KRIBB11

Catalog No.S8402 Batch:S840201

Technical Data

Formula	C₁₃H₁₂N₆O₂
Molecular Weight	284.27	CAS No.	342639-96-7
Solubility (25°C)*	In vitro	DMSO	3 mg/mL (10.55 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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.)

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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). 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.

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.

References

[1] Yoon YJ, et al. J Biol Chem. 2011, 286(3):1737-47.

Selleck's KRIBB11 has been cited by 13 publications

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
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
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]	PubMed: 34203709
The Meningioma Enhancer Landscape Delineates Novel Subgroups and Drives Druggable Dependencies [ Cancer Discov, 2020, CD-20-0160]	PubMed: 32703768

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SHIPPING AND STORAGE
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