PI3K

AS-605240 is an orally active inhibitor of PI3-kinase γ that inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

AZD6482 is a PI3Kbeta inhibitor (IC50=0.021M) used in antithrombotic therapy.

BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.

CAL-101 is an isoform-selective inhibitor of PI3K that induces apoptosis of chronic lymphocytic leukemia (CLL) cells.

GDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) , with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR respectively.

GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM).

IC-87114 was the first isoform-selective PI3K inhibitor :p110M-NM-4(IC50 = 0.13 M-BM-5M) vs. p110M-NM-1(IC50 = 200 M-BM-5M), p110M-NM-2(IC50 = 16 M-BM-5M) and p110M-NM-3(IC50 = 61 M-BM-5M).

LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR.

PIK-293 is a PI3-K inhibitor. PIK-293 inhibits the p110α, p110β, p110δ. PIK-293 is the parent compound of PIK-294.

PIK-294 is a PI3 Kinase inhibitor that is 20- to 60-fold more potent than the parent compound, PIK-293. It is one of the most potent p110δ-selective inhibitors that has been reported.

PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM.2 It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 μM and 1.3 μM, respectively.

PIK-90 is a synthetic phosphoinositide 3-kinase (PI3K) inhibitor with IC50 values (nM) of 11, 350, 18, and 58 for p110 α, β, γ and δ isoforms, low mTOR activity.

Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.

Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.

Desmethyl-VS-5584 is a demethyl analogue of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.

TG100-115 inhibits PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively).

TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.

XL147 is a potent, selective and orally bioavailable small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K) with potential antineoplastic activity.

XL765 is a PI3K/mTOR dual kinase inhibitor and it is more potent compared to an agent that inhibits either PI3K kinase or mTOR kinase alone.

ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms.

BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor.

GDC-0980 (RG7422) is a selective, potent, orally bioavailable inhibitor of Class I PI3 kinase and mTOR kinase (TORC1/2) with in vitro IC50 of 5, 27, 7 and 14 nM for p110 α, β, δ and γ isoforms, respectively.

PF-04691502 is a PI3K/mTOR kinase inhibitor, is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway.

GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.

YM201636 is a cell-permeable and selective inhibitor of PIKfyve (IC50 = 33 nM).

PKI-587 is a highly potent PI3K/mTOR kinase inhibitor that inhibits PI3K-α,β,γ, δ isoforms and mTOR with IC50 of 0.4, 6.0, 5.4, 6.0 and 1.6 nM respectively.

PKI-402 is a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor.

NU-7441 (KU-57788) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor. The IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively.

AS-252424 is a potent inhibitor of PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000, and 20,000 nM respectively.

3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).

CUDC-907 (Fimepinostat) is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses.

Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).

NVP-BGT226, novel phosphoinositide 3-kinase/mTOR dual inhibitor, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo.

CH5132799 is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM).

CAY10505 is a potent inhibitor of PI3K, selectively inhibiting the γ isoform (IC50 = 30 nM) better than the α, β, and δ isoforms (IC50 = 0.94, 20, and 20 μM, respectively).

AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.

D-106669 is a highly potent and selective PI3K inhibitor, (PI3Kα IC50 <10 nM, >3 log selectivity against tyrosine or serine/threonine kinases, except ERK1 and 2).

The S-enantiomer of A66 is a potent inhibitor of the p110alpha isoform of PI 3-kinase (PIK3CA).

PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR).

PX-866 is a small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity.

Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.

BLY719 is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.

CZC24832 is a selective inhibitor of PI 3-Kinase γ (IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay).

Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

NVP-BAG956 acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor, displaying much reduced potency against VEGFR1 (IC50 = 2.56 uM) and little or no activity toward a panel of 15 other kinases (IC50 >10 uM).

BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity.

GSK2636771 is a potent, orally bioavailable, PI3K beta-selective inhibitor.

TG 100713 is an inhibitor of PI3-kinase that inhibits endothelial cell proliferation.

IPI-145, also known as INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.