Cathepsin B Inhibitor

CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.

CA-074 is a potent inhibitor of cathepsin B with a K_i of 2 to 5 nM.

Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC₅₀ values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis.

LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC₅₀ of 10 μM.

SNJ-1945 is an orally active, blood-brain barrier-penetrant Calpain inhibitor. SNJ-1945 inhibits Cathepsin L, Cathepsin B, and Ca²⁺ -independent proteases. SNJ-1945 suppresses ROS production and downregulates Cyclooxygenase-2 and Caspase-1. SNJ-1945 alleviates left ventricular systolic dysfunction, reduces cerebral ischemia-induced injury, and decreases the score of experimental autoimmune encephalomyelitis in mouse models. SNJ-1945 can be used in research related to post-cardiac arrest reperfusion injury, Parkinson's disease, multiple sclerosis, and proliferative retinopathy.

Cathepsin L-IN-7 is an inhibitor of cathepsin L, cathepsin B and cathepsin S. Cathepsin L-IN-7 has an IC₅₀ of 0.011 μM against cathepsin L and an IC₅₀ of 0.062 μM against cathepsin S, while it shows weak inhibitory activity against cathepsin B. Cathepsin L-IN-7 binds to the active site of cysteine proteases and blocks their proteolytic function. Cathepsin L-IN-7 can be used in research on viral infections and cancer.

Z-FA-FMK ((1S)-Z-FA-FMK) is a potent Cathepsin B and L inhibitor. Z-FA-FMK blocks the induction of DEVDase activity, DNA fragmentation, and externalization of phosphatidylserine by selective synthetic retinoid-related molecules (RRMs). Z-FA-FMK inhibits apoptosis. Z-FA-FMK inhibits caspase activity and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. Z-FA-FMK is a viral inhibitor. Z-FA-FMK inhibits reovirus replication in a susceptible host.

Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC₅₀=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis.

L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC₅₀ of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (K_i=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (K_i=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss.

3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC₅₀, 6.5 μM; K_i, 19.5 μM), with no obvious effect on cathepsin B.

L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC₅₀s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC₅₀ of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.

Cathepsin K inhibitor 6 (compound 19) is an inhibitor of cathepsin K (Cat K) with an IC₅₀ of 17 nM. Cathepsin K inhibitor 6 also has inhibitory effects on other isoforms, with IC₅₀s of 0.05 μM (Cat L) and 0.3 μM (Cat B), respectively.

Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC₅₀s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II.

Cathepsin L-IN-6 (Compound 6a) is a selective cathepsin L inhibitor with an IC₅₀ of 0.021 μM. Cathepsin L-IN-6 suppresses cathepsin L activity by directly binding to cathepsin L. Cathepsin L-IN-6 inhibits IL-6 and IL-8. Cathepsin L-IN-6 shows a high anti-inflammatory activity. Cathepsin L-IN-6 can be used in the research of acute lung injury.

Ac-VLPE-FMK, a tetrapeptidyl mono-fluoromethyl ketone (m-FMK), is a Cat-B and Cat-L inhibitor. Ac-VLPE-FMK can be used for the research of cancer aggressiveness.

SPR38 is a potent SARS-CoV-2 main protease inhibitor, with a K_i of 0.260 μM. SPR38 also inhibits hCatL and hCatB, with K_i values of 1.92 μM and 11.1 μM, respectively.

SmCB1-IN-1 (Compound 2h) is an inhibitor for S. mansoni cathepsin B1 (SmCB1) with an K_i of 0.05 μM. SmCB1-IN-1 exhibits selectivity toward human off-target cathepsins (29% and 37% inhibition for CatB and CatL at 20 μM). SmCB1-IN-1 inhibits 68% Schistosoma mansoni at 1 μM.

FGA145 is a dual, selective inhibitor for M^pro and human Cathepsin L, with K_is of 3.71 μM, 9.82 μM and 53 nM, for Mal-M^pro, pET21-M^pro and Cathepsin L, respectively. FGA145 reveals a multitarget effects in the antiviral activity.

AM4299B is an inhibitor for thiol protease. AM4299B inhibits bovine spleen cathepsin B, human kidney cathepsin L and papain with IC₅₀s of 0.7, 0.5 and 20 μM, respectively. AM4299B can be used in research in osteoporosis, and has potential to be used as an antiparasitic agent.