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KRIBB11

Catalog No. T3652 CAS 342639-96-7

KRIBB11 is an inhibitor of Heat shock factor (HSF) inhibitor.

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KRIBB11, CAS 342639-96-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 70.00
25 mg	In stock	$ 162.00
50 mg	In stock	$ 276.00
100 mg	In stock	$ 537.00
200 mg	In stock	$ 755.00
500 mg	In stock	$ 1,150.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.91%

Purity: 98.64%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	KRIBB11 is an inhibitor of Heat shock factor (HSF) inhibitor.
Targets&IC50	HSF1:1.2 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].
Kinase Assay	HCT-116 cells are washed with PBS and then homogenized with a 27-gauge syringe in binding buffer (10 mm Tris-HCl (pH 7.4), 50 mm KCl, 5 mm MgCl2, 1 mm EDTA, and 0.1 mm Na3VO4). The cell lysate is centrifuged at 13,000 rpm for 30 min at 4°C, and the supernatant is collected. The HCT-116 cell lysate supernatant is precleared by incubating with Dynabeads M-280 streptavidin for 30 min at 4°C and captured by magnet separation. The cleared supernatants are incubated with biotinyl-KRIBB11 compound. After overnight incubation at 4°C, proteins associated with the biotinyl-KRIBB11 compound are precipitated with Dynabeads M-280 streptavidin. Precipitated samples are separated by a magnet. Samples are washed with 1 mL of ishing buffer containing 50 mm HEPES (pH 7.5), 50 mm NaCl, 1 mm EDTA, 1 mm EGTA, 0.1% Tween 20, 10% (v/v) glycerol, 1 mm NaF, 0.1 mm Na3VO4, and protease inhibitor mixture tablets (1 tablet/10 mL). Samples are boiled in SDS-PAGE sample buffer, separated by 10% polyacrylamide gel, and immunoblotted with antibodies against HSF1, HSF2, HSP90, or CDK9.
Cell Research	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)

Molecular Weight	284.27
Formula	C13H12N6O2
CAS No.	342639-96-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 3 mg/mL (10.55 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Metabolism Compound Library Anti-Breast Cancer Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Anti-Metabolism Disease Compound Library Endoplasmic Reticulum Stress Compound Library Bioactive Compound Library Apoptosis Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KRIBB11 342639-96-7 Apoptosis Cytoskeletal Signaling Metabolism HSP Inhibitor KRIBB 11 inhibit KRIBB-11 Heat shock proteins inhibitor

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