ADAMs

(S,S)-TAPI-0 is an inhibitor of TACE (IC50 = 50-100 nM) as well as other matrix and membrane metalloproteases

TAPI-2 is an inhibitor of TACE, ADAMs, ACE secretase, and other MMPs (metalloproteinases). TAPI-2 blocks release of DCC7, APP, TNFα, L-selectin, NOTCH, TGFα, IL-6R9, erbB2/HER2, and ACE. This inhibitor has been used in tissue culture.

TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors.

GI 254023X is a selective ADAM10 metalloprotease inhibitor; displays over 100-fold higher potency at ADAM10 compared to ADAM17.

TMI-1 is a novel orally active dual inhibitor of ADAM17 (TACE) and MMP.

KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.

GW280264X is an ADAM17 inhibitor.

JG26 is a potent ADAM inhibitor with IC50 values of 12 nM for ADAM8, 1.9 nM for ADAM17, and 150 nM for ADAM10. It also inhibits MMP-12 with an IC50 of 9.4 nM. JG26 suppresses AngII-induced EGFR transactivation and ERK activation, upregulates ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. Additionally, JG26 demonstrates anti-metastatic effects in colorectal cancer and holds research potential in Hodgkin lymphoma and vascular diseases.

(R)-TAPI-2 is a potent inhibitor targeting matrix metalloproteinases (MMPs), tumor necrosis factor alpha-converting enzyme (TACE), and a disintegrin and metalloproteinase (ADAM), exhibiting an IC50 value of 20 μM for MMP activity. This compound is utilized in research focused on inflammation, cancer progression, and cell signaling due to its ability to modulate proteolytic processes. Additionally, (R)-TAPI-2 has demonstrated efficacy in preventing viral entry, specifically in the context of SARS-CoV infections, making it valuable for virology studies.