mTORC1 Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
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; mTORC1, IC50: 8 nM|
|S2658||Omipalisib (GSK2126458, GSK458)||
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, respectively. Phase 1.
|Pan||mTORC1, Ki: 0.18 nM|
Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM; exhibits 1000-fold selectivity for mTOR than PI3K.
|Pan||mTORC1, IC50: 2 nM|
KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM; no effect on PI3Ks.
|Pan||mTORC1, IC50: ~10 nM|
OSI-027 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.
|Pan||mTORC1, IC50: 22 nM|
|S2238||Palomid 529 (P529)||
Palomid 529 (P529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS6 but no effect observed on pMAPK or pAktT308. Phase 1.
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