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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.

Synonyms: GSK-5959

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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
Synonyms :
GSK-5959
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 Huh-7 inhibited stem cell factor expression Commun Biol. 2021 Jul 20;4(1):888.
Hep3B Hep3B inhibited cell proliferation Commun Biol. 2021 Jul 20;4(1):888.
MHCC97L MHCC97L inhibited cell proliferation and colony formation Commun Biol. 2021 Jul 20;4(1):888.
22Rv1 22Rv1 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 Du145-DtxR 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 high-grade serous ovarian cancer cells 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 ovarian cancer cells 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

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