AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1. 5μM AZD1480 induces G2/M arrest and cell death by inhibiting Aurora kinases. AZD1480 is a p ...
XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting 50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1. XL019 is a highly selective JAK2 inhibitor, binds to the active site of JAK2 displaying 50-fold selectivity against JAK1 and TYK2. ...
Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα , PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2. PKI-587 shows potent inhibitory activity against PI3K-α, PI3K-γ and mTOR with IC50 of ...
CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and 100-fold selectivity over PI3Kα and PI3Kδ. CZC24832 has excellent selectivity to PI3Kγ. Out of the 154 identified lipid and protein kinases and the 922 ...
CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM in cell-free assays; ability to distinguish between GSK-3 and its closest homologs Cdc2 and ERK2. CHIR-99021 shows greater than 500-fold selectivity for ...
SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB 216763 displays similar potency for GSK-3β with 96% inhibitionat 10 μM while exhibiting minimal activity against 24 other protein kinas ...
Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat inhibits the activities of HDAC1 and HDAC3 with IC50 of 10 nM and 20 nM, respectively. Vorinostat also results in a marked hyperacetylation of ...
Entinostat (MS-275) stron gly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Phase 3. MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. ...
XL388 is a highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases. In MCF7 cells, XL388 blocks mTORC1 phosphorylation of p70S6K (T389)with an IC50 value of 94 nM and blocks mTORC2 phosphoryl ...
Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ , mTORC1/2 with K i of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Phase 1. GSK2126458 potently inhibits the activity of common a ...
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