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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). Group: Pharmaceutical. Alternative Names: N-Ala-Ala-Phe-CMK; Tripeptidyl Peptidase Inhibitor II; L-Alaninamide,L-alanyl-N-[(1S)-3-chloro-2-oxo-1-(phenylmethyl)propyl]-. CAS No. 184901-82-4. Pack Sizes: 100 mg. Product ID: BAT-015706. Molecular formula: C18H23ClF3N3O5. Mole weight: 453.84. Custom synthesis is available. Send your inquiries for more information.
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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. Group: Pharmaceutical. Alternative Names: (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)-. CAS No. 18797-80-3. Pack Sizes: 10 mg. Product ID: B2703-464490. Molecular formula: C23H23NO6. Mole weight: 409.43. Custom synthesis is available. Send your inqui
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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. Group: Pharmaceutical. Alternative Names: 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. CAS No. 2229711-68-4. Pack Sizes: 5 mg. Product ID: B1370-380753. Molecular formula: C45H49N5O4. Mole weight: 723.9. Custom synthesis is available. Send your inquiries for more information.
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Boc-LRR-AMC (trifluoroacetate salt)
Boc-LRR-AMC is a fluorogenic substrate for the trypsin-like activity of the 26S proteasome or 20S proteolytic core. Group: Pharmaceutical. Alternative Names: Boc-Leu-Arg-Arg-AMC.TFA; N-[(1,1-dimethylethoxy)carbonyl]-L-leucyl-L-arginyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-L-argininamide, trifluoroacetate salt. Pack Sizes: 50 mg. Product ID: BAT-016477. Molecular formula: C35H53F3N10O9. Mole weight: 814.87. Custom synthesis is available. Send your inquiries for more information.
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Bortezomib
Bortezomib is a potent, reversible and selective 20S proteasome inhibitor with a Ki of 0.6 nM. It is an antineoplastic agent that is used in treatment of refractory multiple myeloma and certain lymphomas. Group: Pharmaceutical. Alternative Names: PS-341; PS 341; PS341; LDP 341; LDP-341; LDP341; MLN341; MLN-341; MLN 341; B-[(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic Acid; Velcade; ((R)-3-Methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid; N-[(1R)-1-(Dihydroxyboryl)-3-methylbutyl]-Nα-(2-pyrazinylcarbonyl)-L-phenylalaninamide. CAS No. 179324-69-7. Pack Sizes: 1 g. Product ID: BBF-05860. Molecular formula: C19H25BN4O4. Mole weight: 384.24. Custom synthesis is available. Send your inquiries for more information.
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Broussonin B
Broussonin B is a natural phenols found in the branch of Broussonetia papyrifera, it has moderate inhibitory activities against a chymotrypsin-like activity of the proteasome. Group: Pharmaceutical. Alternative Names: 4-[3-(4-Hydroxyphenyl)propyl]-3-methoxyphenol. CAS No. 73731-86-9. Pack Sizes: 1 mg. Product ID: NP5061. Molecular formula: C16H18O3. Mole weight: 258.32. Custom synthesis is available. Send your inquiries for more information.
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Carfilzomib
Carfilzomib is a tetrapeptide epoxyketone and an analog of epoxomicin, acting as a selective proteasome inhibitor, such as the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC50 = 14 nM). It has been used as an injectable antineoplastic agent (IV only). Group: Pharmaceutical. Alternative Names: Kyprolis; PR171; PR-171; PR 171; (2S)-4-methyl-N-[(2S)-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide. CAS No. 868540-17-4. Pack Sizes: 250 mg. Product ID: B0084-305419. Molecular formula: C40H57N5O7. Mole weight: 719.9. Custom synthesis is available. Send your inquiries for more information.
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Ixazomib Citrate
The citrate salt form of Ixazomib which is a proteasome inhibitor. It is undergoing a rollover Phase II trial against multiple myeloma, amyloidosis and lymphoma in sorts of countries. IC50 = 3.4 nM. Group: Pharmaceutical. Alternative Names: 4-(carboxymethyl)-2-((R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-6-oxo-1,3,2-dioxaborinane-4-carboxylic acid; MLN9708; MLN-9708; MLN 9708. CAS No. 1239908-20-3. Pack Sizes: 100 mg. Product ID: BBF-04173. Molecular formula: C20H23BCl2N2O9. Mole weight: 517.12. Custom synthesis is available. Send your inquiries for more information.
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K-7174 dihydrochloride
K-7174, one of proteasome inhibitory homopiperazine derivatives, exhibits a therapeutic effect, which is stronger when administered orally than intravenously, without obvious side effects in a murine myeloma model. Moreover, K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib. Group: Pharmaceutical. Alternative Names: 1,4-bis((E)-5-(3,4,5-trimethoxyphenyl)pent-4-en-1-yl)-1,4-diazepane dihydrochloride; K7174; K 7174; K-7174; K-7174-2HCl; K-7174 dihydrochloride. CAS No. 191089-60-8. Pack Sizes: 100 mg. Product ID: B2693-463577. Molecular formula: C33H50Cl2N2O6. Mole weight: 641.67. Custom synthesis is available. Send your inquiries for more information.
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Marizomib
Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity. Marizomib irreversibly binds to and inhibits the 20S catalytic core subunit of the proteasome by covalently modifying its active site threonine residues. Group: Pharmaceutical. Alternative Names: (-)-Salinosporamide A; ML 858; ML858; ML-858; Marizomib; NPI 0052; NPI0052; NPI-0052; Salinosporamide A. CAS No. 437742-34-2. Pack Sizes: 1 mg. Product ID: BBF-05732. Molecular formula: C15H20ClNO4. Mole weight: 313.78. Custom synthesis is available. Send your inquiries for more information.
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MG-132
MG-132 is a potent Proteasome inhibitor with potential anticancer activity. MG-132 induces MCPIP1 expression; induces C6 glioma cell apoptosis via oxidative stress; induces AIF nuclear translocation through down-regulation of ERK and Akt/mTOR pathway. Group: Pharmaceutical. Alternative Names: Z-Leu-leu-leu-al. CAS No. 133407-82-6. Pack Sizes: 100 mg. Product ID: B2693-361205. Molecular formula: C26H41N3O5. Mole weight: 475.62. Custom synthesis is available. Send your inquiries for more information.
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ML241
ML241 is a selective p97 ATPase inhibitor and IC50 value is 100 nM. It can inhibit degradation of a p97-dependent but not a p97-independent proteasome substrate in a dual-reporter cell line. ML241 may be a novel agent for the treatment of cancer. Uses: Anticancer. Group: Pharmaceutical. Alternative Names: 2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine; ML241; ML-241; ML 241. CAS No. 1346528-06-0. Pack Sizes: 100 mg. Product ID: B0084-475332. Molecular formula: C23H24N4O. Mole weight: 372.46. Custom synthesis is available. Send your inquiries for more information.
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MV151
MV151 is a cell-permeable, fluorescent, broad-spectrum proteasome inhibitor for labeling proteasomes in vitro and in vivo. MV151 specifically targets all active subunits of the proteasome and immunoproteasome in living cells, allowing for rapid and sensitive in-gel detection. Group: Pharmaceutical. Alternative Names: MV 151; MV-151; Bodipy TMRAhx(3)L(3)VS. CAS No. 945611-88-1. Pack Sizes: 1 mg. Product ID: B1370-108391. Molecular formula: C59H91BF2N8O9S. Mole weight: 1137.27. Custom synthesis is available. Send your inquiries for more information.
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Pseudolaric acid B
Pseudolaric acid B (PAB), which comes from the bark of Pseudolarix kaempferi Gordon, has diverse effects that are relevant to cancer therapy, including apoptosis of cancer cells (IC50 = ~1 μM), preventing angiogenesis, and inhibiting tumor growth in vivo. pseudolaric acid B can trigger apoptosis by decreasing Bcl-2 levels and activating caspase-3 protease. The future development of PAB as a cancer therapeutic is ongoing. Besides, PAB significantly suppressed proliferation of DU145 cells in a dose-dependent manner without obvious cytotoxicity. PAB may inhibit growth of HRPC DU145 cells and induce apoptosis through ROS generation and Bcl-2 degradation via the activation of the ubiquitin-proteasome pathway. Uses: Antifungal/antifertility. Group: Pharmaceutical. Alternative Names: PLAB; 1H-4,9a-Ethanocyclohepta[c]pyran-7-carboxylicacid,4a-(acetyloxy)-3-[(1E,3E)-4-carboxy-1,3-pentadien-1-yl]-3,4,4a,5,6,9-hexahydro-3-methyl-1-oxo-,7-methyl ester, (3R,4S,4aS,9aR)-; Pseudolarix acid B; Pseudolaric acid. CAS No. 82508-31-4. Pack Sizes: 10 mg. Product ID: NP1536. Molecular formula: C23H28O8. Mole weight: 432.46. Custom synthesis is available. Send your inquiries for more information.
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RAMB4
RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. Group: Pharmaceutical. Alternative Names: PTP1B-IN-9; 3,5-bis(3,4-dichlorobenzylidene)piperidin-4-one. CAS No. 145888-79-5. Pack Sizes: 25 mg. Product ID: B1370-063301. Molecular formula: C19H13Cl4NO. Mole weight: 413.13. Custom synthesis is available. Send your inquiries for more information.
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(R)-MG132
(R)-MG-132 is a reversible, cell permeable and selective tripeptide aldehyde proteasome inhibitor (IC50 = 0.22 μM), the most potent stereoisomer of MG-132. It exhibits cytostatic and cytotoxic effects in tumor cells in vitro. Group: Pharmaceutical. Alternative Names: (R)-MG132; (R)-MG 132; MolPort-009-019-420; Cbz-L-leu-D-leu-L-leu-H; KS-000006AS; N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-D-leucinamide. CAS No. 1211877-36-9. Pack Sizes: 10 mg. Product ID: BAT-010215. Molecular formula: C26H41N3O5. Mole weight: 475.62. Custom synthesis is available. Send your inquiries for more information.
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Serdemetan
Serdemetan, also known as JNJ-26854165, is an orally bioavailable, small-molecule HDM2 antagonist with potential antineoplastic activity. HDM2 antagonist JNJ-26854165 inhibits the binding of the HDM2-p53 complex to the proteasome, blocking the degradation of p53; p53 signaling and p53-mediated induction of tumor cell apoptosis may thus be restored. In addition to p53, degradation of other HDM2 client proteins may be inhibited. HDM2 (human homolog of double minute 2), a zinc finger protein, is a negative regulator of the p53 pathway; often overexpressed in cancer cells, this oncoprotein has been implicated in cancer cell proliferation and survival. Group: Pharmaceutical. Alternative Names: JNJ-26854165; JNJ26854165; JNJ 26854165. CAS No. 881202-45-5. Pack Sizes: 100 mg. Product ID: B1370-099769. Molecular formula: C21H20N4. Mole weight: 328.42. Custom synthesis is available. Send your inquiries for more information.
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Steviol
Steviol is a diterpenoiic carboxylic alcohol and is isolated from the herbs of Stevia rebaudiana. It is the aglycon derivative of natural sweetener steviol glycosides and is found to be highly mutagenic compared to Stevioside. It inhibits the proliferation of the gastrointestinal cancer cells and the human osteosarcoma U2OS cell line in a dose- and time-dependent manner. It also inhibits human organic anion transporters (hOATs) in uptake assays using murine cells from the S2 segment of proximal tubules. It is selective for hOAT1 and hOAT3 over hOAT2 and hOAT4. It increases CYP3A29 expression and enhances pancreatic beta-cell function and taste sensation by potentiation of TRPM5 channel activity. It can be used to treat polycystic kidney disease. It can promote proteasome and lysosome-mediated AQP2 degradation and slow cyst growth by reducing AQP2 transcription. Group: Pharmaceutical. Alternative Names: (4α)-13-Hydroxy-kaur-16-en-18-oic Acid; 13-Hydroxy-kaur-16-en-18-oic Acid; 13-Hydroxykaurenoic Acid; Ent-13-hydroxy-kauran-16-en-19-oic Acid; 1H-2,10a-Ethanophenanthrene; 13-O-Glucosylsteviol; Hydroxydehydrostevic Acid; (4R,4aS,6aR,9S,11aR,11bS)-9-hydroxy-4,11b-dimethyl-8-methylenetetradecahydro-6a,9-methanocyclohepta[a]naphthalene-4-carboxylic acid. CAS No. 471-80-7. Pack Sizes: 20 mg. Product ID: NP1541. Molecular formula: C20H30O3. Mole weight: 318.45. Custom synthesis is available. Send your inquiries for more information
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VER-155008
VER-155008 is an adenosine-derived inhibitor of heat shock protein 70 (Hsp70; IC50 = 0.5 μM) that is selective over Hsp90. It targets the nucleotide-binding domain (NBD) of Hsp70 and similarly binds the NBDs of Hsp70 cognates Hsc70 (Ki = 10 μM) and glucose-regulated protein 78 (Grp78; KD = 80 nM). VER-155008 inhibits the proliferation of human breast and colon cancer cell lines, inducing apoptosis or caspase-independent cell death. It induces the proteasome-dependent degradation of Hsp90 client proteins and potentiates the apoptotic activity of Hsp90 inhibitors. VER-15508 also triggers paraptosis in anaplastic thyroid carcinoma cells. Group: Pharmaceutical. Alternative Names: 8-(3,4-Dichlorobenzyl)amino-5'-O-(4-cyanobenzyl)adenosine; C07; VER 155008; VER155008; 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-Adenosine; 4-((((2R,3S,4R,5R)-5-(6-amino-8-(3,4-dichlorobenzylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)methyl)benzonitrile. CAS No. 1134156-31-2. Pack Sizes: 100 mg. Product ID: B1370-272446. Molecular formula: C25H23Cl2N7O4. Mole weight: 556.4. Custom synthesis is available. Send your inquiries for more information.
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Corosolic acid
Corosolic acid, that is isolated from the barks of Lagerstroemia speciosa, contains anti-angiogenic activity that can suppress FAK signaling induced by angiopoietin-1. Corosolic acid exerts its anticancer activity against colon cancer cells by promoting the N-terminal phosphorylation and subsequent proteasomal degradation of β-catenin. Besides, Corosolic acid induced apoptosis in colorectal cancer (CRC), rendering this compound a potential anticancer agent for the treatment of CRC. Corosolic acid, as a new plant medicine for preventing and treating obesity and type II diabetes, and a functional natural health food and pharmaceutical raw material, has become a popular product in the market. Uses: Anti-angiogenic/anticancer. Group: Pharmaceutical. Alternative Names: 2-A-HYDROXYURSOLIC ACID; 2ALPHA-HYDROXYURSOLIC ACID; 2,3-DIHYDROXYURS-12-EN-28-OIC ACID; HYDROXYURSOLIC ACID; COROSOLIC ACID; Corsolicacid; Corosolic; (2a,3b)-2,3-Dihydroxy-urs-12-en-28-oic acid. CAS No. 4547-24-4. Pack Sizes: 50 mg. Product ID: NP7232. Molecular formula: C30H48O4. Mole weight: 472.7. Custom synthesis is available. Send your inquiries for more information.
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HSP990
HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (HSP90) with potential antineoplastic activity. HSP990 binds to and inhibits the activity of Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation. HSP90, upregulated in a variety of tumor cells, is a molecular chaperone that plays a key role in the conformational maturation, stability and function of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation and/or immune responses. Group: Pharmaceutical. Alternative Names: NVP-HSP990; NVP HSP990; NVPHSP990; HSP 990; HSP-990. CAS No. 934343-74-5. Pack Sizes: 100 mg. Product ID: B1370-460667. Molecular formula: C20H18FN5O2. Mole weight: 379.39. Custom synthesis is available. Send your inquiries for more information.
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Luminespib
Luminespib, also known as AUY-922 (or NVP-AUY922), is a derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Hsp90 inhibitor AUY922 has been shown to bind with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation of oncogenic client proteins. Group: Pharmaceutical. Alternative Names: Luminespib; AUY-922; AUY922; AUY 922; NVP-AUY-922; NVP-AUY922; VER-52296; VER52296; VER 52296. CAS No. 747412-49-3. Pack Sizes: 50 mg. Product ID: B0084-251226. Molecular formula: C26H31N3O5. Mole weight: 465.54. Custom synthesis is available. Send your inquiries for more information.
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