mTORC1 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S7035 XL388

XL388 is a highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases.

Selective mTORC1, IC50: 8 nM
S1627 Nitazoxanide (NSC 697855)

Nitazoxanide (NTZ, NSC 697855) is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). Nitazoxanide modulates autophagy and inhibits mTORC1 signaling.

Selective
S2658 Omipalisib (GSK2126458)

Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1.

Pan mTORC1, Ki: 0.18 nM
S2827 Torin 1

Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.

Pan mTORC1, IC50: 2 nM
S1226 KU-0063794

KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM in cell-free assays; no effect on PI3Ks.

Pan mTORC1, IC50: ~10 nM
S2624 OSI-027

OSI-027 (ASP4786, CERC 006, AEVI-006) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. OSI-027 induces autophagy in cancer cells. Phase 1.

Pan mTORC1, IC50: 22 nM
S8784 PQR620

PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. PQR620 has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure.

Pan TORC1, IC50: 250 nM
S2238 Palomid 529 (P529)

Palomid 529 (P529, SG 00529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS6. Phase 1.

Pan