In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO
40%PEG300
5%Tween80
50%ddH2O
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
1.470mg/ml
(5.17mM)
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.
Clear solution
5% DMSO
95% Corn oil
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
2.800mg/ml
(9.85mM)
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.
* <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). This compound induces growth arrest and apoptosis.
Targets
HSF1 (Cell-based assay)
1.2 μM
In vitro
KRIBB11 inhibits HSF1 activity in a concentration-dependent manner. It down-regulates HSP70 and HSP27. This compound 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. This chemical inhibits heat shock-induced recruitment of pTEFb to the hsp70 promoter and p-TEFb-dependent Phosphorylation of polⅡ CTD Ser-2.
In Vivo
Using a mouse xenograft model, KRIBB11 treatment decreases tumour volume by 47% compared with untreated control mice. In addition, HSP70 protein levels are significantly decreased in tumours from mice treated with this compound, supporting the notion that it exerts its in vivo anti-tumour activity through HSF1 inhibition.
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.
Enhancement of Triple-Negative Breast Cancer-Specific Induction of Cell Death by Silver Nanoparticles by Combined Treatment with Proteotoxic Stress Response Inhibitors
[ Nanomaterials (Basel), 2024, 14(19)1564]
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]
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]
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]
Generation of GCaMP6s-Expressing Zebrafish to Monitor Spatiotemporal Dynamics of Calcium Signaling Elicited by Heat Stress
[ Int J Mol Sci, 2021, 22(11)5551]
Targeting HSF1 as a Therapeutic Strategy for Multiple Mechanisms of EGFR Inhibitor Resistance in EGFR Mutant Non-Small-Cell Lung Cancer
[ Cancers (Basel), 2021, 13(12)2987]
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.
