mtorc2

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.

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.

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

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.

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.

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

JR-AB2-011 is a selective mTORC2 inhibitor with an IC 50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association ( K i : 0.19 μM) and is cytotoxic in glioblastoma [1].

WYE-354(IC50=5 nM) is an effective, selective and ATP-competitive mTOR inhibitor. It blocks mTORC2 P-AKT(S473) and mTORC1 P-S6K(T389), not P-AKT(T308). The selectivity for mTOR is higher than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR).

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

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.

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

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

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

Thioether-cyclized helix B peptide, CHBP (TFA), is the trifluoroacetic (TFA) salt of CHBP. This form enhances metabolic stability and exhibits renoprotective effects by promoting autophagy, achieved through the inhibition of mTOR C1 and activation of mTOR C2 [1].

Thioether-cyclized helix B peptide (CHBP) enhances metabolic stability and exerts renoprotective effects by promoting autophagy through the inhibition of mTOR C1 and activation of mTOR C2 [1].

BIA is an inhibitor of the interaction between TMBIM6 and mTORC2, which ultimately blocks AKT activation and cancer progression.

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.

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

CC-115 is a inhibitor of mTOR DNA-PK (IC50= 21 13 nM).

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.

RMC-6272 (RM-006) is a bi-steric inhibitor that selectively targets mTORC1, displaying potent and selective (> 10-fold) inhibition over mTORC2. Compared to Rapamycin, RMC-6272 demonstrates enhanced inhibition of mTORC1 and induces increased cell death in TSC2 null tumors.

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).

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.

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

CZ415 is a potent and highly selective mTOR inhibitor.

DCBCI0901 is an inhibitor of phosphatidylinositide 3-kinase (PI3K), raptor-mTOR (mTOR complex 1 or mTORC1) and rictor-mTOR (mTOR complex 2 or mTORC2) with potential antineoplastic activity.

CC214-2 is a potent dual inhibitor of mTORC1 and mTORC2, known for its ability to impede autophagy by modulating mammalian target of rapamycin (mTOR) signaling. With this capacity, CC214-2 shows promise in shortening the duration of tuberculosis (TB) [1].

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).

Gedatolisib (PF-05212384) is a highly effective dual inhibitor targeting the PI3Kα/γ (IC50: 0.4/5.4 nM)and mTOR (IC50: 1.6 nM) in the PI3K/mTOR signaling pathway.

BI-860585 is an inhibitor of Raptor-Mammalian Target of Rapamycin (mTOR) Complex 1 (mTOR Complex 1; mTORC1) and rictor-mTOR Complex 2 (mTOR Complex 2; mTORC2), with potential Anti-tumor activity.

Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.

Onatasertib (CC223) is an orally available mTOR inhibitor with potential antitumor activity. Onatasertib inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. Onatasertib is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivity than the related lipid kinase PI3Kα (IC50: 4 μM).

OXA-01 is a potent mTORC1 and mTORC2 inhibitor, with IC 50 values of 29 nM and 7 nM, respectively [1]. OXA-01 demonstrates broad anti-tumor activity.

TMBIM6 antagonist-1 (BAX-inhibitor-1) is a bax inhibitor

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

PP30 is an inhibitor of mTORC1 and mTORC2. It is selective within the PI3K family, inhibiting other PI3Ks only at high concentrations.

PI-103 Hydrochloride is a potent dual inhibitor of PI3K and mTOR, demonstrating inhibitory IC50 values of 8 nM for p110α, 88 nM for p110β, 48 nM for p110δ, 150 nM for p110γ, 20 nM for mTORC1, and 83 nM for mTORC2, respectively. Additionally, it inhibits DNA-PK with an IC50 of 2 nM and induces autophagy [1] [2] [3] [4].

(32-Carbonyl)-RMC-5552 is a highly effective mTOR inhibitor, exhibiting inhibitory effects on both mTORC1 and mTORC2 substrate phosphorylation. Specifically, it significantly suppresses the phosphorylation of p-P70S6K-(T389), p-4E-BP1-(T37/36), and p-AKT1/2/3-(S473) with pIC50 values > 9, >9 and 8~9, respectively.

CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR kinase, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively blocks both mTORC1 and mTORC2 signaling pathways.

WYE-687 dihydrochloride is an ATP-competitive inhibitor of mTOR, demonstrating potent activity with an IC 50 value of 7 nM. It effectively suppresses the activation of both mTORC1 and mTORC2. Additionally, WYE-687 exhibits inhibitory effects on PI3Kα and PI3Kγ, with IC 50 values of 81 nM and 3.11 μM, respectively.

WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1 pS6K(T389) and mTORC2 P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).