INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases [1]. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inh
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Serine/threonine-protein kinase mTOR inhibitor
Product Description
INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). A potent and selective TORC1/2 inhibitor
1.Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. (2009) mTOR Mediated Anti-Cancer Drug Discovery.. Drug Discov Today Ther Strateg, 6 (2):(47-55). [PMID:20622997][10.1021/op500134e]
2.Schenone S, Brullo C, Musumeci F, Radi M, Botta M. (2011) ATP-competitive inhibitors of mTOR: an update.. Curr Med Chem, 18 (20):(2995-3014). [PMID:21651476][10.1021/op500134e]
3.Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, Shi EY, Stumpf CR, Christensen C, Bonham MJ et al.. (2012) The translational landscape of mTOR signalling steers cancer initiation and metastasis.. Nature, 485 (7396):(55-61). [PMID:22367541][10.1021/op500134e]
4.Arendse LB, Murithi JM, Qahash T, Pasaje CFA, Godoy LC, Dey S, Gibhard L, Ghidelli-Disse S, Drewes G, Bantscheff M et al.. (2022) The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages.. Sci Transl Med, 14 (667):(eabo7219). [PMID:36260689][10.1021/op500134e]
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