KRIBB11

Catalog No.S8402 Batch:S840202

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Technical Data

Formula

C13H12N6O2
Molecular Weight 284.27 CAS No. 342639-96-7
Solubility (25°C)* In vitro DMSO 57 mg/mL (200.51 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
2.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of 56 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.47mg/ml Taking the 1 mL working solution as an example, add 50 μL of 29.4 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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). KRIBB11 induces growth arrest and apoptosis.
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 (from reference)

Cell Assay:[1]
  • 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.
Animal Study:[1]
  • Animal Models

    Pathogen-free Balb/c nude mice

  • Dosages

    50 mg/kg/day

  • Administration

    i.p.

Selleck's KRIBB11 has been cited by 15 publications

PANX1-mediated ATP release confers FAM3A's suppression effects on hepatic gluconeogenesis and lipogenesis [ Mil Med Res, 2024, 11(1):41] PubMed: 38937853
USP36 stabilizes nucleolar Snail1 to promote ribosome biogenesis and cancer cell survival upon ribotoxic stress [ Nat Commun, 2023, 14(1):6473] PubMed: 37833415
USP36 stabilizes nucleolar Snail1 to promote ribosome biogenesis and cancer cell survival upon ribotoxic stress [ Nat Commun, 2023, 14(1):6473] PubMed: 37833415
Reactive sulfur species disaggregate the SQSTM1/p62-based aggresome-like induced structures via the HSP70 induction and prevent parthanatos [ J Biol Chem, 2023, 299(6):104710] PubMed: 37060999
Reactive sulfur species disaggregate the SQSTM1/p62-based aggresome-like induced structures via the HSP70 induction and prevent parthanatos [ J Biol Chem, 2023, 299(6):104710] PubMed: 37060999
HSF1 facilitates the multistep process of lymphatic metastasis in bladder cancer via a novel PRMT5-WDR5-dependent transcriptional program [ Cancer Commun (Lond), 2022, 42(5):447-470] PubMed: 35434944
Adhesion-mediated mechanosignaling forces mitohormesis [ Cell Metab, 2021, S1550-4131(21)00183-2] PubMed: 34019840
Nuciferine protects against folic acid-induced acute kidney injury by inhibiting ferroptosis [ Br J Pharmacol, 2021, 178(5):1182-1199] PubMed: 33450067
Ferroptosis inducer erastin sensitizes NSCLC cells to celastrol through activation of the ROS-mitochondrial fission-mitophagy axis [ Mol Oncol, 2021, 10.1002/1878-0261.12936] PubMed: 33675143
Generation of GCaMP6s-Expressing Zebrafish to Monitor Spatiotemporal Dynamics of Calcium Signaling Elicited by Heat Stress [ Int J Mol Sci, 2021, 22(11)5551] PubMed: 34074030

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.