Inobrodib (CCS-1477)

Catalog No.S9667 Synonyms: CBP-IN-1, CBP/p300-IN-4

For research use only.

Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.

Inobrodib (CCS-1477) Chemical Structure

CAS No. 2222941-37-7

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4)is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
Targets
p300/CBP bromodomain [1] androgen receptor [1] c-Myc [1]
In vitro

CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases AR- and C-MYC–regulated gene expression.[2]

In vivo

In AR-SV–driven models, CCS1477 has antitumor activity, regulating AR and C-MYC signaling. Early clinical studies suggest that CCS1477 modulates KLK3 blood levels and regulates CRPC biopsy biomarker expression.[2]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: 22Rv1 cells, C4-2 cells
  • Concentrations: 500 nM, 96 nM
  • Incubation Time: 5 hr, 24 hr
  • Method:

    22Rv1 and C4-2 cells are plated in hormone-deficient media for 72 hours, following which cells are treated with vehicle (0 nmol/L) or CCS1477 500 nmol/L for 5 hours, followed by the addition of 10 nmol/L dihydrotestosterone for 3 hours. Then ChIP is performed. 22Rv1 cells are seeded at equal density in hormone-deficient media. After 72 hours, cells are treated with either vehicle control, 100 nmol/L JQ1, or 96 nmol/L CCS1477. After 24 hours, cells are harvested and lysed, and RNA is extracted using TRIzol, per the manufacturer's instructions.

Animal Research:

[2]

  • Animal Models: male CD1 mice
  • Dosages: 3 mg/kg, 30 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 534.60
Formula

C30H32F2N4O3

CAS No. 2222941-37-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=NO1)C)C2=CC3=C(C=C2)N(C(=N3)C4CCCC(=O)N4C5=CC(=C(C=C5)F)F)C6CCC(CC6)OC

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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