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KRIBB11

SKU: orb1303955

Description

KRIBB11

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Images & Validation

Key Properties

CAS Number342639-96-7
MW284.27
Purity98.11%
FormulaC13H12N6O2
SMILESCNc1ccc(c(Nc2ccc3[nH]ncc3c2)n1)[N+]([O-])=O
TargetHSP,Apoptosis
SolubilityDMSO:3 mg/mL (10.55 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.52 mM)

Bioactivity

Target IC50
HSF1:1.2 μM
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.
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.
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)

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Inhibitor, Heat shock proteins, HSF1, HSP, inhibit, KRIBB 11, KRIBB11, KRIBB-11, Apoptosis

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    C13H12N6O2

    1 g, 500 mg, 50 mg, 100 mg, 200 mg, 10 mg, 5 mg, 25 mg
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Key Properties

No computed properties available.

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Protocol Information

KRIBB11 (orb1303955)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 ml x 10 mM (in DMSO)
$ 90.00
5 mg
$ 90.00
10 mg
$ 110.00
25 mg
$ 210.00
50 mg
$ 320.00
100 mg
$ 580.00
200 mg
$ 800.00
500 mg
$ 1,190.00
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