Cathepsin Inhibitor

Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC₅₀: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC₅₀: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC₅₀: 50 nM).

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.

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

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].

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.

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

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.

SARS-CoV-2 3CLpro-IN-22 (Compound 17) is a cathepsin L (CTSL ) inhibitor with an IC₅₀ value of 32.5 nM. SARS-CoV-2 3CLpro-IN-22 can be used for the study of SARS-CoV-2 virus.

Cathepsin K inhibitor 7 (compound 7) is a Cathepsin K inhibitor with the pK_i of 7.3 aganist CatK. Cathepsin K inhibitor 7 can be used for study of osteoporosis.

MK 1256 is a highly selective and orally active inhibitor of tissue protease K (Cat K) with an IC₅₀ of 0.62 nM. MK 1256 shows extremely high selectivity towards other tissue proteases (all > 1100 times), with only a slightly lower selectivity for tissue protease F (Cat F) (110 times). MK 1256 exhibits strong anti-bone resorption activity in the osteoporosis model of rhesus monkeys with ovariectomy. MK 1256 can be used for research on osteoporosis.

Z-Arg-Lys-AOMK is a cathepsin B inhibitor that can cross the blood-brain barrier. Z-Arg-Lys-AOMK reduces cytosolic cathepsin B activity in homogenates of mouse cerebral cortex and hippocampal tissues, and alleviates motor dysfunction associated with CCI-TBI. Z-Arg-Lys-AOMK can be used in the research of traumatic brain injury.

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

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

SH491 (Compound 33) is an antiosteoporosis agent. SH491 inhibits RANKL-induced osteoclast differentiation on bone-marrow-derived monocytes (BMMs) (IC₅₀: 11.8 nM). SH491 inhibits the expression of osteoclastogenesis-related marker genes (TRAP, CTSK, MMP-9, and ATPase v0d2) and proteins (TRAP, CTSK, MMP-9).

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78).

Z-FK-ck (Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone) is a potent and selective gingipain-K-specific inhibitor. Z-FK-ck prolongs plasma thrombin time (TT) in a dose- and time-dependent manner.