pi3kc2β

PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).

Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM ATR DNA-PK inhibition is 28 nM 35 nM 118 nM, respectively.

A66 is a specific and effective p110α inhibitor(IC50=32 nM).

AZD3458 is a potent and highly selective inhibitor of PI3Kγ (PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ with pIC50s of 9.1, 5.1, <4.5, and 6.5, respectively).

PQR530 is a highly potent dual pan-PI3K mTORC1 2 inhibitor. PQR530 inhibited protein kinase B (PKB, pSer473) and ribosomal protein S6 (pS6, pSer235 236) phosphorylation with IC50 values of 0.07 μM. It also showing antitumor activity.

PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.

PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .

PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.

AZD 6482 (KIN-193) is a potent and selective inhibitor of p110β and PI3Kβ with IC50 values ​​of 0.69nM and 10nM, respectively. AZD 6482 is particularly effective in blocking AKT signaling and tumor growth dependent on p110β activation or PTEN loss.

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2 3 3 15 30 23 nM for p110α β δ γ, mTOR, and DNA-PK).

MIPS-21335 is a potent PI3KC2α inhibitor with an IC50 value of 7 nM and additionally exhibits inhibitory activity against PI3KC2β, p110α, p110β, and p110δ with IC50 values of 0.043, 0.140, 0.386, and 0.742 μM, respectively. This compound demonstrates an antithrombotic effect [1].