mTORC2 Inhibitor

Torin 1 is a potent inhibitor of mTOR with an IC₅₀ of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC₅₀ values between 2 and 10 nM. Torin 1 is an effective inducer of autophagy.

AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC₅₀ of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2.

Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC₅₀ of 1 nM for mTOR kinase.

Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC₅₀s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.

eALM1137 is a mTOR inhibitor with an IC₅₀ of 4.8 nM. eALM1137 mediates dual inhibition of the mTORC1 and mTORC2 signaling pathways, and inhibits DNA-PK (IC₅₀=77 nM). eALM1137 exhibits antiproliferative and cytostatic activities, and induces G1 cell cycle arrest. eALM1137 is applicable to the research of glioblastoma multiforme.

Torin 2 is an mTOR inhibitor with EC₅₀ of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC₅₀: 200 nM). Torin 2 also inhibits DNA-PK with an IC₅₀ of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.

Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC₅₀s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2.

Dihydromyricetin is a potent inhibitor with an IC₅₀ of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC₅₀ of 22 μM.

Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with K_is of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. Omipalisib has anti-cancer activity.

PI-103 is a potent PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.

JR-AB2-011 is a selective mTORC2 inhibitor with an IC₅₀ value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (K_i: 0.19 μM).JR-AB2-011 decreases the phosphorylation level of Akt, decreases MMP2 activity, thereby reducing the ability of tumor cells to migrate and invade. JR-AB2-011 also induces non-apoptotic cell death.

Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC₅₀ of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.

Aloe emodin (Rhabarberone) is a natural hydroxyanthraquinone with antitumor activities. aloe-emodin can bind with mTORC2 and inhibit its kinase activity. Aloe emodin exerts antiproliferation effects and induces cellular apoptosis. Aloe emodin also exhibits antiviral activity that against influenza A virus.

Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC₅₀ of 8 nM. PP242 inhibits both mTORC1 and mTORC2 with IC₅₀s of 30 nM and 58 nM, respectively.

Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC₅₀s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations.

KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC₅₀s of 10 nM.

Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC₅₀s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a?K_i?of 17 nM for mTOR.

Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC₅₀s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.

CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC₅₀s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.

OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC₅₀ of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC₅₀s of 22 nM and 65 nM, respectively.