|Description||LY294002 is a potent inhibitor of phosphoinositide PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively.|
|Appearance||White to off-white solid|
|Current Developer||Eli Lilly|
740 Y-P is a cell-permeable phosphopeptide activator of PI3K. It binds to the p85 N- and C-terminal SH2 domains of PI3K but not to GST or the N-terminal domain ...
PIK-294 is a potent PI3K inhibitor.
Pilaralisib is a Class 1 phosphatidylinositol 3 kinase (PI3K) family inhibitor. It is an orally bioavailable small molecule, targeting the class I PI3K family o...
NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) and is a highly potent mTOR inhibitor, with reasonable liver microsome stability.
GDC-0084, a PI3K inhibitor, has been found to have probable antineoplastic effect and could pass blood-brain barrier with favourable penetration. It was just li...
AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
TG100-115, inhibited PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively), whereas both PI3Kα and -β were relatively unaffected (IC50 values>1 μM). As a ga...
PI3Kα inhibitor 1
PI3Kα inhibitor 1 is an inhibitor of PI3Kα as well as HDAC and probably have antineoplastic activity. IC50: ＜0.1 μM.
CNX-1351 is a selective covalent Inhibitor of PI3Kα. In an end point assay, CNX-1351 potently inhibited PI3Kα and was 20−400 times less potent against β, γ, an...
CH5132799 is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3K; (IC(50)=0.014 uM). In human tumor cell lines ...
1,3-Dicaffeoylquinic acid, a caffeoylquinic acid derivative found in artichoke, acts as an anti-hyperlipidemic agent and activates PI3K/Akt.
AS-252424 is a novel, potent PI3Kγ inhibitor (IC50 of 30 nM) with a 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.
Alpelisib, also known as BLY719, is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor...
LY3023414, a quinoline derivative, has been found to be a PI3Kα and mTOR inhibitor that could influence cell proliferation and cycle of tumor cells. It was just...
CAL-130 is a potent and selective PI3K gamma and delta inhibitor with potential anticancer activity. Constitutive phosphoinositide 3-kinase (PI3K)/Akt activatio...
NVP-BKM120 Hcl(BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively.
CZC24832 is the first selective inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with efficacy in in vitro and in vivo models of inflammation. Extensive target-...
RP-6530, a purine derivative, has been found to be a PI3Kδ/γ inhibitor that could exhibit cytotoxicity in some lymphoma primary cells so that is significant in ...