proteolytic

MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.

AU-15330 is a proteolytic targeting chimera (PROTAC) that simultaneously targets SMARCA4, SMARCA2, and PBRM1 for degradation and exhibits cytotoxicity in H3.3K27M cells but not in H3 wild-type cells. [2]

CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5. It inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM. CSN5i-3 has a killing effect on a variety of cancer cells and can be used as an anticancer drug. [2]

Pronase E is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.

Hydrocortisone (Cortisol) is a glucocorticoid hormone secreted by the adrenocortex. Hydrocortisone agonizes the glucocorticoid receptor, which promotes proteolytic metabolism, gluconeogenesis, capillary wall stabilization, and renal calcium excretion, as well as suppressing immune and inflammatory responses.

Compstatin is a cyclic peptide consisting of 13 amino acid residues and is a potent inhibitor of complement system C3. Compstatin is species-specific and has inhibitory effects only on the complement system of primates. Studies have shown that it can bind to baboon C3 and is resistant to proteolytic cleavage in baboon blood. Its IC50 values for the classical pathway and alternative pathway are 63 μM and 12 μM, respectively.

MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM ). The biologically active form of MLN9708 (Ixazomib Citrate) is MLN2238 in aqueous solutions or plasma.

PI-1840(IC50 = 27 nM)is a reversible and selective chymotrypsin-like (CT-L) inhibitor, with little proteasome proteolytic effects on trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).

Ixazomib (MLN2238) , a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50 Ki: 3.4 0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31 3500 nM).

Z-Arg(Z)2-OH can be used in the assay to screen proteolytic activities in mite homogenates.

γ-Glu-Phe TFA(7432-24-8 free base) is a dipeptide composed of gamma-glutamate and phenylalanine and is a proteolytic breakdown product of larger proteins. It is probably formed by transpeptidation between glutathione and the corresponding amino acid, catalyzed by gamma-glutamyl transpeptidase.

ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).

CAY10406 is a trifluoromethyl analog of an isatin sulfonamide compound that selectively inhibits caspases 3 and 7. The non-trifluoromethyl compound exhibits Ki values of 1.2 nM and 6 nM for caspases 3 and 7, respectively. For all of the other caspases tested, it is 100 to 1,000 times less potent. Caspases 3 and 7 are 'effector caspases' that are downstream from the initiating steps of apoptosis, and are implicated in the main proteolytic processing of the apoptotic signal. No data is currently available for caspase inhibition by CAY10406.

Ac-ESMD-CHO functions as an inhibitor of both caspase-3 and caspase-7, specifically obstructing the proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site [1] [2].

MI-1851 is a potent peptidomimetic inhibitor. MI-1851could prevent proteolytic processing of the S protein from SARSCoV-2 by endogenous furin in HEK293 cells.

Skp2 inhibitor 2 (14f) impedes the F-box protein S-phase kinase-associated protein 2 (Skp2), demonstrating an IC50 of 10.2 μM against Skp2-Cks1. This compound targets Skp2, a component of cullin-RING ligases that recruits and ubiquitinates substrates, playing roles in both proteolytic and non-proteolytic processes [1].

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 μM), showing no effect on PAR-2, PAR-3, or PAR-4. It inhibits the aggregation of human platelets induced by SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), with high selectivity relative to U46619. RWJ-56110 dihydrochloride also blocks angiogenesis and the formation of new vessels in vivo, and induces cell apoptosis[1][2].

Leucylproline is a peptide that proteolytic breakdown product by larger proteins.

Substance P (1-7) 2TFA(68060-49-1(free base)) is the major bioactive metabolite formed after proteolytic degradation of the tachykinin substance P (SP),with anti-inflammatory, anti-nociceptive and anti-hyperalgesic effects

GTPγS tetralithium (Guanosine 5'-[γ-thio]triphosphate tetralithium) is a G-protein activator, a non-hydrolyzable GTP analog that protects proteins from proteolytic degradation.GTPγS tetralithium is involved in the detection of cells expressing recombinant receptors and endogenous receptors. GTPγS tetralithium is involved in the detection of GPCR signaling in cells expressing recombinant receptors as well as in cells and tissues expressing endogenous receptors, and can be assayed to measure agonist-induced desensitization of two human polymorphic α2B-adrenoceptor variants.

Bradykinin (1-5) is a major stable metabolite of Bradykinin, formed by the proteolytic action of angiotensin-converting enzyme (ACE). The Bradykinin (BK) fragment (1-5) (RPPGF) is one of the most stable naturally occurring metabolites and may be used as a marker for BK production in vivo.

γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is the substrate of CRF21 [gamma-Glutamylcyclotransferase (GGCT)].

AD4, an artemisinin derivative functioning as a proteolytic targeting chimera (PROTAC) for PCLAF, effectively degrades PCLAF in RS4;11 cells with an IC50 of 0.6 nM. This degradation activates the p21 Rb axis, resulting in antitumor activity. Furthermore, AD4 has been demonstrated to prolong survival in NOD SCID mice transplanted with RS4;11 cells, showcasing its in vivo efficacy [1].

Compstatin TFA, a potent inhibitor of the complement system C3 characterized by species specificity, is a 13-residue cyclic peptide. It selectively binds to baboon C3 and demonstrates resistance to proteolytic cleavage in baboon blood (similar to humans), effectively inhibiting the activation of the primate complement system. Notably, Compstatin TFA exhibits IC 50 values of 63 μM and 12 μM for the classical and alternative complement pathways, respectively [1] [2] [3].