Proteasomes are very large protein complexes inside all eukaryotes and archaea, and in some bacteria. In eukaryotes, they are located in the nucleus and the cytoplasm. The main function of the proteasome is to degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Enzymes that carry out such reactions are called proteases. Proteasomes are part of a major mechanism by which cells regulate the concentration of particular proteins and degrade misfolded proteins. The degradation process yields peptides of about seven to eight amino acids long, which can then be further degraded into amino acids and used in synthesizing new proteins. Proteins are tagged for degradation with a small protein called ubiquitin. The tagging reaction is catalyzed by enzymes called ubiquitin ligases. Once a protein is tagged with a single ubiquitin molecule, this is a signal to other ligases to attach additional ubiquitin molecules. The result is a polyubiquitin chain that is bound by the proteasome, allowing it to degrade the tagged protein.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
Autophagy LRRK2 ULK Mitophagy
Cell Cycle/DNA Damage >
Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeleton >
Arp2/3 Complex Dynamin Gap Junction Protein Integrin Kinesin Microtubule/Tubulin Mps1 Myosin PAK
Epigenetics >
AMPK Aurora Kinase DNA Methyltransferase Epigenetic Reader Domain HDAC Histone Acetyltransferase Histone Demethylase Histone Methyltransferase JAK MicroRNA PARP PKC Sirtuin Protein Arginine Deiminase
GPCR/G Protein >
5-HT Receptor Adenosine Receptor Adenylate Cyclase Adiponectin Receptor Adrenergic Receptor Angiotensin Receptor Bombesin Receptor Bradykinin Receptor Cannabinoid Receptor CaSR CCR CGRP Receptor Cholecystokinin Receptor CRFR CXCR Dopamine Receptor EBI2/GPR183 Endothelin Receptor GHSR Glucagon Receptor Glucocorticoid Receptor GNRH Receptor GPCR19 GPR109A GPR119 GPR120 GPR139 GPR40 GPR55 GPR84 Guanylate Cyclase Histamine Receptor Imidazoline Receptor Leukotriene Receptor LPL Receptor mAChR MCHR1 (GPR24) Melatonin Receptor mGluR Motilin Receptor Neurokinin Receptor Neuropeptide Y Receptor Neurotensin Receptor Opioid Receptor Orexin Receptor (OX Receptor) Oxytocin Receptor P2Y Receptor Prostaglandin Receptor Protease-Activated Receptor (PAR) Ras RGS Protein Sigma Receptor Somatostatin Receptor TSH Receptor Urotensin Receptor Vasopressin Receptor Melanocortin Receptor
Immunology/Inflammation >
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JAK/STAT Signaling >
EGFR JAK Pim STAT
MAPK/ERK Pathway >
ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
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ATP Synthase BCRP Calcium Channel CFTR Chloride Channel CRAC Channel CRM1 EAAT2 GABA Receptor GlyT HCN Channel iGluR Monoamine Transporter Monocarboxylate Transporter Na+/Ca2+ Exchanger Na+/HCO3- Cotransporter Na+/K+ ATPase nAChR NKCC P-glycoprotein P2X Receptor Potassium Channel Proton Pump SGLT Sodium Channel TRP Channel URAT1
Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
PROTAC E3 Ligase Ligand-Linker Conjugate Ligand for E3 Ligase PROTAC Linker PROTAC-linker Conjugate for PAC
Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

RA190

RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

  • CAS Number: 1617495-03-0
  • MF: C28H23Cl5N2O2
  • MW: 596.76
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Anticancer agent 82

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].

  • CAS Number: 2319587-80-7
  • MF: C19H18Cl2N4O
  • MW: 389.28
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

20S Proteasome-IN-3

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].

  • CAS Number: 1803040-07-4
  • MF: C34H43N3O8
  • MW: 621.72
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TCH-165

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.

  • CAS Number: 1446350-60-2
  • MF: C39H37N3O3
  • MW: 595.743
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

calpeptin

Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets[1]. Calpeptin is also an inhibitor of cathepsin K[2].

  • CAS Number: 117591-20-5
  • MF: C20H30N2O4
  • MW: 362.463
  • Catalog: Cathepsin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 550.7±45.0 °C at 760 mmHg
  • Melting Point: 60-75 °C
  • Flash Point: 286.8±28.7 °C

Ac-Nle-Pro-Nle-Asp-AMC

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].

  • CAS Number: 355140-49-7
  • MF: C33H45N5O9
  • MW: 655.739
  • Catalog: Proteasome
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 902.2±75.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 499.4±37.1 °C

MUN57694

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 

  • CAS Number: 858557-69-4
  • MF: C23H25N3O4
  • MW: 407.46
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Carfilzomib-d8

Carfilzomib-d8 is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

  • CAS Number: 1537187-53-3
  • MF: C40H49D8N5O7
  • MW: 727.96
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 975.6±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 543.8±34.3 °C

Calpain Inhibitor VI

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].

  • CAS Number: 190274-53-4
  • MF: C17H25FN2O4S
  • MW: 372.455
  • Catalog: Proteasome
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NIC-0102

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].

  • CAS Number: 2806031-94-5
  • MF: C21H25BF2N2O4
  • MW: 418.24
  • Catalog: NOD-like Receptor (NLR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MG132

(R)-MG-132 is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor[1].

  • CAS Number: 1211877-36-9
  • MF: C26H41N3O5
  • MW: 475.621
  • Catalog: Proteasome
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 682.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 366.3±31.5 °C

Z-LLY-FMK

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].

  • CAS Number: 133410-84-1
  • MF: C30H40FN3O6
  • MW: 557.65
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ac-PAL-AMC

Ac-PAL-AMC is a fluorogenic substrate specific for 20S proteasome LMP2/β1i activity[1].

  • CAS Number: 1431362-79-6
  • MF: C26H34N4O6
  • MW: 498.571
  • Catalog: Proteasome
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 845.2±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 465.0±34.3 °C

Davelizomib

Davelizomib is proteasome inhibitor with antineoplastic effect[1].

  • CAS Number: 2409841-51-4
  • MF: C21H26BF2N3O7
  • MW: 481.25
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VR23

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.

  • CAS Number: 1624602-30-7
  • MF: C19H16ClN5O6S
  • MW: 477.878
  • Catalog: Proteasome
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 699.3±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 376.7±34.3 °C

(Rac)-Calpain Inhibitor XII

(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM), with lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.

  • CAS Number: 181769-57-3
  • MF: C26H34N4O5
  • MW: 482.572
  • Catalog: Proteasome
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(-)-3-<(1E)-1,3-dimethylpent-1-enyl>-10-hydroxy-7-methoxy-1H-naphtho<2,3-c>pyran-8,9(8H)-dione

Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent ubiquitin-proteasome system (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC50 value of 3.2 μM. Anti-tumor agent[1].

  • CAS Number: 138039-33-5
  • MF: C21H22O5
  • MW: 354.39600
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ixazomib (MLN2238)

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 (Ki of 0.93 nM).

  • CAS Number: 1072833-77-2
  • MF: C14H19BCl2N2O4
  • MW: 361.029
  • Catalog: Autophagy
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KZR-616

KZR-616 (KZR616) is a potent, selective dual immunoproteasome subunit LMP7/LMP2 inhibitor with IC50 of 39 nM/139 nM, weakly inhibits β5, MECL-1 and no acitivty against β1 subunit; shows no inhibition at 10 uM against a broad selectivity panel of 20 serine, metallo-, cysteine and aspartyl proteases and 11 hydrolases; demonstrates efficacy in the anti-collagen antibody induced arthritis (CAIA) models. Other Indication Phase 2 Clinical

  • CAS Number: 1629677-75-3
  • MF: C30H42N4O8
  • MW: 586.686
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FK-448 Free base

FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM.

  • CAS Number: 85858-76-0
  • MF: C25H30N2O3
  • MW: 406.52
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MG-115

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].

  • CAS Number: 133407-86-0
  • MF: C25H39N3O5
  • MW: 461.59
  • Catalog: Apoptosis
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 678.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 364.3±31.5 °C

Thrombin inhibitor 5

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].

  • CAS Number: 328108-09-4
  • MF: C11H9FN4O3
  • MW: 264.21
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Epoxomicin

Epoxomicin is a cell-permeable and irreversible proteasome inhibitor, primarily the chymotrypsin-like activity.

  • CAS Number: 134381-21-8
  • MF: C28H50N4O7
  • MW: 554.719
  • Catalog: Proteasome
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 795.7±60.0 °C at 760 mmHg
  • Melting Point: 107-109ºC
  • Flash Point: 435.0±32.9 °C

Aclarubicin

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].

  • CAS Number: 57576-44-0
  • MF: C42H53NO15
  • MW: 811.86800
  • Catalog: DNA/RNA Synthesis
  • Density: 1.42 g/cm3
  • Boiling Point: 897.7ºC at 760 mmHg
  • Melting Point: 151-153ºC
  • Flash Point: 496.7ºC

Bortezomib (PS-341)

Bortezomib (PS-341) is a potent 20S proteasome inhibitor with a Ki of 0.6 nM.

  • CAS Number: 179324-69-7
  • MF: C19H25BN4O4
  • MW: 384.237
  • Catalog: Autophagy
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 122-124°C
  • Flash Point: N/A

Celastrol

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.

  • CAS Number: 34157-83-0
  • MF: C29H38O4
  • MW: 450.610
  • Catalog: Autophagy
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 645.7±55.0 °C at 760 mmHg
  • Melting Point: 185-200ºC
  • Flash Point: 358.3±28.0 °C

benzyloxycarbonylleucyl-leucyl-leucyl-4-methyl-coumaryl-7-amide

Z-Leu-Leu-Leu-AMC is a fluorogenic substrate for measuring the chymotrypsin-like protease activity of the 20S proteasome[1].

  • CAS Number: 152015-61-7
  • MF: C36H48N4O7
  • MW: 648.78900
  • Catalog: Proteasome
  • Density: 1.174g/cm3
  • Boiling Point: 854.4ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 470.5ºC

Proteasome-IN-1

Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.

  • CAS Number: 374080-21-4
  • MF: C42H35N5O3
  • MW: 657.76
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PTP1B-IN-9

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].

  • CAS Number: 145888-79-5
  • MF: C19H13Cl4NO
  • MW: 413.12500
  • Catalog: Proteasome
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Suc-Gly-Gly-Phe-pNA

Suc-Gly-Gly-Phe-pNA is the chymotrypsin substrate with an Km value of 1.6 mM[1][2].

  • CAS Number: 68982-90-1
  • MF: C23H25N5O8
  • MW: 499.47300
  • Catalog: Proteasome
  • Density: 1.401g/cm3
  • Boiling Point: 1005.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 562ºC