Review Article

Recent Advances in ADAM17 Research: A Promising Target for Cancer and Inflammation

Table 1

Summary of biochemical selectivity testing of ADAM17 inhibitors against a panel zinc of metalloproteases. Synthetic substrates were used for all assays. All results are IC50, μM.

LeadMMP1MMP2MMP8MMP9MMP12MMP14ADAM33ADAM9ADAM10ADAM17

Number 17 [136]NTNT>100NTNT>100NTNT>1004.2
Number 19 [136]NT>100>100>100NT>100NTNT>1004.3
KP-457 [135]>1000.722.25.4NT2.14NTNT0.750.011
INCB3619 [18]>0.50.045NT0.3NT0.81.03>50.0220.014
Complex I [139]NTNTNTNTNTNTNTNTNT11
MEDI3622 [147]NTNTNTNT>10NTNTNT>100.0031
D1(A12) [140]NTNTNTNTNTNTNTNT>10.0045
D8 [143]NTNTNTNTNTNTNTNTNT0.0012
4mut [19, 152]NTNTNT>1.0NT>1.0NTNTNT0.1

NT: not tested.