GSK690693 Chemical Structure
[Ala92]-p16 (84-103) is a CDK inhibitor with IC50 of 1.5μM for cyclin-dependent kinase-4 (cdk4)/cyclin D1
Bax inhibitor peptide,negative control is a negative control peptide for the Bax inhibitor peptides V5 and P5.
JNK and p38 MAPK inhibitor
SRC kinase inhibitor
Perifosine is an Akt inhibitor. the antiproliferative properties of perifosine with an IC50 of 0.6–8.9 µM.
Targeting VHL-deficient RCC cells, in renal cell carcinoma (RCC) cells that have lost the von Hippel-Lindau (VHL) tumor suppressor activity (IC50 = 625 μM).
MK-2206 is a highly selective inhibitor of Akt1, Akt2 and Akt3 with IC50 of 8 nM, 12 nM and 65 nM, respectively.
BTZ043 racemate is a decaprenylphosphoryl-b-D-ribose 2’-epimerase inhibitor with MIC of 2.3 and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.
cathepsin K inhibitor with an IC50 of 0.2nM.
Akt inhibitor
GSK690693 is an aminofurazan-derived,novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor. It is selective for the Akt isoforms(inhibits Akt kinases 1, 2, and 3 with IC50 values of 2, 13, and 9 nM respectively)versus the majority of kinases in other families; however, it does inhibit additional members of the AGC kinase family. [1,2]
GSK690693 inhibited proliferation and induced apoptosis in a subset of tumor cells with potency consistent with intracellular inhibition of Akt kinase activity. [1]
Daily administration of GSK690693 produced significant antitumor activity in mice bearing established human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts. [1]
| Molecular Weight (WM): | 425.48 |
|---|---|
| Formula: | C21H27N7O3 |
| CAS No.: | 937174-76-0 |
| Synonyms: |
N/A
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| Dissolve in (25°C): | DMSO ≥39mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

| Cell growth of sensitive (DLD1 and U87) and multi-drug resistant (DLD1-TxR and U87-TxR) cells assessed after 72 h of GSK690693 treatment. GSK690693 efficacy decreased in DLD1-TxR in comparison to its sensitive counterpart - DLD1. Colorectal carcinoma cell line (DLD1) possesses mutated p53, while its resistant counterpart (DLD1-TxR) additionally acquired the LOH in PTEN gene during the course of resistance induction. However, concentration-dependent cell growth inhibition induced by GSK690693 does not differ between sensitive (U87) and resistant (U87-TxR) glioblastoma cell lines. Both, U87 and U87-TxR have wt-p53 and PTEN-null. The results were obtained by the Sulforhodamine B assay. All values represent average ± SD obtained from two independent experiments, n = 5. |
Data independently produced by Dr Milica Pesic of Institute for Biological Research GSK690693 purchased from Selleck
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