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PD318088

Catalog No. T6152 CAS 391210-00-7

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

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PD318088, CAS 391210-00-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 46.00
2 mg	In stock	$ 83.00
5 mg	In stock	$ 133.00
10 mg	In stock	$ 252.00
25 mg	In stock	$ 473.00
50 mg	In stock	$ 695.00
100 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 163.00

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Purity: 99.69%

Biological Description

Chemical Properties

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Description	PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
In vitro	PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure. [1]
Kinase Assay	Enzyme Assays: Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software.

Molecular Weight	561.09
Formula	C16H13BrF3IN2O4
CAS No.	391210-00-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 14 mg/mL (24.95 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 112 mg/mL (199.61 mM)

References and Literature

1. Ohren JF, et al. Nat Struct Mol Biol, 2004, 11(12), 1192-1197.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Inhibitor Library MAPK Inhibitor Library Anti-COVID-19 Compound Library Reprogramming Compound Library Anti-Ovarian Cancer Compound Library Bioactive Compounds Library Max Anti-Obesity Compound Library HIF-1 Signaling Pathway Compound Library

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Related compounds with same targets

zapnometinib PD184161 Selumetinib BIX02188 GW 284543 hydrochloride Refametinib Pimasertib trans-Zeatin

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Keywords

PD318088 391210-00-7 MAPK MEK Mitogen-activated protein kinase kinase PD 318088 inhibit PD-318088 MAPKK MAP2K Inhibitor inhibitor

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