Cathepsin Inhibitor

TS-24 is an inhibitor for cathepsin S, with an IC₅₀ of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis.

CTSD Human Pre-designed siRNA Set A contains three designed siRNAs for CTSD gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

MPI8 (TG0205221) TFA is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 TFA exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). MPI8 TFA can be used in clinical studies of COVID-19.

MIV-247 is a selective cathepsin S inhibitor with K_is of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.

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.

SSAA09E1 is a cathepsin L blocker (IC₅₀: 5.33 μM).SSAA09E1 inhibits stages of viral entry. SSAA09E1 can be used for SARS-CoV infection research

Z-Phe-Phe-Diazomethylketone is a selective inhibitor of cathepsin L.

Dual Cathepsin L/JAK-IN-1 (Compound A8) is a dual inhibitor of Cathepsin L (CTSL) and JAK, with IC₅₀ values of 0.68 μM, 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for CTSL, JAK1/2/3, and TYK2, respectively. Dual Cathepsin L/JAK-IN-1 effectively blocks the activation of the MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. Dual Cathepsin L/JAK-IN-1 can be used in research on acute lung injury (ALI).

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.

Cathepsin L-IN-5 (D6-3) is a potent Cathepsin L (CatL) inhibitor with an IC₅₀ of 0.27 nM. Cathepsin L-IN-5 effectively blocks the CatL function and substantially hinders the entry of the SARS-CoV-2 pseudovirus to cells by inhibiting the cleavage of the spike protein. Cathepsin L-IN-5 can be utilized in SARS-CoV-2 research.

CTSL Human Pre-designed siRNA Set A contains three designed siRNAs for CTSL gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Asperphenamate (Standard) is the analytical standard of Asperphenamate. This product is intended for research and analytical applications. Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively[1][2].

Leupeptin is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin can be used in research on chronic inflammatory diseases and skin tumorigenesis.

Mesaconic acid (Standard) is the analytical standard of Mesaconic acid. This product is intended for research and analytical applications. Mesaconic acid (Citronic acid; Methylfumaric acid) is an orally active anti-inflammatory and antioxidant agent. Mesaconic acid reduces the level of NF-κB in colon tissues, downregulates the expression of Keap1 and Bax, upregulates the expression of Nrf2 and Bcl2, and decreases the expression of Caspase-1. Mesaconic acid reduces the levels of NLRP3, ASC and Casp-1 in colon, liver and kidney tissues. Mesaconic acid reduces pro-inflammatory cytokine levels, increases the level of the anti-inflammatory cytokine IL-10, elevates NAD⁺ levels, regulates oxidative stress markers and antioxidant enzyme levels, and upregulates intestinal barrier proteins in colon, liver and kidney tissues. Mesaconic acid increases the abundance of beneficial gut bacteria and reduces the abundance of harmful gut bacteria in rapidly aging mice, and exhibits anti-aging properties. Mesaconic acid acts as a flame retardant and serves as a competitive inhibitor of fumarate reduction. Mesaconic acid can be used in the research of aging-related inflammation.

(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. (S,S)-Z-FA-FMK blocks LPS-induced production of IL-1α and IL-1β. (S,S)-Z-FA-FMK can be used as a negative control for caspase-1 and caspase-2 inhibitors because it lacks an aspartic acid residue at the P1 position.

Cathepsin Inhibitor 4 (Compound 45) is a selective inhibitor for Cathepsin S with K_i of 0.04 nM.

TSC25 is a potent cruzipain (CZP) inhibitor, with an IC₅₀ of 3.34 nM and a pIC₅₀ of 8.48.

3-Epiursolic Acid (Standard) is the analytical standard of 3-Epiursolic Acid (HY-N4289). This product is intended for research and analytical applications. 3-Epiursolic Acid is a natural triterpenoid and a competitive inhibitor of Cathepsin L, with an IC₅₀ of 6.5 μM and a K_i of 19.5 μM. 3-Epiursolic Acid acts through competitive inhibition of Cathepsin L. 3-Epiursolic Acid can be used in research on Cathepsin L inhibitors and tumor-associated proteases.

NCO-700 is a dual cathepsin B and calcium-activated neutral protease (CANP) inhibitor with IC₅₀ values of 0.8 and 46 μM, respectively. NCO-700 reduces the degradation of myocardial fibrin by inhibiting protease activity. NCO-700 also has inhibitory effects on hormone-independent tumor cells, such as prostate cancer cells, and induces apoptosis. NCO-700 can be used to study myocardial ischemia and refractory hormone-independent tumors.

CTSC-IN-1 (B22) is a CTSC inhibitor. CTSC-IN-1 inhibits CTSC activity by binding to S2 pocket and S1 site. CTSC-IN-1 can be used in the study inflammatory bowel disease.