Cathepsin Inhibitor

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).

FGA146 is a dual, selective inhibitor for M^pro and human Cathepsin L, with K_is of 2.19 μM, 0.96 μM and 0.87 μM, for Mal-M^pro, pET21-M^pro and Cathepsin L, respectively. FGA146 reveals an antiviral activity against SARS-CoV-2.

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.

RKLLW-NH2 is a Cathepsin L inhibitor.

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 C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC₅₀ of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC₅₀ values of 203.4 and 177.6 nM, respectively.

Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a K_i of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.

CTSL/CAPN1-IN-2 (Compound 14b) is an orally active inhibitor of both CTSL and CAPN1, with IC₅₀ values of 6.88 nM and 347.6 nM, respectively. CTSL/CAPN1-IN-2 possesses anti-inflammatory properties and favorable pharmacokinetic characteristics. CTSL/CAPN1-IN-2 exhibits broad-spectrum antiviral activity against coronaviruses by blocking viral entry.

JNJ 10329670 is a potent and selective noncovalent cathepsin S inhibitor with a K_i value of 34 nM for human cathepsin S. JNJ 10329670 blocks invariant chain proteolysis in B cells and dendritic cells, as well as antigen-induced T cell proliferation.

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

Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC₅₀ value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies.

Gardenin B (Standard) is the analytical standard of Gardenin B (HY-N6037). This product is intended for research and analytical applications. Gardenin B is a flavonoid isolated from Gardenia jasminoides. Gardenin B is a methoxyflavone compound and an inhibitor of USP7, ODC (IC₅₀: 6.24 μg/mL), and Cathepsin D (IC₅₀: 5.61 μg/mL). Gardenin B exhibits antioxidant and antitumor activities. Gardenin B shows IC₅₀ values of 8.87 and 10.59 μg/mL for DPPH and NO scavenging, respectively, and also possesses ferric ion reducing ability. Additionally, Gardenin B can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. Gardenin B can be used in cancer research.

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