vps34

Vps34-IN-2 is a potent and selective Vps34 inhibitor (IC50s: 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively).

Vps34-PIK-III (VPS34-IN2), a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and results in the stabilization of autophagy substrates.

Vps34-IN-1 (VPS34-IN1) is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM in vitro, which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.

Vps34-IN-4 is a potent and selective inhibitor of VPS34 (IC50: 15 nM).

3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50 = 60 μM) and class III VPS34 (IC50 = 25 μM). 3-Methyladenine inhibits autophagy.

SAR-260301, an orally available and selective inhibitor of PI3Kβ [IC50: 23 nM].

CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM, exhibiting over 10-1500 fold selectivity over other class I, II, and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM), and PI4KIIIB (IC50, 300.2 nM). It inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells.

SAR-405 is a potent and selective PIK3C3/Vps34 inhibitor (IC50:1.2 nM; Kd:1.5 nM) that prevents autophagy and synergizes with MTOR inhibition in tumor cells. SAR405 treatment also inhibits autophagy induced either by starvation or by MTOR (mechanistic target of rapamycin) inhibition. Combining SAR405 with everolimus results in a significant synergy on the reduction of cell proliferation using renal tumor cells.

Buparlisib Hydrochloride (BKM120 HCl) is a specific and orally bioavailable pan-class I PI3K inhibitor that competitively inhibits PI3K/AKT kinase at the nanomolar level and suppresses cancer cell growth, making it suitable for studying breast cancer, glioblastoma, and solid tumours.

Buparlisib (BKM120) is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110α, p110β, and p110δ).

Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay.

PF-4989216 is a potent and selective PI3K inhibitor with IC50 values of 2 nM (p110α), 142 nM (p110β), 65 nM (p110γ), 1 nM (p110δ), and 110 nM (VPS34).

Vps34-IN-3 is a potent, selective, and orally bioavailable inhibitor of VPS34 kinase (Vps34).

SAR405 (R enantiomer) is the less active form of SAR405, an inhibitor of PIK3C3/Vps34.

Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.

Idelalisib (GS-1101) is a small molecule inhibitor of the PI3K catalytic subunit p110δ (IC50: 2.5 nM). The selectivity for p110δ is 40- to 300-fold than p110α/β/γ.

Acalisib (CAL-120) (GS-9820) is a potent and selective inhibitor of PI3Kδ.

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

Pilaralisib (XL-147) is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others.

VS-5584 (SB2343) is a pan-PI3K/mTOR kinase inhibitor.

CHMFL-PI4K-127 (compound 15g) is a highly selective inhibitor of PfPI4K (Plasmodium falciparum PI4K kinase) with oral activity (IC50=0.9 nM) and exhibits strong inhibitory activity against Plasmodium falciparum 3D7 (EC50=25.1 nM), demonstrating significant anti-malaria effects.

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.