Research Area
Product Type
United States ( Change Country )
GSK1120212 (JTP-74057) Chemical Structure
Recommended Products
AZD6244 (Selumetinib)
AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.
CI-1040 (PD184352)
CI-1040 (PD184352) is a MEK 1/2 inhibitor. Ki of 300nM
PD0325901
PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.
RDEA119 (BAY 869766)
MEK inhibitor with EC50 of 73 nM.
U0126-EtOH
U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
PD98059
PD 98059 is an inhibitor of MEK1 and MEK2 with IC50 values of 4 μM and 50 μM respectively.
AS703026
AS703026 is a highly selective and potent noncompetitive inhibitor of MEK1/2 with an IC50 range of 5-11 nM.
BIX 02188
BIX02188 is a MEK5-selective inhibitor with an IC50 of 0.8 ± 1.0 μM.
BIX 02189
BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.
PD318088
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor.
Biological Activity
GSK1120212 (JTP-74057) is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2. [1] GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases. After treatment of GSK1120212 (JTP-74057), it led to the growth inhibition and upregulate p15INK4b and/or p27KIP1 in most of the colorectal cancer cell lines tested. In nude animal mice studies, JTP-74057 inhibited tumor growth of HT-29 and COLO205 xenografts when GSK1120212 (JTP-74057) was daily oral administered for 14 days. GSK1120212 (JTP-74057) showed an additive or a synergistic action in combination with the standard-of-care agents, 5-fluorouracil, oxaliplatin or SN-38. Sensitivity to JTP-74057-induced apoptosis may be an important factor for the estimation of in vivo efficacy, and sensitivity was enhanced by an Akt inhibitor. [2] GSK1120212 (JTP-74057) is originally developed by GlaxoSmithKline and is recruiting for phase I clinical trials for the treatment of solid tumors.
References on GSK1120212 (JTP-74057)
- [1] Int J Oncol. 2011 Jul;39(1):23-31.
- [2] Clin Cancer Res. 2011 Mar 1;17(5):989-1000.
Chemical Information
| Molecular Weight (WM): | 615.39 |
|---|---|
| Formula: | C26H23FIN5O4 |
| CAS No.: | 871700-17-3 |
| Synonyms: |
GSK212
|
| Dissolve in (25°C): | DMSO ≥6mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Notes:
Related Inhibitors
Recommended Screening Libraries
Chemical Library
A collection of 864 bioactive compounds
Inhibitor Library
A collection of 481 inhibitors
Kinase Inhibitor Library
A collection of 194 kinase inhibitors
Tyrosine Kinase Inhibitor Library
A collection of 85 tyrosine kinase inhibitors.
FDA Approved Drug Library
A collection of 426 FDA approved drugs
Natural Product Library
A collection of 139 natural products
Chemotherapeutic Agent Library
A collection of 40 chemotherapeutic agents
Epigenetics Compound library
A unique collection of 17 small molecule modulators
Stem Cell Compound library
A unique collection of 47 small molecule inhibitors
GPCR Compound library
A unique collection of 63 GPCR small molecules
We have 1 customer reviews of GSK1120212 (JTP-74057).
- (1)
- (0)
- (0)
- (0)
- (0)
- (0)
- (0)
- (0)
- (0)
Average Customer Review
(1 customer reviews)
-
Click to enlarge
Mouse carcinoma cells were treated with the inhibitors for 16 and 40h at the concentrations indicated. The effect on S-phase was evident at 16 hrs. (A) whereas apoptosis was induced at 40h. (B) Biological effects of the compounds correlated with effects on phosphorylation of the MEK target ERK. (C) IC50 on S-phase and ERK-posphorylation: TAK-733=1-10nM, GSK1120212=<1nM.
Mouse carcinoma cells were treated with the inhibitors for 16 and 40h at the concentrations indicated. The effect on S-phase was evident at 16 hrs. (A) whereas apoptosis was induced at 40h. (B) Biological effects of the compounds correlated with effects on phosphorylation of the MEK target ERK. (C) IC50 on S-phase and ERK-posphorylation: TAK-733=1-10nM, GSK1120212=<1nM.
Data independently produced by one customer GSK1120212 (JTP-74057) purchased from Selleck
Check our customer reviews
Mouse carcinoma cells were treated with the inhibitors for 16 and 40h at the concentrations indicated. The effect on S-phase was evident at 16 hrs. (A) whereas apoptosis was induced at 40h. (B) Biological effects of the compounds correlated with effects on phosphorylation of the MEK target ERK. (C) IC50 on S-phase and ERK-posphorylation: TAK-733=1-10nM, GSK1120212=<1nM. |
Data independently produced by one customer
We give free samples and rewards to people who would like to provide us useful scientific data(western blot, etc.) > See Details
Recently Viewed Items
Keywords:buy GSK1120212 (JTP-74057) | GSK1120212 (JTP-74057) supplier | purchase GSK1120212 (JTP-74057) | GSK1120212 (JTP-74057) cost | GSK1120212 (JTP-74057) manufacturer | order GSK1120212 (JTP-74057) | GSK1120212 (JTP-74057) distributor