[CAS NO. 342639-96-7] KRIBB11
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PRODUCTS SPECIFICATIONS [342639-96-7]
Catalog
SLK-S8402
Brand
Selleck
CAS
342639-96-7
DESCRIPTION [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
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 .
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.
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.
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