Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of natural product small molecules within a cell or tissue. In each pathway, enzymes catalyze the conversion of substrates into structurally similar products. Metabolic processes typically transform small molecules, but also include macromolecular processes such as DNA repair and replication, and protein synthesis and degradation. Metabolism maintains the living state of the cells and the organism.

Proteases are used throughout an organism for various metabolic processes. Proteases control a great variety of physiological processes that are critical for life, including the immune response, cell cycle, cell death, wound healing, food digestion, and protein and organelle recycling. On the basis of the type of the key amino acid in the active site of the protease and the mechanism of peptide bond cleavage, proteases can be classified into six groups: cysteine, serine, threonine, glutamic acid, aspartate proteases, as well as matrix metalloproteases. Proteases can not only activate proteins such as cytokines, or inactivate them such as numerous repair proteins during apoptosis, but also expose cryptic sites, such as occurs with β-secretase during amyloid precursor protein processing, shed various transmembrane proteins such as occurs with metalloproteases and cysteine proteases, or convert receptor agonists into antagonists and vice versa such as chemokine conversions carried out by metalloproteases, dipeptidyl peptidase IV and some cathepsins. In addition to the catalytic domains, a great number of proteases contain numerous additional domains or modules that substantially increase the complexity of their functions.

Imbalances in metabolic activities have been found to be critical in a number of pathologies, such as cardiovascular diseases, inflammation, cancer, and neurodegenerative diseases.

References:
[1] Turk B, et al. EMBO J. 2012 Apr 4;31(7):1630-43.
[2] Eatemadi A, et al. Biomed Pharmacother. 2017 Feb;86:221-231.


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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
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MMP-13-IN-1

MMP-13-IN-1 is a potent and selective inhibitor of MMP-13 with a IC50 value of 16 nM. MMP-13-in-1 can be used for atherosclerosis research[1].

  • CAS Number: 2925249-49-4
  • MF: C19H16F3N3O3
  • MW: 391.34
  • Catalog: MMP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-689502

L-689502 is a potent inhibitor of HIV-l protease with an IC50 of 1 nM.

  • CAS Number: 138483-63-3
  • MF: C39H51N3O7
  • MW: 673.83800
  • Catalog: HIV Protease
  • Density: 1.24g/cm3
  • Boiling Point: 886.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 490.2ºC

LY56110

LY56110 is an orally active aromatase inhibitor. LY56110 inhibits P-450-dependent p-nitroanisole O-demethylation and ethylmorphine N-demethylation in hepatic microsomes isolated from rat, with the IC50 of 2.5 and 11 μΜ, respectively. LY56110 can be used for neurological disorder study[1][2].

  • CAS Number: 26766-37-0
  • MF: C17H12Cl2N2
  • MW: 315.20
  • Catalog: Cytochrome P450
  • Density: 1.296g/cm3
  • Boiling Point: 438.3ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 251.5ºC

FAAH-IN-8

FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 value of 6.7 nM and a Ki value of 5 nM. FAAH-IN-8 has high blood-brain permeability and a significant antioxidant profile with no neurotoxicity[1].

  • CAS Number: 2867633-84-7
  • MF: C18H14N4O
  • MW: 302.33
  • Catalog: FAAH
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fitusiran

Fitusiran (ALN-AT3SC), an small interfering RNA, specifically targets antithrombin (AT) messenger RNA to lower production of AT in the liver. Fitusiran increases thrombin generation and has the potential for the research of the hemophilia[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FAAH/cPLA2α-IN-1

FAAH/cPLA2α-IN-1 is a dual inhibitor of FAAH and cPLA2α with IC50s of 32 and 47 nM, respectively[1].

  • CAS Number: 1696401-38-3
  • MF: C19H26N4O5
  • MW: 390.43
  • Catalog: FAAH
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NSC 663284(DA3003-1)

NSC 663284 is a Cdc25 dual specificity phosphatases inhibitor with an IC50 of 0.21 μM.

  • CAS Number: 383907-43-5
  • MF: C15H16ClN3O3
  • MW: 321.759
  • Catalog: Phosphatase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 478.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 243.4±28.7 °C

Anecortave Acetate

Anecortave acetate is a potent ocular angiostatic agent. Anecortave acetate inhibits neovascularization which is induced by many different angiogenic factors, and increases plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate can be used to research ocular neovascular diseases[1][2].

  • CAS Number: 7753-60-8
  • MF: C23H30O5
  • MW: 386.48100
  • Catalog: PAI-1
  • Density: 1.23g/cm3
  • Boiling Point: 551.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 188.4ºC

20-HETE inhibitor-1

20-HETE inhibitor-1 (comp 83) is a 20-HETE formation inhibitor[1]

  • CAS Number: 2472030-28-5
  • MF: C19H24N4O
  • MW: 324.42
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LP533401 HCI

LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

  • CAS Number: 1040526-12-2
  • MF: C27H23ClF4N4O3
  • MW: 562.943
  • Catalog: Tryptophan Hydroxylase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

YM-01(YM-1)

YM-1 is a stable and soluble MKT-077 (HY-15096) analog and an orally active Hsp70 inhibitor. YM-1 induces cell death of HeLa cells and up-regulates the level of p53 and p21 proteins[1][2].

  • CAS Number: 409086-68-6
  • MF: C20H20ClN3OS2
  • MW: 417.975
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

PF-4191834

PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain[1].

  • CAS Number: 1029317-21-2
  • MF: C22H23N3O2S
  • MW: 393.50200
  • Catalog: 5-Lipoxygenase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

TRAP-14 trifluoroacetate salt

SFLLRNPNDKYEPF is a synthetic thrombin receptor agonist peptide.

  • CAS Number: 137339-65-2
  • MF: C81H118N20O23
  • MW: 1739.92000
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ubenimex

Bestatin is a natural, broad-spectrum, and competitive aminopeptidase inhibitor.

  • CAS Number: 58970-76-6
  • MF: C16H24N2O4
  • MW: 308.373
  • Catalog: Aminopeptidase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 604.7±55.0 °C at 760 mmHg
  • Melting Point: 245 °C (dec.)(lit.)
  • Flash Point: 319.5±31.5 °C

MMP3 inhibitor 1

MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC50 of 1 nM[1].

  • CAS Number: 312930-75-9
  • MF: C23H31N3O6S
  • MW: 477.57
  • Catalog: MMP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Saquinavir mesylate

Saquinavir mesylate is an HIV Protease Inhibitor used in antiretroviral therapy. IC50 Value:Target: HIV ProteaseSaquinavir is a protease inhibitor. Proteases are enzymes that cleave protein molecules into smaller fragments. HIV protease is vital for both viral replication within the cell and release of mature viral particles from an infected cell. Saquinavir binds to the active site of the viral protease and prevents cleavage of viral polyproteins, preventing maturation of the virus. Saquinavir inhibits both HIV-1 and HIV-2 proteases.Studies have also looked at Saquinavir as a possible anti-cancer agent.

  • CAS Number: 149845-06-7
  • MF: C39H54N6O8S
  • MW: 766.946
  • Catalog: HIV
  • Density: N/A
  • Boiling Point: 1015ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 567.7ºC

TC-E 5005

TC-E 5005 is a potent and selective PDE10A inhibitor with IC50 values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate[1].

  • CAS Number: 959705-64-7
  • MF: C15H18N4O
  • MW: 270.33000
  • Catalog: Phosphodiesterase (PDE)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

22-alpha-Hydroxy Cholesterol

22(R)-Hydroxycholesterol (Narthesterol) is an endogenous LXR agonist. 22(R)-Hydroxycholesterol (Narthesterol) can be used for tangier disease research[1].

  • CAS Number: 17954-98-2
  • MF: C27H46O2
  • MW: 402.65
  • Catalog: LXR
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 513.1±23.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 213.5±17.2 °C

Deoxyarbutin

Deoxyarbutin is a new effective lighten ingredient, can effectively inhibit tyrosinase activity and melanin synthesis to get significant and lasting lightening effect.

  • CAS Number: 53936-56-4
  • MF: C11H14O3
  • MW: 194.227
  • Catalog: Tyrosinase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 349.8±32.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 165.3±25.1 °C

AQX-016A

AQX-016A is an orally active and potent SHIP1 agonist. AQX-016A can activate recombinant SHIP1 enzyme in vitro and stimulate SHIP1 activity. AQX-016A also can inhibit the PI3K pathway and TNFa production, can be useful for various inflammatory diseases research[1][2].

  • CAS Number: 849669-54-1
  • MF: C22H32O2
  • MW: 328.49
  • Catalog: Phosphatase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dimethyl-bisphenol A

Dimethyl-bisphenol A (DMBPA) is a potent HIF-1α inhibitor. Dimethyl-bisphenol A can decrease Vegfa mRNA expression[1].

  • CAS Number: 1568-83-8
  • MF: C17H20O2
  • MW: 256.34
  • Catalog: HIF/HIF Prolyl-Hydroxylase
  • Density: 1.022g/cm3
  • Boiling Point: 364.8ºC at 760 mmHg
  • Melting Point: 54-59ºC
  • Flash Point: 136.3ºC

HM03

HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity[1].

  • CAS Number: 500565-15-1
  • MF: C26H27ClN4O2
  • MW: 499.43200
  • Catalog: HSP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Isolindleyin

Isolindleyin, a butyrophenone, is a tyrosinase inhibitor, with a Kd of 54.8 μM for human tyrosinase. Isolindleyin exhibits anti-inflammatory, analgesic and anti-melanogenic activities[1].

  • CAS Number: 87075-18-1
  • MF: C23H26O11
  • MW: 478.44600
  • Catalog: Tyrosinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CCT129957

CCT129957 is an indole derivative and a potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of ~3 μM and a GC50 of 15 μM. CCT129957 inhibits Ca2+ release in squamous carcinoma cells at ~15 μM[1][2].

  • CAS Number: 883098-58-6
  • MF: C17H15N3O3
  • MW: 309.32
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tarenflurbil

Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM.

  • CAS Number: 51543-40-9
  • MF: C15H13FO2
  • MW: 244.261
  • Catalog: RAR/RXR
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 376.2±30.0 °C at 760 mmHg
  • Melting Point: 110-113ºC
  • Flash Point: 181.3±24.6 °C

Fidarestat

Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease.

  • CAS Number: 136087-85-9
  • MF: C12H10FN3O4
  • MW: 279.224
  • Catalog: Aldose Reductase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DHODH-IN-5

DHODH-IN-5 is a potent human dihydroorotate dehydrogenase (DHODH) inhibitor, with a pIC50 of 7.8 for human recombinant DHODH. DHODH-IN-5 inhibits measles virus replication, with a pMIC50 of 8.8[1].

  • CAS Number: 1644156-56-8
  • MF: C21H24N4O2
  • MW: 364.44
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ML-​226

ML226 is a potent α/β hydrolase domain-containing protein 11 (ABHD11) inhibitor in vitro and in situ with IC50s of 15 and 0.68 nM, respectively[1].

  • CAS Number: 2055172-43-3
  • MF: C23H26N4O2
  • MW: 390.478
  • Catalog: MAGL
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 576.8±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 302.7±27.9 °C