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Catalog:
SLK-S8402
Brand:
Selleck
CAS:
342639-96-7
Overview
MDL
MFCD30182306
Molecular Weight
284.27
Molecular Formula
C13H12N6O2
SMILES
O=[N+](C1=CC=C(NC)N=C1NC2=CC3=C(NN=C3)C=C2)[O-]
For research use only.
Storage
3 years,-20°C,powder 1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
3.5178 mL
17.5889 mL
35.1778 mL
5 mM
0.7036 mL
3.5178 mL
7.0356 mL
10 mM
0.3518 mL
1.7589 mL
3.5178 mL
50 mM
0.0704 mL
0.3518 mL
0.7036 mL
Description
KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor . KRIBB11 induces growth arrest and .
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.
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.
