KRIBB11

Catalog No.S8402

KRIBB11 Chemical Structure

Molecular Weight(MW): 284.27

KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1).

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Biological Activity

Description KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1).
Targets
HSF1 [1]
(Cell-based assay)
1.2 μM
In vitro

KRIBB11 inhibits HSF1 activity in a concentration-dependent manner. It down-regulates HSP70 and HSP27. KRIBB11 can inhibit cancer cell proliferation, arrests the cell cycle at G2/M phase and induces apoptosis. But it does not inhibit heat shock-induced recruitment of HSF1 to the hsp70 promoter or phosphorylation of HSF1 Ser-230. KRIBB11 inhibits heat shock-induced recruitment of pTEFb to the hsp70 promoter and p-TEFb-dependent Phosphorylation of polⅡ CTD Ser-2[1].

In vivo Using a mouse xenograft model, KRIBB11 treatment decreases tumor volume by 47% compared with untreated control mice. In addition, HSP70 protein levels are significantly decreased in tumors from mice treated with KRIBB11, supporting the notion that KRIBB11 exerts its in vivo antitumor activity through HSF1 inhibition[1].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: HCT-116 cells
  • Concentrations: 0, 1, 2, 5, 7, 10, 20, 30 μM
  • Incubation Time: 48 h
  • Method: HCT-116 cells are treated with KRIBB11 at various concentrations for 48 h. Cells are then harvested by trypsinization, fixed with 70% chilled ethanol, and preserved at −20 °C before FACS analysis. Fixed cells are washed twice with phosphate-buffered saline (PBS) solution before being suspended in 500 μl of PBS and treated with 100 mg/ml RNase A at 37 °C for 30 min. Propidium iodide is then added to a final concentration of 50 mg/ml for DNA staining, and 20,000 fixed cells are analyzed on a FACSCalibur system. Cell cycle distribution is analyzed using the ModFit program.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Pathogen-free Balb/c nude mice
  • Formulation: 10% dimethylacetamide, 50% PEG300, and 40% distilled water
  • Dosages: 50 mg/kg/day
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 3 mg/mL (10.55 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 284.27
Formula

C13H12N6O2

CAS No. 342639-96-7
Storage powder
in solvent
Synonyms N/A

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID