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PD318088 is a novel, small-molecule inhibitor of MEK1/2. MEK1 and MEK2 are closely related, dual-specificity tyrosine/threonine protein kinases found in the Ras/Raf/MEK/ERK mitogen-activated protein kinase (MAPK) signaling pathway. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 induces several conformational changes in the unphosphorylated MEK1 and MEK2 enzymes that lock them into a closed but catalytically inactive species.
| Molecular Weight | 561.09 |
| Formula | C16H13BrF3IN2O4 |
| CAS Number | 391210-00-7 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related MEK Products |
|---|
| AS703026
Pimasertib (AS-703026) is a novel selective MEK1/2 inhibitor, and induces pleiotropic anti-myeloma activity in vitro and in vivo. |
| AZD6244
AZD6244 (ARRY-142886, Selumetinib) is a potent MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nM. |
| AZD8330
AZD8330 (ARRY-424704) is a novel, selective, highly efficacious, uncompetitive MEK inhibitor with an IC50 of 7 nM. |
| CI-1040
CI-1040 (PD184352) is a targeted signal transduction inhibitor of MEK with a ki value of 300nM in vitro. |
| ARRY-162 (Binimetinib)
ARRY-162 (MEK-162; Binimetinib) is a selective, potent inhibitor of MEK and cellular pERK with IC50 of 12 nM and 11 nM, respectively. |
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