Inhibitors

An orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC 50 = 182 nM, K i = 0.99 nM) that is shown to act in a reversible and time-dependent manner.

A cell-permeable pyrido-pyrimidine compound that acts as a highly selective and potent inhibitor against both mTORC1 &amp mTORC2 (IC 50 = ~10 nM against mTOR activity in raptor or rictor immunoprecipitate from HEK293 with 100 &#181M ATP), with

A cell-permeable pyridinonequinoline derivative that acts as a highly potent, ATP-competitive inhibibitor against mTOR and DNA-PK (IC 50 = 4.32 and 6.

A Torin1 (Cat. No.

Other Notes Please note that Sigma-Aldrich provides this product to early discovery researchers as part of a collection of rare and unique chemicals. Sigma-Aldrich does not collect analytical data for this product.

A dihydroquinilone-pyrazoline NMDA antagonist, which is selective for NMDA receptors that are comprised of recombinant subunits GluN1/GluN2C (IC 50 = 5.4 &#181M) and GluN1/GluN2D (2.

A cell-permeable phenylacetate based compound that specifically blocks the Nur77-p38&#945 interaction by directly targeting the ligand-binding domain of Nur77 (~1 to 10 &#181M) and impedes Nur77 phosphorylation by p38&#945. Does neither modulate

A cell-permeable aminobenzophenone compound that acts as a potent, ATP-binding pocket-targeting inhibitor against p38&#945 and p38&#946 2 (82% and 93% inhibition with 1 &#181M inhibitor, respectively IC 50 of p38&#945 inhibition = 40 nM) with

A cell permeable, potent, and selective oxime PDE4D inhibitor (IC 50 = 0.67 &#181M) which displays much reduced activities toward other PDE4 isoforms.

A cell-permeable, blood-brain barrier permeant, pyrazolo[3,4 d]pyrimidinone compound that acts as a highly potent, selective, and active site-targeting inhibitor of phosphodiesterase 9A (PDE9A K i = 2.8 nM, 4.

A cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC 50 = 11, 18, 47, 58, 64, 350, and 830 nM against p110&#945, p110&#947, PI 3-KC2&#945,

A cell-permeable thienopyrimidine compound that acts as a potent, ATP-competitive inhibitor against class IA (IC 50 = 3 nM/p110&#945, 33 nM/p110&#946, 3 nM/p110&#948) &amp IB (IC 50 = 75 nM/p110&#947) PI 3-K kinases, including the two known