

CAS No. :901245-65-6
Formula : C22H26N4O3
M.W : 394.47
SMILES Code : O=C(NC1=C(N2CCCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
MDL No. :MFCD14744183

Safety of GSK-5959

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of GSK-5959

epigenetics

Isoform Comparison

Biological Activity

Target
  • BRPF

    BRPF3, pIC50:7.1

    BRPF2, pIC50:5.2

In Vitro:

Cell Line
Concentration Treated Time Description References
Huh-7 10 μM 24 h inhibited stem cell factor expression Commun Biol. 2021 Jul 20;4(1):888.
Hep3B 10 μM 24 h inhibited cell proliferation Commun Biol. 2021 Jul 20;4(1):888.
MHCC97L 10 μM 24 h inhibited cell proliferation and colony formation Commun Biol. 2021 Jul 20;4(1):888.
22Rv1 5 µM 24 h Assessment of potential ABCB1 functional inhibition by BRPF inhibitors via calcein retention assay, demonstrating that GSK-5959 treatment significantly increased green fluorescence accumulation in resistant cells. Cell Death Dis. 2024 Feb 12;15(2):132.
Du145-DtxR 1.25–5 µM 72 h Validation of dose-response curves for BRPF inhibitors on Dtx-resistant cells, showing that GSK-5959 combined with Dtx restored taxane sensitivity in resistant cells. Cell Death Dis. 2024 Feb 12;15(2):132.
high-grade serous ovarian cancer cells 10 µM 12 days To evaluate the effect of BRPF1 inhibition on high-grade serous ovarian cancer cells, results showed reduced cell proliferation Sci Rep. 2025 Mar 4;15(1):7602.
ovarian cancer cells 10 µM 12 days To evaluate the effect of BRPF1 inhibition on ovarian cancer cell proliferation, results showed that GSK6853 significantly inhibited cell proliferation Sci Rep. 2025 Mar 4;15(1):7602.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Subcutaneous tumor model Intraperitoneal injection 30 mg/kg Once daily for 2 weeks Significantly inhibited tumor growth without observable toxicity Commun Biol. 2021 Jul 20;4(1):888.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.35mL

5.07mL

2.54mL

References

 

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