Showing 1537–1552 of 5741 results

Losmapimod (GW856553X)

Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.

Skepinone-L

Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.

Thiamet G

Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37,000-fold selectivity over human lysosomal –hexosaminidase.

PF-04418948

PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1.

GSK650394

GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.

Bisindolylmaleimide I (GF109203X)

Bisindolylmaleimide I (GF109203X) is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.

Bisindolylmaleimide IX (Ro 31-8220 Mesylate)

Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1.

CNX-2006

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.

Idasanutlin (RG-7388)

Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Phase 3.

DBeQ

DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor with IC50 of 1.5 μM.

BIO

BIO is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor.

RKI-1447

RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, has anti-invasive and antitumor activities.

GZD824 Dimesylate (HQP1351)

GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.

1-Azakenpaullone

1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.

PF-04620110

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.