mtorc2

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

PQR620 is a novel potent and selective, brain penetrant inhibitor of mTORC1/2.

FT-1518 is an orally available, selective and potent mTORC1 and mTORC2 inhibitor with anticancer and antitumor activity for cancer research.

JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. It inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM) and exhibits cytotoxicity in glioblastoma [1].

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

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.

Torkinib (PP 242) (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).

KU-0063794 is a potent and highly specific dual inhibitor of mTORC1 and mTORC2.

Palomid 529 (SG 00529) has been used in trials studying the treatment of Age-Related Macular Degeneration.

MTI-31 (LXI-15029) is a potent, orally active, and highly selective inhibitor of mTORC1 and mTORC2, exhibiting a Kd of 0.20 nM for mTOR and >5,000-fold selectivity over PIK3CA, PIK3CB, and PIK3G in binding assays, with an IC50 of 39 nM for mTOR in a LANCE assay of mTOR substrate phosphorylation with 100 μM ATP [1].

AZD 3147 is an inhibitor of mTORC with IC50s of 40.7 and 5.75 nM for mTORC1 and mTORC2. AZD 3147 shows IC50s of 912, 5495, 9333, and 6310 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively.

XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.

OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.

Omipalisib (GSK2126458) is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic 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-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).

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).

PI-103 Hydrochloride is a dual PI3K/Akt and mTOR inhibitor exhibiting nM-level inhibition of p110α, p110β, p110δ, p110γ, DNA-PK, mTORC1, and mTORC2. PI-103 induces autophagy, mitochondrial apoptosis, and cell cycle arrest, making it suitable for leukaemia research.

Voxtalisib (XL765) (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.

AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.

mTOR inhibitor-3 is a selective mTOR inhibitor (Ki= 1.5 nM). mTOR inhibitor-3 inhibits mTORC1 and mTORC2 in cellular and in vivo experiments.

WYE-125132 (WYE-132 (WYE-125132)) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.

GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.

WAY-600 is a potent, ATP-competitive, and selective inhibitor of mTOR with an IC50 of 9 nM; it blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308), and is selective for mTOR over PI3Kα (>100-fold) and PI3Kγ (>500-fold).