PI3K/Akt/mTOR Signaling

MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM.

A butyrolactone derivative and autophagy inhibitor

Ipatasertib dihydrochloride (GDC-0068 (dihydrochloride)) (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.

Tenalisib (RP6530) (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.

PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor with an IC50 of 7 nM. PI4KIIIbeta-IN-9 also inhibits PI3Kδ and PI3Kγ with IC50s of 152 nM and 1046 nM, respectively.

PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2.

PF-AKT400 (AKT protein kinase inhibitor) is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).

Parsaclisib (INCB050465) (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib (INCB050465) shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib (INCB050465) can be used for the research of relapsed or refractory B-cell malignancies.

Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 shows antiviral activity against SARS-CoV-2 (IC50 of 3.1 μM), HCoV-229E (IC50 of 0.7 μM) and HCoV-OC43.

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.

JNJ-47117096 hydrochloride (MELK-T1 hydrochloride) is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.

GSK2110183 hydrochloride is the structural analogue of GSK2110183.

A dual inhibitor of PI3K and mTOR

Pomiferin (NSC 5113) (NSC 5113) acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 μM).

Recilisib (Ex-RAD) is a radiation protection agent that can activate the activities of AKT and PI3K in cells.

GSK2110183 is the structural analogue of GSK2110183.

BEBT-908 (PI3Kα inhibitor 1) (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .

Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib.

AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.

VX-984 (M9831) (M9831) is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 (M9831) efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 (M9831) can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research.

FT-1518 is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor, and exhibits antitumor activity.

K-80003 (TX-803) is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.

A dual inhibitor of PI3Kα and mTOR