|Description||ON 146040 was highly potent in killing hematologic tumor cells with IC50 values in the 150 to 1,000 nM range. In biochemical testing, ON 146040 inhibited PI3K α/δ isoforms (IC50 ≈ 14 and 20 nM, respectively) without having a major effect on β/γ isoforms (IC50 ≈ 3 and 1 μM, respectively). ON 146040 was also found to inhibit Abl1 and several mutant versions of this kinase (IC50 < 150 nM), although the compound was not found to be active against the T315I mutant. Following treatment with ON 146040, STAT3 and STAT5 phosphorylation were down-regulated in leukemia and myeloma cells.|
AS605240 is a selective PI3Kgamma inhibitor, has been proved effective on several inflammatory diseases. Orally administration of AS605240 significantly prevent...
AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ. Phase 1.
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-...
1,3-Dicaffeoylquinic acid, a caffeoylquinic acid derivative found in artichoke, acts as an anti-hyperlipidemic agent and activates PI3K/Akt.
AZD-8835 was selected as a clinical candidate for the treatment of PIK3CA-dependent cancers and is currently in phase I clinical trials. It is an orally bioavai...
PI-3065 is a novel potent and selective PI3K p110δ inhibitor with IC50 of 15 nM; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mTOR.
GDC-0941 is a potent pan inhibitor of class I catalytic subunits of PI3K that inhibits p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM.
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.
ZSTK474 is a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, which strongly inhibits cancer cell proliferation. Phosphoinositide 3-kinase (PI3K) is a pote...
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...
Inhibition of p110α alone by A66 treatment is sufficient to block insulin signalling to Akt/PKB in certain cell lines that harbor H1047R mutations in PIK3CA and...
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 ...
CAL-130 is a potent and selective PI3K gamma and delta inhibitor with potential anticancer activity. Constitutive phosphoinositide 3-kinase (PI3K)/Akt activatio...
SAR-405 is a potent and selective inhibitor of phosphoinositide 3-kinase (PI3K) class III isoform Vps34 (IC50= 1.2 nM, Kd= 1.5 nM) without disrupting other PI3K...
In the absence of PTEN phosphatase tumor suppressor function, PI3Kγ or PI3Kδ alone can support leukemogenesis, whereas inactivation of both isoforms suppressed ...
Seletalisib is a selective Phosphatidylinositol 3 kinase delta inhibitor originated by UCB.It is a Immunomodulator. Phaes I clinical trials for Plaque psoriasis...
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.
PF-4989216 is a novel potent and selective PI3K inhibitor. PF-4989216 inhibits the phosphorylation of PI3K downstream molecules and subsequently leads to inhib...
GSK-2269557 HCl salt
GSK-2269557 is a selective Phosphatidylinositol 3 kinase delta inhibitor originated by GlaxoSmithKline. GSK-2269557 is highly selective for PI3Kδ over the close...
PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR (Kis= 10.6 nM and 12.5 nM for mTOR and PI3Kα, respectively).