human cathepsin l

SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).

Acetyl-Calpastatin (184-210)(human) acetate is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively.

VK13 (Compound 6) is a potent inhibitor of human cathepsin L (hCatL) and SARS-CoV-2 3CLpro (3CL-PR), with Ki values of 2.6 nM and 0.55 nM, respectively. It also exhibits activity against CoV-2, with an EC50 value of 1.25 μM.

FGA145 is a dual inhibitor of Mpro and human Cathepsin L, with Ki values of 3.71 μM for Mal-Mpro, 9.82 μM for pET21-Mpro, and 53 nM for Cathepsin L. Additionally, FGA145 exhibits multi-target antiviral activity.

FGA146 is a selective inhibitor of Mpro and human Cathepsin L, with Ki values of 2.19 μM for Mal-Mpro, 0.96 μM for pET21-Mpro, and 0.87 μM for Cathepsin L. It exhibits antiviral activity against SARS-CoV-2.

Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V, exhibiting high affinity with Ki values of 41 pM, 68 pM, and 53 pM, respectively. It effectively inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. In vitro studies confirm its inhibitory effect on bone resorption in human tissue, and in vivo studies on cynomolgus monkeys validate its efficacy in reducing bone resorption.

SID 26681509 quarterhydrate is a reversible, potent, selective, competitive inhibitor of human cathepsin L (IC50: 56 nM). SID 26681509 inhibits in vitro propagation of Plasmodium falciparum (IC50: 15.4 μM) and inhibits Leishmania major (IC50: 12.5 μM) and does not inhibit histone G activity.

Thiocarbazate, also known as CID16725315, is an inhibitor of human cathepsin L. Inhibition of cathepsin L thus holds promise for therapeutic intervention for both SARS-CoV and Ebola virus infection. With respect to the development of antiviral agents, inhibitors of human cathepsin L are not subject to resistance because of rapid mutations of the viral genome. Cathepsin L is therefore an attractive target for drug development.

Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. In the cathepsin L inhibition assay, The oxocarbazate caused a time-dependent 17-fold drop in IC50 from 6.9 nM (no preincubation) to 0.4 nM (4-h preincubation). Slowly reversible inhibition was demonstrated in a dilution assay. CID23631927 demonstrate activity in blocking both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into human embryonic. CID 23631927 was a subnanomolar, slow-binding, reversible inhibitor of human cathepsin L that blocked SARS-CoV and Ebola pseudotype virus entry in human cells. Inhibition of cathepsin L thus holds promise for therapeutic intervention for both SARS-CoV and Ebola virus infection.

SPR39, a potent inhibitor of the SARS-CoV-2 main protease (Mpro), demonstrates inhibitory Ki values of 0.252 µM for SARS-CoV-2 Mpro, and 3.38 and 7.88 µM for human Cathepsin L (hCatL) and human Cathepsin B (hCatB) respectively. It exhibits antiviral properties and cytotoxicity.

SPR38, a potent inhibitor of the SARS-CoV-2 main protease, exhibits a Ki value of 0.260 μM. Additionally, it effectively inhibits human cathepsin L (hCatL) and human cathepsin B (hCatB), displaying Ki values of 1.92 μM and 11.1 μM, respectively.

Acetyl-Calpastatin(184-210)(human) TFA, a potent, selective, and reversible calpain inhibitor, has Ki values of 0.2 nM for µ-calpain and 6 μM for cathepsin L, indicating high specificity and efficacy in enzyme inhibition [1] [2].

Olgotrelvir sodium, an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L), effectively inhibits both the replication of SARS-CoV-2 and its entry into host cells [1].