Proteasome Inhibitor

BSc2118 is a 20S proteasome inhibitor with an IC₅₀ of approximately 50 nM. BSc2118 induces G₂/M phase cell cycle arrest and apoptosis in myeloma cells, inhibits cytoprotective autophagy, and suppresses tumor angiogenesis. BSc2118 reduces MMP9 activity, promotes angioneurogenesis, and alleviates recombinant tissue-type plasminogen activator-induced cerebral toxicity. BSc2118 is applicable to studies related to cerebral ischemia and multiple myeloma.

LMP7/LMP2-IN-1 (Compound 19) is the orally active inhibitor for immunoproteasome subunits LMP7 and LMP2 with IC₅₀ of 257 and 10 nM. LMP7/LMP2-IN-1 reduces the generation of antibody, downregulates the cells in spleen germinal center B and in plasma in NP-OVA-immunized mice, and can be used in research about autoimmune diseases.

Immunoproteasome-IN-2 is selective immunoproteasome inhibitor with IC₅₀ = 232.3 nM for LMP7, IC₅₀ = 9384.9 nM for β5. Immunoproteasome-IN-2 exhibits ancillary inhibitory activity against LMP2 and MECL-1 subunits. Immunoproteasome-IN-2 demonstrates anti-inflammatory efficacy in a mouse model of arthritis and shows a favorable safety profile in toxicological studies with reduced hepatotoxicity and hematotoxicity. Immunoproteasome-IN-2 has LMP7/β5 selectivity directly correlated with lower systemic toxicity. Immunoproteasome-IN-2 can be employed for research in arthritis.

N-Acetyl-L-leucyl-L-leucyl-L-methional is a Calpain II inhibitor with an IC₅₀ of 0.24 μM against porcine Calpain II. N-Acetyl-L-leucyl-L-leucyl-L-methional forms a stable tetrahedral adduct with the thiol group at the active site of Calpain II, thereby inhibiting proteolytic activity. N-Acetyl-L-leucyl-L-leucyl-L-methionally inhibits cathepsins in a non-selective manner. N-Acetyl-L-leucyl-L-leucyl-L-methional reduces SARS-CoV-2 infection levels in human coronary artery endothelial cells in vitro. N-Acetyl-L-leucyl-L-leucyl-L-methional can be used in research related to cataracts and coronavirus infections.

Phepropeptin B, a microbial secondary metabolite, is a proteasome inhibitor with an IC₅₀ of 11 μg/mL.

M3258 (Standard) is the analytical standard of M3258 (HY-111790). This product is intended for research and analytical applications. M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC₅₀=3.6 nM) and cellular (IC₅₀=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells.

(Rac)-PD 151746 is the optically inactive racemate of PD 151746 (HY-19749). PD 151746 is a neuroprotective calpain inhibitor with Ki values of 0.26 μM (u-calpain) and 5.33 μM (m-calpain), respectively.

β5i-IN-1 is a potent and selective inhibitor of β5i with a IC₅₀ of 8.463 nM. β5i-IN-1 releases TNF-α and IL-6 and influences the transcriptional activity of NF-κB. β5i-IN-1 can be used in study idiopathic pulmonary fibrosis.

Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. 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.

Cerpegin, a pyridinone-fused c-lactone, is an inhibitor of 20S proteasome. Cerpegin can be used as a tranquillizer, anti-inflammatory, analgesic and antiulcer.

Carmaphycin-17 (CP-17) is a selective 20S proteasome inhibitor with an EC₅₀ of 217 ?nM. Carmaphycin-17 has potent antimicrobial activity against Trichomonas vaginalis. Carmaphycin-17 overcomes Metronidazole (HY-B0318) resistance and significantly reduces parasite burden upon topical treatment without any apparent adverse effects in vaginal trichomonad infection mice model. Carmaphycin-17 can be used for sexually transmitted disease like trichomoniasis research.

TDI6245 is a Aurora kinase A (AURKA) inhibitor with an IC₅₀ value of 21.64 nM against AURKA. TDI6245 also inhibits the β5 subunit of the 20S proteasome from Plasmodium falciparum (Pf 20S), with IC₅₀ values of 0.11 μM, 31.1 μM and 6.8 μM against Pf 20S β5, human constitutive proteasome β5c and human immunoproteasome β5i subunits, respectively. TDI6245 binds to the AURKA pocket and the substrate cleft of Pf 20S β5 via antiparallel β-sheets and hydrogen bonds. TDI6245 inhibits the growth of Plasmodium falciparum. TDI6245 can be used in research related to triple-negative breast cancer and malaria.

Phepropeptin D, a microbial secondary metabolite, is a proteasome inhibitor with an IC₅₀ of 7.8 μg/mL.

Bepridil hydrochloride (Standard) (CERM 1978 (Standard);Org 5730 hydrochloride (Standard)) is the analytical standard of Bepridil hydrochloride (HY-103315). This product is intended for research and analytical applications. Bepridil hydrochloride is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

Aloin (mixture of A&B) (Standard) is the analytical standard of Aloin (mixture of A&B) (HY-N6013). This product is intended for research and analytical applications. Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticum collagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma.

Ixazomib (Standard) is the analytical standard of Ixazomib. This product is intended for research and analytical applications. Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC₅₀ of 3.4 nM (K_i of 0.93 nM).

Gabexate (mesylate) (Standard) is the analytical standard of Gabexate (mesylate). This product is intended for research and analytical applications. Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation.

4'-Hydroxychalcone (Standard) is the analytical standard of 4'-Hydroxychalcone (HY-N7056). This product is intended for research and analytical applications. 4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.

Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity.

Bepridil-d₅ hydrochloride (CERM 1978-d₅; Org 5730-d₅ hydrochloride) is the deuterated-labeled Bepridil hydrochloride (HY-103315). Bepridil hydrochloride (CERM 1978; Org 5730 hydrochloride) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.