Insulin-Receptor Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S2703 GSK1838705A

GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.

Selective Insulin Receptor, IC50: 1.6 nM
S1124 BMS-754807

BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.

Selective Insulin Receptor, IC50: 1.7 nM
S1093 GSK1904529A

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.

Selective Insulin Receptor, IC50: 25 nM
S1012 BMS-536924

BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.

Selective Insulin Receptor, IC50: 73 nM
S1091 OSI-906 (Linsitinib)

OSI-906 (Linsitinib) is a selective inhibitor of IGF-1R with IC50 of 35 nM; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.

Selective Insulin Receptor, IC50: 75 nM
S1034 NVP-AEW541

NVP-AEW541 is a potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM, greater potency and selectivity for IGF-1R in a cell-based assay.

Selective Insulin Receptor, IC50: 0.14 μM
S1234 AG-1024

AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).

Selective Insulin Receptor, IC50: 57 μM