mtor inhibitor 2

mTOR inhibitor-2 is an inhibitor of selective and oral mTOR (IC50 of 7 nM).

2H-Imidazo[4,5-b]pyrazin-2-one, 1,3-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-1-[(tetrahydro-2H-pyran-4-yl)methyl]- is a potent mTOR inhibitor with IC50 of 0.176 μM and >30 μM for mTOR and PI3Kα, respectively.

PI3K mTOR Inhibitor-2 is a potent pan inhibitor of PI3K and mTOR with IC50s of 3.4, 34, 16.1, and 4.7 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively. PI3K mTOR Inhibitor-2 demonstrates antitumor activity.

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

PKI-402 is a potent PI3K and mTOR inhibitor. PKI-402 inhibits PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ with IC50s of 2, 3, 7, 14 and 16 nM, respectively.

PI3K Akt mTOR-IN-2 is a potent PI3K AKT mTOR inhibitor with anticancer effects and selectivity for MDA-MB-231 cells (IC50 2.29 μM). It induces cell cycle arrest and apoptosis in cancer cells.

mTOR HDAC-IN-1 (Compound 50) is a dual inhibitor of mTOR and HDAC, with IC50 values of 0.49 nM and 0.91 nM, respectively, holding potential as an anti-cancer agent [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).

mTOR inhibitor 9a inhibited the growth of human LNCap cells with an ic50 of 80 nm. 1-methyl-3 -{4-[4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)thieno[3,2-d]pyrimidin-2-yl]phenyl}urea may have antitumor activity.

mTOR inhibitor 11 is a useful organic compound for research related to life sciences. The catalog number is T9309 and the CAS number is 1195785-35-3.

mTOR inhibitor 13 is a selective mTOR inhibitor with IC50 of 0.29nM and 119nM for mTOR and PI3Kα, respectively.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).

Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα).

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.

Sapanisertib (INK 128) is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.

Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.

Ch282-5, an orally active inhibitor targeting the Bcl-2 protein, promotes mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. It demonstrates antiproliferative effects on colorectal cancer cells, effective both in vitro and in vivo, while also inhibiting metastasis. Further, Ch282-5 augments Oxaliplatin-induced autophagy (Autophagy) by downregulating Mcl-1 protein and raising platelet count, which helps mitigate the adverse effects of Navitoclax.

AKT-IN-25 (Compound 14a) is an inhibitor of Akt that prevents the phosphorylation of Akt, thereby hindering the PI3K Akt mTOR signaling pathway. It arrests the cell cycle at the G1 phase, inhibits the migration of PANC-1 cells, and suppresses the proliferation of cancer cells PANC-1, PATU-T, and SUIT-2, with IC50 values of 3.05, 1.32, and 3.85 μM, respectively.

Topo I II-IN-2 (Compound 3g) is an inhibitor of both Topo I and Topo II. It exhibits inhibitory activity against NCI-H446 and NCI-H1048 cells with IC50 values of 1.30 μM and 1.42 μM, respectively. Topo I II-IN-2 induces mitochondrial apoptosis, disrupts mitochondrial function, and stimulates activity generation. Additionally, it inhibits the PI3K Akt mTOR pathway, effectively preventing the proliferation, invasion, and migration of small cell lung cancer (SCLC) cells in vitro.

SKLB-D18 is a potent and selective inhibitor of ERK1/2 and ERK5, with IC50 values of 38.69, 40.12, and 59.72 nM, respectively. It also serves as an autophagy agonist, influencing mTOR/p70S6K and NCOA4-mediated ferroptosis, potentially mitigating multidrug resistance. SKLB-D18 demonstrates significantly superior efficacy against triple-negative breast cancer (TNBC) in both in vitro and in vivo studies.

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.