RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
Anticancer agent 82 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Anticancer agent 82 shows better oral bioavailability and pharmacokinetic profiles than FiVe1[1].
20S Proteasome-IN-3 is a 20S proteasome β5 subunit inhibitor (IC50=1.64 μM)[1][2]. 20S Proteasome-IN-3 shows anti-tumor proliferation activity[2].
TCH-165 is a specific small molecule modulator of proteasome assembly, regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation; enhances the degradation of both α-syn and tau, does not induce the degradation of GAPDH, enhances the degradation of intrinsically disordered proteins in cell culture; display a decrease in assembled 26S and an increase in 20S proteasome in treated cells.
Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome. Ac-Nle-Pro-Nle-Asp-AMC can be used for the 26S proteasome caspase-like activity analysis[1][2][3].
MUN57694 is 26S proteasome inhibitor. MUN57694 was reported in WO 2006128196. This product has not formal name. For the convenience of scientific communication, we named it by combining its Inchi key (3 letters from the first letter of each section) with the last 5 digits of its CAS number or its molecule weight if its CAS number is not available
Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract[1].
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β[1].
Z-LLY-FMK (Calpain Inhibitor IV) is a calpain inhibitor, involved in apoptosis of many cell systems. Z-LLY-FMK inhibits the intestine apoptosis after common bile duct ligation[1].
VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).IC50 value: 1 nM (trypsin-like proteasome), 50-100 nM(chymotrypsin-like proteasome), 3 μM (caspase-like proteasome)Target: proteasomein vitro: VR23 is a novel proteasome inhibitor targeting β2 of the 20S proteasome subunit. VR23 produces a synergistic effect in killing multiple myeloma cells, including those that were resistant to bortezomib. VR23 as a structurally novel proteasome inhibitor with desirable properties as an anticancer agent.in vivo: VR23 shows effective antitumor and antiangiogenic activities in mice.
FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM.
MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis[1][2][3].
Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor, with IC50s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for research of venous thromboembolism[1].
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis[1][2][3].
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with a Ki of 0.6 nM.
Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. PTP1B-IN-9 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. PTP1B-IN-9 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity[1].
Suc-Gly-Gly-Phe-pNA is the chymotrypsin substrate with an Km value of 1.6 mM[1][2].
RTS-V5 is a dual HDAC/proteasome inhibitor with IC50s of 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
Isovalerylcarnitine-d9 (chloride) is the deuterium labeled Isovalerylcarnitine (chloride)[1]. Isovalerylcarnitine chloride, a product of the catabolism of L-leucine, is a potent activator of the Ca2+-dependent proteinase (calpain) of human neutrophils[2].
Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.IC50 value: 36 nM/82 nM(20S proteasome β5/LMP7) [1]Target: 20S proteasomeThe anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP, as well as inhibition of migration of MM cells and angiogenesis. Oprozomib is demonstrated an absolute bioavailability of up to 39% in rodents and dogs. It is well tolerated with repeated oral administration at doses resulting in >80% proteasome inhibition in most tissues and elicited an antitumor response in multiple human tumor xenograft and mouse syngeneic models.
UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey[1]. UK-101 induces cell apoptosis and can be used for the study of prostate cancer[2].
LMP7-IN-1, a Boronic acid derivative, is a potent and selective immunoproteasome subunit LMP7 (β5i) inhibitor with an IC50 of 1.83 nM (WO2021143923A1; compound 20)[1].
DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation[1].
Ac-ANW-AMC is a fluorogenic substrate for immunoproteasome. Ac-ANW-AMC can be used to measure β5i activity (Ex=345 nm, Em=445 nm)[1][2].
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate[1].
PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor (Ki values for ν and m-calpains are 0.21 and 0.37 μM respectively).target:calpain[1]In vitro: PD150606 also against tetrafluoroethyl-l-cysteine-, bromohydroquinone-, oxidant (t-butylhydroperoxide)- and calcium ionophore (ionomycin)-induced cell death. PD150606 inhibits calpains by binding to the calcium-binding domain of the enzyme. [2] high specificity for calpains relative to other proteases, uncompetitive inhibition with respect to substrate.[3]
MG-262 is a reversible proteasome inhibitor with diverse biological activities[1][2][3].
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research[1].
KZR-504 is a highly selective and orally active inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively.