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Belongs to the AAA-type superfamily and, like EC 3.6.4.5 (minus-end-directed kinesin ATPase), is involved in channel gating and polypeptide unfolding before proteolysis in the proteasome. Six ATPase subunits are present in the regulatory particle (RP) of 26S proteasome. Group: Enzymes. Enzyme Commission Number: EC 3.6.4.8. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-4710; proteasome ATPase; EC 3.6.4.8. Cat No: EXWM-4710.
proteasome endopeptidase complex
A 20-S protein composed of 28 subunits arranged in four rings of seven. The outer rings are composed of α subunits, but the β subunits forming the inner rings are responsible for peptidase activity. In eukaryotic organisms there are up to seven different types of β subunits, three of which may carry the N-terminal threonine residues that are the nucleophiles in catalysis, and show different specificities. The molecule is barrel-shaped, and the active sites are on the inner surfaces. Terminal apertures restrict access of substrates to the active sites. There is evidence that catalytic subunits are replaced by others under some conditions so as to alter the spec...atalytic proteinase; proteasome organelle; alkaline protease; 26S protease; tricorn proteinase; tricorn protease. Enzyme Commission Number: EC 3.4.25.1. CAS No. 140879-24-9. Alkaline Protease. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-4374; proteasome endopeptidase complex; EC 3.4.25.1; 140879-24-9; ingensin; macropain; multicatalytic endopeptidase complex; prosome; multicatalytic proteinase (complex); MCP; proteasome; large multicatalytic protease; multicatalytic proteinase; proteasome organelle; alkaline protease; 26S protease; tricorn proteinase; tricorn protease. Cat No: EXWM-4374.
Proteasome inhibitor i. Uses: Designed for use in research and industrial production. Additional or Alternative Names: CARBOBENZOXY-L-ISOLEUCYL-GAMMA-T-BUTYL-L-GLUTAMYL-L-ALANYL-L-LEUCINAL;BENZYLOXYCARBONYL-L-ISOLEUCYL-[(2S)-2-AMINO-4-(T-BUTYLOXYCARBONYL)BUTANOYL]-L-ALANYL-L-LEUCINAL;PROTEASOME INHIBITOR I;PROTEASOME INHIBITOR I (ALDEHYDE);PROTEASOME INHIBITOR PSI;PSI;N-. Product Category: Heterocyclic Organic Compound. CAS No. 158442-41-2. Molecular formula: C32H50N4O8. Mole weight: 618.76. Purity: >90 %. Product ID: ACM158442412. Alfa Chemistry ISO 9001:2015 Certified.
Proteasome Inhibitor I
The Proteasome Inhibitor I controls the biological activity of Proteasome. This small molecule/inhibitor is primarily used for Protease Inhibitors applications. Group: Fluorescence/luminescence spectroscopy.
Proteasome Inhibitor II
The Proteasome Inhibitor II controls the biological activity of Proteasome. This small molecule/inhibitor is primarily used for Protease Inhibitors applications. Group: Fluorescence/luminescence spectroscopy.
Proteasome Inhibitor III
The Proteasome Inhibitor III controls the biological activity of Proteasome. This small molecule/inhibitor is primarily used for Protease Inhibitors applications. Group: Fluorescence/luminescence spectroscopy.
Proteasome Inhibitor IV
The Proteasome Inhibitor IV controls the biological activity of Proteasome. This small molecule/inhibitor is primarily used for Protease Inhibitors applications. Group: Fluorescence/luminescence spectroscopy.
Proteasome Inhibitor X, PI-083 - CAS 6298-15-3
The Proteasome Inhibitor X, PI-083, also referenced under CAS 6298-15-3, controls the biological activity of Proteasome. This small molecule/inhibitor is primarily used for Protease Inhibitors applications. Group: Fluorescence/luminescence spectroscopy.
Proteasome Inhibitor XX, GL5 - CAS 146304-91-8
The Proteasome Inhibitor XX, GL5, also referenced under CAS 146304-91-8, controls the biological activity of Proteasome. This small molecule/inhibitor is primarily used for Protease Inhibitors applications. Group: Fluorescence/luminescence spectroscopy.
A cell-permeable tetrapeptidyl sulfonyl fluoride -based irreversible proteasome inhibitor that selectively inhibits the hydrolysis of Suc-LLVY-AMC by the beta5 chymotrypsin-like activity (IC50 = 7nM using yeast 20S proteasome), while exhibiting much reduced potency against Z-LLE-AMC hydrolysis by the beta1 caspase-like activity or Z-LLR-AMC hydrolysis by the beta2 trypsin-like activity (29% and 75% inhibition, respectively, with 200uM inhibitor). One hour inhibitor treatment at 5uM in HEK cultures is shown to completely abolish beta5 labeling by the proteasome probe MV151, while only partial MV151 blockage is seen with beta1 and beta2 at an inhibitor concentration of 50uM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. Molecular Formula: C??H??FN?O?S. US Biological Life Sciences.
Proteasome Substrate III, Fluorogenic, is a substrate for proteasome. Also acts as a substrate for calpain, chymotrypsin, and ingensin. Group: Fluorescence/luminescence spectroscopy.
Proteasome Substrate VI, Fluorogenic - CAS 90468-18-1
A fluorogenic substrate probe useful for assaying trypsin-like activity of proteasome. Group: Fluorescence/luminescence spectroscopy.
20S Proteasome is a catalytic core enzyme of the 26S proteasome that degrades ubiquitinated proteins. Fully functional with Z-LLVY-AMC as the substrate. Group: Fluorescence/luminescence spectroscopy.
A cell-permeable flavone derivative that arrests the proliferation of acute myeloid leukemia cells (NB4, U937, HL-60, OCI AML3), in a dose and time-dependent manner (optimum at ~20uM and 96h) and blocks the colony formation in samples from acute myeloid leukemia patients, without affecting normal blood cells. Shown to reduce mitochondrial membrane potential and Bad phosphorylation (at Ser136), induce Bax and caspase 3, 8, and 9 activation in U937 cells. Does not affect the phosphorylation of Akt1, but significantly reduces the expression and phosphorylation of p70S6 kinase in U937 cells. Reported to inhibit the chymotrypsin-like activity of proteasome (IC50 = 2.0uM) and this effect is synergistic with bortezomib. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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1,3-Bis-(Z-Leu-Leu)-diaminoacetone
1,3-Bis-(Z-Leu-Leu)-diaminoacetone, a cysteine protease inhibitor, can specifically and efficiently inhibit the processing of p-Prl signal peptide (IC50 ca. 50 nM) without affecting the activity of signal peptidase and lysosomal cathepsin, proteasome, and other proteases. Synonyms: (Z-LL)2 Ketone; Z-Leu-Leu-NH-CH2-CO-CH2-NH-Leu-Leu-Z; 2,2'-(2-Oxo-1,3-propanediyl)bis[N-[(phenylmethoxy)carbonyl]-L-leucyl-L-leucinamide; 1,3-di-(N-carboxybenzoyl-leucyl-leucyl)aminoacetone; Dibenzyl [(4S,7S,15S,18S)-7,15-diisobutyl-2,20-dimethyl-5,8,11,14,17-pentaoxo-6,9,13,16-tetraazahenicosane-4,18-diyl]biscarbamate. Grades: ≥95%. CAS No. 313664-40-3. Molecular formula: C43H64N6O9. Mole weight: 809.00.
(1R,3S,4S)-tert-Butyl 3-(1H-Benzo[d]imidazol-2-yl)-2-azabicyclo[2. 2. 1]heptane-2-carboxylate can be obtained from (R)-(+)-α-Methylbenzylamine (M288800) which can be used as reactant/reagent in synthesis of urea-containing peptide boronic acids as proteasome inhibitors. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 2.5mg, 5mg. Molecular Formula: C18H23N3O2, Molecular Weight: 313.39. US Biological Life Sciences.
Worldwide
(1S)-3-Hydroxy Bortezomib
(1S)-3-Hydroxy Bortezomib is a metabolite of Bortezomib (B675700), the first proteasome inhibitor to be approved by the US FDA for multiple myeloma, a blood cancer. Bortezomib is a reversible inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 500ug, 5mg. Molecular Formula: C19H25BN4O5, Molecular Weight: 400.24. US Biological Life Sciences.
Worldwide
(1S)-3-Hydroxy Bortezomib-d8
(1S)-3-Hydroxy Bortezomib-d8 is labelled (1S)-3-Hydroxy Bortezomib (H818155) which is a metabolite of Bortezomib (B675700), the first proteasome inhibitor to be approved by the US FDA for multiple myeloma, a blood cancer. Bortezomib is a reversible inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 10mg. Molecular Formula: C19H17D8BN4O5, Molecular Weight: 408.29. US Biological Life Sciences.
[ (1S) -3-Methyl-1- [ [ (2S) -2-methyloxiranyl] carbonyl] butyl] -carbamic Acid 1,1-Dimethylethyl Ester is a reagent in the synthesis of proteasome inhibitor epoxomicin, which has antitumor, antiinflammatory and antibiotic properties. Group: Biochemicals. Grades: Highly Purified. CAS No. 247068-83-3. Pack Sizes: 10mg, 100mg. Molecular Formula: C14H25NO4, Molecular Weight: 271.35. US Biological Life Sciences.
(αR, 3aS, 4S, 6S, 7aR)-Hexahydro-3a, 8, 8-trimethyl-α-pentyl-4, 6-methano-1, 3, 2-benzodioxaborole-2-methanamine is an intermediate in the preparation of Bortezomib (B675700), a dipeptidyl boronate proteasome inhibitor. Group: Biochemicals. Alternative Names: (αR, 3aS, 4S, 6S, 7aR)-Hexahydro-3a, 5, 5-trimethyl-α-pentyl-4, 6-methano-1, 3, 2-benzodioxaborole-2-methanamine Trifluoroacetic Acid Salt. Grades: Highly Purified. Pack Sizes: 50mg. US Biological Life Sciences.
Worldwide
2,2-Dimethylpropanoyl Chloride
2,2-Dimethylpropanoyl Chloride is used in the synthesis of novel guttiferon A derivatives with promising potential to be used in the treatment of malaria. Also used in the synthesis of potent covalent proteasome inhibitors of. Group: Biochemicals. Alternative Names: 1,1-Dimethylethanecarbonyl Chloride; 2,2,2-Trimethylacetyl Chloride; 2,2-Dimethylpropanoyl Chloride; 2,2-Dimethylpropionic Acid Chloride; 2,2-Dimethylpropionyl Chloride; Neopentanoyl Chloride; Pivalic Acid Chloride; Pivalolyl Chloride; Pivalyl Chloride; Trimethylacetyl Chloride; tert-Butyl Chloro Ketone; tert-Butylcarbonyl Chloride. Grades: Highly Purified. CAS No. 3282-30-2. Pack Sizes: 25ml. US Biological Life Sciences.
Worldwide
2-[(2-Pyrazinylcarbonyl)-Bortezomib
2-[(2-Pyrazinylcarbonyl)-Bortezomib is a derivative of Bortezomib (B675700) which is the first proteasome inhibitor to be approved by the US FDA for multiple myeloma, a blood cancer. Bortezomib is a reversible inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 5mg. Molecular Formula: C24H27BN6O5, Molecular Weight: 490.32. US Biological Life Sciences.
Worldwide
2,5-Dimethylpyrazine
2,5-Dimethylpyrazine is used as a reagent in the synthesis of bone-targeted proteasome inhibitors for multiple myeloma (MM). 2,5-Dimethylpyrazine is also used in the preparation of 3-Methyl-2,5-bis-(2-hydroxyethyl)pyrazine (M295340); a degredation product of Clavulanic Acid (C563750) which is a β-lactamase inhibitor, typically added to amoxicillin to increase its effectiveness. Group: Biochemicals. Grades: Highly Purified. CAS No. 123-32-0. Pack Sizes: 5g, 25g. Molecular Formula: C6H8N2. US Biological Life Sciences.
Worldwide
2-Bromo-1,4-dichlorobenzene
2-Bromo-1,4-dichlorobenzene is a reactant used in the synthesis of C-13 and C-14-labeled versions of the investigational proteasome inhibitor MLN9708. Group: Biochemicals. Grades: Highly Purified. CAS No. 1435-50-3. Pack Sizes: 10g, 25g. Molecular Formula: C6H3BrCl2, Molecular Weight: 225.9. US Biological Life Sciences.
Worldwide
2-Ethyl-2-methyl-1,3-dioxolane
2-Ethyl-2-methyl-1,3-dioxolane is used as a reagent in the synthesis of Strychnine Hydrochloride (S687710); a compound that acts as an antagonist for cholinesterases and beta amyloid aggregation. Also used as a reagent in the study of the prodrugs of peptide aldehyde as proteasome inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 126-39-6. Pack Sizes: 1g, 10g. Molecular Formula: C6H12O2, Molecular Weight: 116.16. US Biological Life Sciences.
Worldwide
(2R)-2-Amino-4-methyl-1-[(2R)-2-methyloxiran-2-yl]pentan-1-one Trifluoroacetate Salt
(2R)-2-Amino-4-methyl-1-(2-methyloxiran-2-yl)pentan-1-one Trifluoroacetate Salt s an impurity of carfilzomib (C183460). Carfilzomib is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg, 50mg. Molecular Formula: C11H18F3NO4, Molecular Weight: 285.26. US Biological Life Sciences.
Worldwide
(2R)-4-Oxo-2-oxetanecarboxylic Acid
(2R)-4-Oxo-2-oxetanecarboxylic Acid is the R-isomer of 4-Oxo-2-oxetanecarboxylic Acid and is used as a reagent in the synthesis of UCK 14A2 derivatives as proteasome inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 177019-47-5. Pack Sizes: 5mg, 10mg. Molecular Formula: C4H4O4, Molecular Weight: 116.07. US Biological Life Sciences.
(2R,4S)-4-((t-Butoxycarbonyl)amino)-1,2-dihydroxy-2,6-dimethyl-3-oxohepan-4-tyl is an intermediate used in the synthesis of Carfilzomib (2S,4S)-Diol (C183495), which is a derivative of Carflizomib (C183460), a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma. Group: Biochemicals. Grades: Highly Purified. CAS No. 1541172-78-4. Pack Sizes: 1mg, 2.5mg. Molecular Formula: C14H27NO5, Molecular Weight: 289.37. US Biological Life Sciences.
(2R,4S)-4-((t-Butoxycarbonyl)amino)-2-hydroxy-2,6-dimethyl-3-oxoheptyl Acetate is an intermediate in synthesizing Carfilzomib (2S,4S)-Diol (C183495), a derivative of Carflizomib (C183460), which is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg, 10mg. Molecular Formula: C16H29NO6, Molecular Weight: 331.4. US Biological Life Sciences.
(2S)-2-Amino-4-methyl-1-[(2R)-2-methyloxiranyl]-1-pentanone Trifluoroacetate is an intermediate of Carfilzomib (C183460) which is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma. Group: Biochemicals. Grades: Highly Purified. CAS No. 247068-85-5. Pack Sizes: 1mg, 10mg. Molecular Formula: C11H18F3NO4, Molecular Weight: 285.26. US Biological Life Sciences.
(2S, 3R) -3-Hydroxy-2- (6-phenylpicolinamido) butanoic Acid is an intermediate in the synthesis of Delanzomib (D230710), an orally active proteasome inhibitor. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences.
(2S,4R)-4-((t-Butoxycarbonyl)amino)-1,2-dihydroxy-2,6-dimethyl-3-oxohepan-4-tyl is an intermediate used in the synthesis of Carfilzomib (2S,4R)-Diol (C183500), is a derivative of Carflizomib (C183460), a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 2.5mg. Molecular Formula: C14H27NO5, Molecular Weight: 289.37. US Biological Life Sciences.
(2S,4R)-4-((t-Butoxycarbonyl)amino)-2-hydroxy-2,6-dimethyl-3-oxoheptyl Acetate is an intermediate in synthesizing Carfilzomib (2S,4R)-Diol (C183500), a derivative of Carflizomib (C183460), a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg, 10mg. Molecular Formula: C16H29NO6, Molecular Weight: 331.4. US Biological Life Sciences.
Worldwide
(2S,4R)-4-((t-Butoxycarbonyl)amino)-2-hydroxy-2,6-dimethyl-3-oxoheptyl Acetate Trifluoroacetate Salt
(2S,4R)-4-((t-Butoxycarbonyl)amino)-2-hydroxy-2,6-dimethyl-3-oxoheptyl Acetate Trifluoroacetate Salt is an intermediate in synthesizing Carfilzomib (2S,4R)-Diol (C183500), a derivative of Carflizomib (C183460), a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg, 10mg. Molecular Formula: C11H21NO4; (C2HF3O2), Molecular Weight: 231.2911402. US Biological Life Sciences.
Worldwide
(2S,4S)-4-Amino-2-hydroxy-2,6-dimethyl-3-oxoheptyl Acetate TFA Salt
(2S,4S)-4-Amino-2-hydroxy-2,6-dimethyl-3-oxoheptyl Acetate TFA Salt is an intermediate used in the synthesis of Carfilzomib (2S,4S)-Diol (C183495), which is a derivative of Carflizomib (C183460), a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 500ug, 1mg. Molecular Formula: C11H21NO4; C2HF3O2, Molecular Weight: 231.2911402. US Biological Life Sciences.
(2S,4S)-4-((t-Butoxycarbonyl)amino)-2-hydroxy-2,6-dimethyl-3-oxoheptyl Acetate is an intermediate in synthesizing Carfilzomib (2S,4S)-Diol (C183495), a derivative of Carflizomib (C183460), which is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg, 10mg. Molecular Formula: C16H29NO6, Molecular Weight: 331.4. US Biological Life Sciences.
(3aS,4S,6S,7aR)-2-Butylhexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborole is an intermediate in the preparation of Bortezomib (B675700), a dipeptidyl boronate proteasome inhibitor. Group: Biochemicals. Alternative Names: [3aS-(3aα,4 β,6 β,7aα)]-2-Butylhexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborole. Grades: Highly Purified. CAS No. 85167-10-8. Pack Sizes: 1g. US Biological Life Sciences.
(3aS,4S,6S,7aR)-Hexahydro-3a,5,5-trimethyl-2-pentyl-4,6-methano-1,3,2-benzodioxaborole is an intermediate in the preparation of Bortezomib (B675700), a dipeptidyl boronate proteasome inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 476335-09-8. Pack Sizes: 1g. US Biological Life Sciences.
Worldwide
4-Azidobutylamine
4-Azidobutylamine is a PROTAC linker, which refers to the alkyl chain composition. 4-Azidobutylamine can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins [1]. 4-Azidobutylamine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Uses: Scientific research. Group: Signaling pathways. CAS No. 88192-20-5. Pack Sizes: 100 mg; 250 mg; 1 g. Product ID: HY-108374.
7-(N-Benzyloxycarbonylglycyl-glycyl-leucyl)amino-4-methylcoumarin is a fluorogenic substrate for the chymotrypsin-like activity of the 20S proteasome. Synonyms: 7-Z-Gly-gly-leu-ME; L-Leucinamide, N-[ (phenylmethoxy)carbonyl]glycylglycyl-N- (4-methyl-2-oxo-2H-1-benzopyran-7-yl)-; Z-GGL-AMC. Grades: ≥98%. CAS No. 97792-39-7. Molecular formula: C28H32N4O7. Mole weight: 536.58.
8-Hydroxyquinoline Hemisulfate Salt Hemihydrate
8-Hydroxyquinoline Hemisulfate Salt Hemihydrate is a 20S proteasome inhibitor. It can be used in pharmacological activity and biological study of treatment of drug-resistant bacterial and fungal infections with metal chelating compounds such as clioquinol analogs and combination with other antibiotics in relation to β lactamase. Group: Biochemicals. Grades: Highly Purified. CAS No. 207386-91-2. Pack Sizes: 100g, 250g. Molecular Formula: C9H11NO6S, Molecular Weight: 261.25. US Biological Life Sciences.
Worldwide
AAF-CMK trifluoroacetate salt
AAF-CMK is a serine protease inhibitor which irreversibly inhibits TPPII (tripeptidyl peptidase II), a giant protease which may substitute for some proteasome function, and reversibly inhibits Cln2 (TPPI). Synonyms: N-Ala-Ala-Phe-CMK; Tripeptidyl Peptidase Inhibitor II; L-Alaninamide,L-alanyl-N-[(1S)-3-chloro-2-oxo-1-(phenylmethyl)propyl]-. Grades: ≥95%. CAS No. 184901-82-4. Molecular formula: C18H23ClF3N3O5. Mole weight: 453.84.
Ac-Arg-Leu-Arg-AMC
Ac-Arg-Leu-Arg-AMC is a fluorogenic substrate for the determination of the trypsin-like activity of purified proteasomes (Km = 78 μM). Synonyms: Ac-RLR-AMC; N2-Acetyl-L-arginyl-L-leucyl-N-(4-methyl-2-oxo-2H-chromen-7-yl)-L-argininamide; L-Argininamide, N2-acetyl-L-arginyl-L-leucyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-. Grades: ≥95%. CAS No. 929903-87-7. Molecular formula: C30H46N10O6. Mole weight: 642.76.
Acetylcorynoline
Acetylcorynoline, which can be extracted from the tubers of Corydalis ambigua, inhibits the maturing of bone marrow-derived dendritic cells in mice. However, it is only cytotoxic in amounts of greater than 20 μM. Acetylcorynoline may be one of the potent immunosuppressive agents through the blockage of dendritic cells maturation and function. Acetylcorynoline significantly decreases dopaminergic neuron degeneration induced by 6-hydroxydopamine in BZ555 strain; prevents α-synuclein aggregation; recovers lipid content in OW13 strain; restores food-sensing behavior, and dopamine levels; and prolongs life-span in 6-hydroxydopamine-treated N2 strain, thus showing its potential as a possible antiparkinsonian drug. Acetylcorynoline may exert its effects by decreasing egl-1 expression to suppress apoptosis pathways and by increasing rpn5 expression to enhance the activity of proteasomes. Uses: Antifungal/anti-inflammatory. Synonyms: (5bR,6S,12bR)-5b,6,7,12b,13,14-Hexahydro-5b,13-dimethyl-[1,3]benzodioxolo[5,6-c]-1,3-dioxolo[4,5-i]phenanthridin-6-ol 6-acetate; Corynoline acetate; O-Acetylcorynoline; [1,3]Benzodioxolo[5,6-c]-1,3-dioxolo[4,5-i]phenanthridin-6-ol,5b,6,7,12b,13,14-hexahydro-5b,13-dimethyl-, 6-acetate, (5bR,6S,12bR)-. Grades: >98%. CAS No. 18797-80-3. Molecular formula: C23H23NO6. Mole weight: 409.43.
Ac-Nle-Pro-Nle-Asp-AMC
Ac-Nle-Pro-Nle-Asp-AMC is a substrate for proteasomes. It can be cleaved by the caspase-like site of proteasome, also known as postglutamyl peptide hydrolase (PGPH). AMC (7-amino-4-methylcoumarin) is released and produces the fluorescence utilized to quantify the caspase-like site activity. Ac-Nle-Pro-Nle-Asp-AMC also inhibits the chymotrypsin-like activity of the proteasome allosterically when bound to the caspase-like site. Synonyms: Ac-Nle-Pro-Nle-Asp-7-amido-4-Methylcoumarin; Ac-nLPnLD-AMC; N-acetyl-L-norleucyl-L-prolyl-L-norleucyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-L-α-asparagine; L-α-Asparagine, N-acetyl-L-norleucyl-L-prolyl-L-norleucyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-; (3S) -4-Hydroxy-3- ({ (2S) -1-hydroxy-2-[ (hydroxy{ (2S) -1-[N- (1-hydroxyethylidene) -L-norleucyl]-2-pyrrolidinyl}methylene) amino]hexylidene}amino) -4-[ (4-methyl-2-oxo-2H-chromen-7-yl) imino]butanoic acid. Grades: ≥98%. CAS No. 355140-49-7. Molecular formula: C33H45N5O9. Mole weight: 655.74.
Ac-RLR-AMC trifluoroacetate salt
Ac-RLR-AMC is a fluorogenic substrate for the 26S proteasome. Ac-RLR-AMC is cleaved to release the fluorescent moiety 7-amino-4-methylcoumarin (AMC), which can be used to quantify the trypsin-like activity of 26S proteasomes. Synonyms: Ac-Arg-Leu-Arg-7-amino-4-methylcoumarin; (S)-2-acetamido-5-guanidino-N-((S)-1-(((S)-5-guanidino-1-((4-methyl-2-oxo-2H-chromen-7-yl)amino)-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)pentanamide, 2,2,2-trifluoroacetate salt. Grades: ≥98%. Molecular formula: C30H46N10O6·CF3COOH. Mole weight: 756.8.
Ac-WLA-AMC
Ac-WLA-AMC is a fluorogenic substrate for the β5c subunit of the 20S proteasome. Ac-WLA-AMC is cleaved to release the fluorescent moiety 7-amino-4-methylcoumarin (AMC), which can be used to quantify the β5c subunit activity. Synonyms: Acetyl-Trp-Leu-Ala-7-amino-4-Methylcoumarin; N-acetyl-L-tryptophyl-L-leucyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-L-alaninamide. Grades: ≥95%. CAS No. 1104011-59-7. Molecular formula: C32H37N5O6. Mole weight: 587.7.
AdaAhx?L?VS - CAS 389064-25-9
A potent, covalent, cell-permeable, irreversible inhibitor of chymotrypsin-like (50-100 nM), trypsin-like (1-5 μM), and PGPH (0.5-1 μM) activities of the 20S proteasome. Group: Fluorescence/luminescence spectroscopy.
Alloxan hydrate
Alloxan hydrate is a diabetogenic agent to induce diabetes. Alloxan hydrate is a proteasome inhibitor. Alloxan causes diabetes in experimental animals through its ability to destroy the insulin-secreting B-cells of the pancreas [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2244-11-3. Pack Sizes: 10 mM * 1 mL; 1 g. Product ID: HY-W017227.
Bortezomib intermediate. A boronic acid dipeptide derivative as proteasome inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 179324-87-9. Pack Sizes: 25mg. US Biological Life Sciences.
Worldwide
AM-114
AM 114 is an inhibitor of chymotrypsin-like activity of the 20S proteasome. In addition, AM-114 shows anticancer activity, It can inhibit cell growth in human colon cancer HCT116 p53+/+ cells. Uses: Anticancer. Synonyms: AM-114; AM 114; AM114; Proteasome Inhibitor IX; ( (1Z, 1'Z)- (1-methyl-4-oxopiperidine-3, 5-diylidene)bis (methanylylidene))bis (4, 1-phenylene))diboronic acid. Grades: 98%. CAS No. 856849-35-9. Molecular formula: C20H21B2NO5. Mole weight: 377.01.
Arimoclomol citrate
Arimoclomol citrate (BRX-220 citrate) is an orally active co-inducer of heat shock proteins ( HSP ) [1]. Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system [2]. Arimoclomol citrate can be used for the study of Niemann - Pick disease type C. Uses: Scientific research. Group: Signaling pathways. Alternative Names: BRX-220 citrate. CAS No. 368860-21-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-106443B.
Arimoclomol maleate
Arimoclomol maleate (BRX-220) is an orally active co-inducer of heat shock proteins ( HSP ) [1]. Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system [2].Arimoclomol maleate can be used for the study of Niemann - Pick disease type C. Uses: Scientific research. Group: Signaling pathways. Alternative Names: BRX-220. CAS No. 289893-26-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-106443A.
ARV-471
ARV-471, an oral estrogen receptor PROTAC protein degrader for the treatment of breast cancer, is an heterobifunctional molecule that promotes the interaction between estrogen receptor alpha and intracellular E3 ligase complexes. It leads to ubiquitylation and subsequent degradation of estrogen receptors through the proteasome. In ER positive breast cancer cell lines, it has a strong ability to degrade ER with a half-maximal degradation concentration (DC50) of ~2 nM. Synonyms: ARV471; ARV 471; (S)-3-(5-(4-((1-(4-((1R,2S)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione; 2,6-Piperidinedione, 3-[1,3-dihydro-1-oxo-5-[4-[[1-[4-[(1R,2S)-1,2,3,4-tetrahydro-6-hydroxy-2-phenyl-1-naphthalenyl]phenyl]-4-piperidinyl]methyl]-1-piperazinyl]-2H-isoindol-2-yl]-, (3S)-; Vepdegestrant; (3S)-3-[1,3-Dihydro-1-oxo-5-[4-[[1-[4-[(1R,2S)-1,2,3,4-tetrahydro-6-hydroxy-2-phenyl-1-naphthalenyl]phenyl]-4-piperidinyl]methyl]-1-piperazinyl]-2H-isoindol-2-yl]-2,6-piperidinedione. Grades: ≥95%. CAS No. 2229711-68-4. Molecular formula: C45H49N5O4. Mole weight: 723.90.
Autophagy Compound Library
A unique collection of 1248 compounds with defined autophagy-inducing or -inhibitory activity for research in autophagy, high throughput screening (HTS) and high content screening (HCS) for new drugs; - Bioactivity and safety confirmed by pre-clinical research and clinical trials; - Targets include Autophagy inducers, Autophagy inhibitors, Proteasome, HIF, HDAC, Aurora Kinase, E3 Ligase, mTOR, etc; - Detailed compound information with structure, target, activity, IC50 value, and biological activity description; - Structurally diverse, medicinally active, and cell permeable; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L3200. Categories: Autophagy Compounds Libraries.
B2
B2 is a cell permeable inhibitor of SIRT2 (sirtuin 2). B2 promotes inclusion formation in cellular models of Huntington's disease and Parkinson's disease. B2 prevents mutant huntingtin-mediated proteasome dysfunction and reduces α-synuclein-mediated toxicity. Synonyms: 5-[4-(4-Chlorobenzoyl)-1-piperazinyl]-8-nitroquinoline; CPNQ. Grades: ≥98% by HPLC. CAS No. 115687-05-3. Molecular formula: C20H17ClN4O3. Mole weight: 396.83.
Baceridin
Baceridin, a cyclic hexapeptide isolated from the culture medium of a plant-related bacillus strain, shows moderate cytotoxicity and weak activity against Staphylococcus aureus. In addition, it is a proteasome inhibitor that inhibits cell cycle progression and induces tumor cell apoptosis through a p53-independent pathway. Synonyms: Cyclo(D-alanyl-L-tryptophyl-L-leucyl-D-leucyl-L-valylisoleucyl); Cyclo(-D-Ala-D-allo-Ile-Val-D-Leu-Leu-Trp); cyclo[D-alanyl-L-tryptophyl-L-leucyl-D-leucyl-L-valyl-(3S)-DL-isoleucyl]. Grades: ≥95%. CAS No. 1622872-91-6. Molecular formula: C37H57N7O6. Mole weight: 695.89.
b-AP15
b-AP15 is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.Not a general deubiquitinase inhibitor. Has minimal inhibition on recombinant and cytosolic nonproteasomal cysteine deubiquitinases. Synonyms: b-AP15; b-AP15; b-AP-15; USP14 Inhibitor III; UCHL5UCH37 Inhibitor II; NSC687852. Grades: >98%. CAS No. 1009817-63-3. Molecular formula: C22H17N3O6. Mole weight: 419.39.
Boc-Leu-Ser-Thr-Arg-AMC
Boc-Leu-Ser-Thr-Arg-AMC is a good fluorescent substrate for activated protein C (Km = 3.3·10-4 M, kcat = 8.4 s-1) and is commonly used to measure tryptic activity of proteasome. Synonyms: Boc-LSTR-AMC; Boc-leucyl-seryl-threonyl-arginine-4-methylcoumaryl-7-amide; Boc-Leu-Ser-Thr-Arg-7-amido-4-methylcoumarin. Grades: ≥95%. CAS No. 73554-93-5. Molecular formula: C34H52N8O10. Mole weight: 732.82.
Boc-L-Valine
Boc-L-Valine is used in amino acid conjugates as proteasome inhibitors. Group: Biochemicals. Alternative Names: N-[ (1, 1-dimethylethoxy) carbonyl]-L-valine; (2S) -2- (tert-Butoxycarbonylamino) -3-methylbutanoic Acid; (2S) -2-[[ (1, 1-Dimethylethoxy) carbonyl]amino]-3-methylbutanoic Acid; (S)-2-(tert-Butoxycarbonylamino)-3-methylbutanoic Acid; (S)-N-tert-Butoxycarbonylvaline; BOC-valine; Boc-L-valine; N-BOC-L-valine; N-BOC-valine; N-tert-Butoxycarbonyl-L-valine; N-tert-Butoxycarbonylvaline; N-tert-Butyloxycarbonyl-L-valine; N-tert-Butyl oxycarbonyl valine; N-α-tert-Butoxycarbonyl-L-valine; NSC 197197; t-Butoxycarbonyl-L-valine; tert-Butoxycarbonyl-L-valine. Grades: Highly Purified. CAS No. 13734-41-3. Pack Sizes: 25g. US Biological Life Sciences.
Worldwide
Bortezomib
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome ( K i =0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PS-341; LDP-341; NSC 681239. CAS No. 179324-69-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-10227.
Bortezomib is the first proteasome inhibitor to be approved b the US FDA for multiple myeloma, a blood cancer. A reversible inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. Group: Biochemicals. Alternative Names: Velcade-deuterated, [ (1R) -3-Methyl-1- [ [ (2S) -1-oxo-3-phenyl-2- [ (pyrazinylcarbonyl) amino] propyl] amino] butyl] -boronic Acid-deuterated. Grades: Highly Purified. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
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