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Pentostatin can inhibit adenosine deaminase irreversibly with Ki of 2.5 pM, as an antineoplastic anti-metabolite used in the treatment of several forms of leukemia.
Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties.
Pracinostat is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6 and has no activity against the class III isoenzyme SIRT I.
Roscovitine is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM and shows little effect on CDK4/6.
Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, > 130-fold selectivity for JAK1/2 versus JAK3.
TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s > 20,000 nM).
U0126 ethanol is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM.
Ulixertinib is a potent and reversible ERK1/ERK2 inhibitor with IC50 of < 0.3 nM for ERK2.
Urolithin B is a natural product with anti-proliferative and antioxidant activity, which can penetrate the blood-brain barrier and may have neuroprotective effects against Alzheimer’s Disease.
Vemurafenib is a potent inhibitor of B-Raf V600E with IC50 of 31 nM in cell-free assay, and is 10-fold selective for B-Raf V600E over wild-type B-Raf in enzymatic assays while the cellular selectivity can exceed 100-fold.
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