Home > Inhibitors & Agonists > Metabolic Enzyme/Protease
Cat. No. Product name CAS No.
DC72370 VM4-037

VM4-037 can be used for the synthesis of VM4-037(18F). VM4-037(18F) is a fluorinated PET imaging agent for carbonic anhydrase IX.

1071470-72-8
DC72371 Tiprelestat

Tiprelestat is a potent human neutrophil elastase inhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease.

820211-82-3
DC72372 DP00477

DP00477 is a potent IDO1 (indoleamine 2,3-dioxygenase 1) inhibitor with an IC50 value of 7.0 µM. DP00477 has the potential for the research of cancer.

169120-56-3
DC72373 ZC0109

ZC0109 is a dual inhibitor of IDO1 and thioredoxin reductase 1 (TrxR1) with IC50s of 50 nM and 3.0 μM, respectively. ZC0109 induces ROS accumulation and cell cycle arrest at G1/S phase, thus leads to cancer cells Apoptosis.

DC72374 (S,S)-GSK321

(S,S)-GSK321 is a (S,S)-enantiomer of GSK321.

1816272-20-4
DC72375 2-TEDC

2-TEDC is a potent inhibitor of 5-, 12-, and 15-lipoxygenase with IC50 values of 0.09 μM, 0.013 μM and 0.5 μM, respectively. 2-TEDC can be used for the research of atheroscrelosi.

132465-10-2
DC72376 PF-03049423 free base

PF-03049423 (Compound PF-5) free base is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 free base can be used for the research of acute ischaemic stroke.

954138-07-9
DC72377 Deltasonamide 1 TFA

Deltasonamide 1 TFA is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors.

2235358-73-1
DC72378 Enalkiren

Enalkiren (A-64662) is a potent dipeptide renin inhibitor with an IC50 of 0.78 nM in a purified renal renin-angiotensinogen system (pH=6.0). Enalkiren suppresses renin activity, and also reduces systolic and diastolic blood pressure. Enalkiren can be used to research essential hypertension.

113082-98-7
DC72379 Flovagatran

Flovagatran (TGN 255) is a potent and reversible thrombin inhibitor (Ki: 9 nM). Flovagatran can be used in the research of arterial and venous thrombosis.

871576-03-3
DC72380 Lucidal

Lucidal (Lucialdehyde C) is a natural lanostante-type triterpene aldehyde that shows inhibitory effects against α-glucosidase (Glucosidase) with an IC50 of 0.635 mM. Lucidal has anticancer and antidiabetic effects.

252351-96-5
DC72381 α-Demethylnaproxen

α-Demethylnaproxen is the major metabolite of Nabumetone, Nabumetone is an orally active COX-2 inhibitor with anti-inflammatory activity.

23981-47-7
DC72382 Abiraterone N-oxide

Abiraterone N-oxide is a metabolite of Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity.

2378463-76-2
DC72383 Abiraterone sulfate

Abiraterone sulfate is a metabolite of Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity.

1993430-25-3
DC72384 Ulodesine

Ulodesine is a purine nucleoside phosphorylase (PNP) inhibitor. Ulodesine inhibits PNP with IC50 value of 2.293 nM/L. Ulodesine can be used for the research of hyporucicemia.

548486-59-5
DC72385 4-Hydroxyphenyl acetate

4-Hydroxyphenyl acetate (4-HPA) is a natural antioxidant and protects cells from oxidative stress-induced necrosis. 4-Hydroxyphenyl acetate blocks the increase of cellular ROS induced by oxidative stress, and up-regulates NQO1 and HO-1 genes by stabilizing and inducing the nuclear translocation of NRF2 transcription factor.

3233-32-7
DC72386 MAHMA NONOate

MAHMA NONOate is a NO donor. MAHMA NONOate effectively inhibits platelet aggregation induced by either collagen or ADP.

146724-86-9
DC72387 PAPA NONOate

PAPA NONOate is a NO donor with a NO release half-life of 77 min (22-25°C). PAPA NONOate may represent a potential treatment for impaired wound healing in diabetes by increasing the rate of collagen synthesis at the wound site.

146672-58-4
DC72388 Virodhamine

Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1 receptor and an agonist of CB2 receptor. Virodhamine induces megakaryocytic differentiation by triggering MAPK signaling and ROS production. Virodhamine can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases.

287937-12-6
DC72389 15(S)-HETE

15(S)-HETE is an endogenous metabolite present in Urine that can be used for the research of Zellweger Syndrome.

54845-95-3
DC72390 3-Hydroxysebacic acid

3-Hydroxysebacic acid is an endogenous metabolite present in Urine that can be used for the research of Medium Chain Acyl Co A Dehydrogenase Deficiency.

73141-46-5
DC72391 5(S)-HETE

5(S)-HETE is an endogenous metabolite present in Blood that can be used for the research of Rheumatoid Arthritis, Rhinitis and Asthma.

70608-72-9
DC72392 Deoxypyridinoline

Deoxypyridinoline is an endogenous metabolite present in Urine that can be used for the research of Heart Failure.

83462-55-9
DC72393 D-Glyceric acid

D-Glyceric acid is an endogenous metabolite present in Urine that can be used for the research of Primary hyperoxaluria Type I and Glutaric Acidemia Type 2.

6000-40-4
DC72394 GDP-L-fucose

GDP-L-fucose is a nucleotide sugar that is a key substrate for the biosynthesis of fucose oligosaccharides, providing the fucose moiety for the oligosaccharides.The formation of GDP-L-fucose occurs through two pathways, the major ab initio metabolic pathway and the minor remedial metabolic pathway.

15839-70-0
DC72395 Hexanoylglycine

Hexanoylglycine is an endogenous metabolite present in Urine that can be used for the research of Ethylmalonic Encephalopathy.

24003-67-6
DC72396 Tetracosanoyl-sulfatide

Tetracosanoyl-sulfatide is an endogenous metabolite present in Urine that can be used for the research of Mild Metachromatic Leukodystrophy.

151122-71-3
DC72397 9AzNue5Ac

9AzNue5Ac, 9-azido-9-deoxy-N-acetylneuraminic acid, is a click chemistry reagent and a Neu5Ac analogue with the substitution of 9-hydroxyl group with an azide. 9AzNue5Ac could be metabolized and incorporated into sialoglycans in living cells and mice. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity.

76487-51-9
DC72398 L-Cysteine S-sulfate sodium hydrate

L-Cysteine S-sulfate sodium hydrate is a potent N-methyl-d-aspartate (NMDA) glutamatergic receptors agonist. L-Cysteine S-sulfate sodium hydrate is the substrate for cystine lyase, it can be used in mass spectrometry operations.

150465-29-5
DC72399 Acetoacetic acid

Acetoacetic acid is an endogenous metabolite present in Cerebrospinal_Fluid and Blood that can be used for the research of Meningitis, Pregnancy, 3 Hydroxy 3 Methylglutaryl CoA Lyase Deficiency, Preeclampsia/Eclampsia, Diabetes Mellitus Type 2, Glucose Transporter Type 1 Deficiency Syndrome and Succinyl CoA:3 Oxoacid CoA Transferase Deficiency.

541-50-4
DC72400 D-Fructose-6-phosphate

D-Fructose 6-phosphate is an endogenous metabolite present in Saliva that can be used for the research of Lewy Body Dementia.

643-13-0
DC72401 D-Ribofuranose

D-Ribofuranose (D-Ribose) is an endogenous metabolite present in Cerebrospinal_Fluid that can be used for the research of Ribose 5 Phosphate Isomerase Deficiency and Medium Chain Acyl Co A Dehydrogenase Deficiency.

613-83-2
DC72402 Estrone sulfate

Estrone sulfate is an endogenous metabolite present in Blood that can be used for the research of X-Linked Ichthyosis and Obesity.

481-97-0
DC72403 Isocitric acid

Isocitric acid is an endogenous metabolite present in Saliva and Cellular_Cytoplasm that can be used for the research of Alzheimer's Disease, Lewy Body Dementia and Anoxia.

320-77-4
DC72404 L-Xylulose

L-Xylulose is an endogenous metabolite present in Blood, Cerebrospinal_Fluid and Urine that can be used for the research of Ribose 5 Phosphate Isomerase Deficiency.

527-50-4
DC72405 N1-Acetylspermine

N1-Acetylspermine is an endogenous metabolite present in Urine that can be used for the research of Leukemia.

25593-72-0
DC72406 Normetanephrine

Normetanephrine is an endogenous metabolite present in Cerebrospinal_Fluid that can be used for the research of Hypertension.

97-31-4
DC72407 Phytanic acid

Phytanic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Alpha Methylacyl CoA Racemase Deficiency, Rhizomelic Chondrodysplasia Punctata and Infantile Refsum Disease.

14721-66-5
DC72408 Pristanic acid

Pristanic acid is an endogenous metabolite present in Blood that can be used for the research of Alpha Methylacyl CoA Racemase Deficiency and Zellweger Syndrome.

1189-37-3
DC72409 AAF-CMK

AAF-CMK is a TPPII (tripeptidylpeptidase II) inhibitor, shows anti-tumor activity and induces apoptosis. AAF-CMK can be used in leukemia research.

102129-66-8
DC72410 Ac-Phe-Gly-pNA

Ac-Phe-Gly-pNA is the chymotrypsin specific substrate.

34336-99-7
DC72531 ICeD-2 Featured

ICeD-2 is a inducer of cell death, can induce HIV-1 infected cell kill. ICeD-2-mediated HIV-1 infected cell kill is dependent on HIV-1 protease activity. ICeD-2 potently blocks hydrolysis of Gly-Pro-AMC by dipeptidyl peptidase DPP8 and DPP9. ICeD-2 shows strong stabilization of DPP9 in PBMCs.

DC72662 18β-Glycyrrhetyl-3-O-sulfate

18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)) is a potent type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) inhibitor with an IC50 of 0.10 µM using rat kidney microsome. 18β-Glycyrrhetyl-3-O-sulfate is the major metabolite of Glycyrrhetinic acid (GA). 18β-Glycyrrhetyl-3-O-sulfate is the substrate of organic anion transporter (OAT) 1 and OAT3. 18β-Glycyrrhetyl-3-O-sulfate has anti-inflammatory effects and has the potential for pseudohyperaldosteronism research.

10251-38-4
DC72663 SW222746 Featured

SW222746 (SW 222746) is a potent selective, orally active inhibitor of 15-Prostaglandin dehydrogenase (15-PGDH) with IC50 of 3 nM.

2241676-74-2
DC72664 Bradykinin potentiator C

Bradykinin potentiator C is a potent angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 7.1 μM for rabbit lung ACE. Bradykinin potentiator C is a postulated prototype of functional peptide.

30953-20-9
DC72665 ASPER-29

ASPER-29 is Asperphenamate analog. ASPER-29 also is a dual cathepsin L and S inhibitor with IC50 value of 6.03 μM and 5.02 μM, respectively. ASPER-29 can be used for the research of the migration and invasion of cancer.

2630388-03-1
DC72666 BMS-820132 Featured

BMS-820132 (BMS 820132) is potent, selective, partial glucokinase (GK) activator with AC50 of 29 nM.

1001419-18-6
DC72667 CAY10581

CAY10581, a pyranonaphthoquinone derivative, is a highly specific and reversible uncompetitive IDO Inhibitor with an IC50 of 55 nM.

1018340-07-2
DC72668 Etazolate hydrochloride

Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.

35838-58-5
DC72669 PAT-347

PAT-347 is an Autotaxin (ATX) inhibitor. ATX is a secretory enzyme that hydrolyzes lysophosphatidylcholine (LPC) and regulates lysophosphatidic acid (LPA) production in the blood.

1689554-51-5
DC72670 EA4

EA4, a derivative of quinone, is an inhibitor for both rPLA and cPLA. EA4 can inhibit rPLA2 with a Ki value of 130 μM. EA4 can be used for the research of hemostasis, thrombosis, and erythropoiesis.

389614-94-2
DC72671 AMP-Deoxynojirimycin

AMP-Deoxynojirimycin (AMP-DNM) is a potent ceramide glucosyltransferase and GCase 2 inhibitor. AMP-Deoxynojirimycin also is a GlcCer biosynthesis inhibitor.

216758-20-2
DC72672 7-Hydroxymethotrexate-d3

7-Hydroxymethotrexate-d3 is the deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate. Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.

432545-62-5
DC72673 Acetyl coenzyme A trilithium

Acetyl-coenzyme A (Acetyl-CoA) trilithium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A trilithium regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A trilithium is also a key precursor of lipid synthesis.

75520-41-1
DC72674 Saccharopine hydrochloride

Saccharopine (L-Saccharopine) hydrochloride, a lysine degradation intermediate, is a mitochondrial toxin. Lysine and α-ketoglutarate are converted into Saccharopine hydrochloride by the lysine-ketoglutarate reductase. Saccharopine hydrochloride is then oxidized to α-aminoapidate semialdehyde and glutamate by the saccharopine dehydrogenase. Saccharopine hydrochloride impairs development by disrupting mitochondrial homeostasis.

DC72675 TRH Precursor Peptide

TRH Precursor Peptide is a precursor peptide of thyrotropin-releasing hormone (TRH). TRH Precursor Peptide formation of TRH in rat brain and pituitary is zinc-dependent.

128578-17-6
DC72676 Mannose 1-phosphate

Mannose 1-phosphate is an endogenous metabolite. Mannose 1-phosphate can be used to synthesize GDP-Man by the enzyme GDP-mannose pyrophosphorylase.

27251-84-9
DC72677 Galactonic acid

Galactonic acid is a sugar acid that is a metabolic breakdown product of galactose. Galactose dehydrogenase is responsible for converting galactose to galactonolactone, which then spontaneously or enzymatically converts to galactonic acid.

13382-27-9
DC72678 UDP-Galactose

UDP-Galactose is a monosaccharide involved in nucleotide sugar metabolism. UDP-Galactose and its derivatives act as a natural agonist for Gi protein-conjugated P2Y14 receptors in the immune system (IC50=0.67 μM, hP2Y14).

2956-16-3
DC72679 Metanephrine

Metanephrine is the O-methylated metabolite of epinephrine that can be used for the research of diagnosis of pheochromocytoma.

5001-33-2
DC72680 PPACK II diTFA

PPACK II diTFA is an irreversible and specific glandular and plasma kallikreins inhibitor.

649748-23-2
DC72681 SPC4061

SPC4061 an antisense nucleotide, is a potent PCSK9 inhibitor. SPC4061 targets the lock-in nucleic acid (LNA) of PCSK9 for the study of hypercholesterolemia and related diseases.

1018108-22-9
DC72785 TP0597850 Featured

TP0597850 is a selective inhibitor of MMP2 (IC50=0.22 nM). TP0597850 has a long MMP2 dissociation half-life (t1/2=265 min).

2642181-22-2
DC72786 cis-ACCP

cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases.

777075-44-2
DC72787 Cimoxatone

Cimoxatone (MD 780515) is a reversible, selectively and orally active type A monoamine oxidase (MAO-A) inhibitor. Cimoxatone enhances the anorectic action of Serotonin.

73815-11-9
DC72789 JUN-1111

JUN-1111 is an irreversible and selective Cdc25 phosphatase inhibitor with IC50 values of 0.38, 1.8, 0.66, 28, 37 µM for Cdc25A, Cdc25B, Cdc25C, VHR, PTP1B, respectively. JUN-1111 induces cell cycle arrest at G1 and G2/M phases. JUN-1111 decreases the expression of phosphoCdk1.

874351-38-9
DC72790 HKB99

HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 inhibits the formation of invasive pseudopodia and increases the level of PAI-2 in vitro. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC).

2414908-90-8
DC72803 Neuraminic acid

Neuraminic acid is an acidic amino sugar with a backbone formed by nine carbon atoms. Neuraminic acid may also be visualized as the product of an aldol-condensation of pyruvic acid and D-mannosamine (2-amino-2-deoxy-mannose). Neuraminic acid is a functional group of some biologically active mucoproteins.

114-04-5
DC72818 INCB3619

INCB3619 is a selective and orally active ADAM inhibitor with IC50 of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity.

791826-72-7
DC72819 18-Hydroxycortisol

18-Hydroxycortisol is an endogenous steroid that secreted by the adrenal cortex. 18-Hydroxycortisol is a cortisol derivative and a steroidogenic intermediate. 18-Hydroxycortisol can be used for primary aldosteronism (PA) research.

86002-90-6
DC72840 Sitagliptin fenilalanil hydrochloride

Sitagliptin fenilalanil is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor.

1339954-75-4
DC72846 S-Allylmercapturic acid

S-Allylmercapturic acid is a biomarker of food intake (BFIs) for garlic consumption.

23127-41-5
DC72854 Vidofludimus hemicalcium

Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR.

1354012-90-0
DC72872 BDM88951

BDM88951 (BDM 88951) is a highly potent, selective inhibitor of endoplasmic reticulum aminopeptidase 2 (ERAP2) with IC50 of 19 nM. BDM88951 displays selectivity index (>150) towards closely related ERAP1 and IRAP enzymes, as well as MMPs, TACE and LAP3. BDM88951 is a potent inhibitor of ERAP2-mediated hydrolysis of two nonapeptides precursors of SIINFEKL, an ovalbumine-derived antigen, in a dose dependent manner. BDM88951 engage ERAP2 in cells and inhibits antigen presentation in a cellular context, also displays favorable in vitro ADME properties and in vivo exposure.

DC72892 MEHP Featured

MEHP (Phthalic acid mono-2-ethylexyl ester) is a competitive inhibitor of CYP2C9 with IC50 of 6.37 μM.

4376-20-9
DC72894 L 691816

L 691816 is a potent, selective and orally active inhibitors of 5-lipoxygenase. L 691816 can be used for the research of allergies and asthma.

150461-07-7
DC72899 Cytidine diphosphate

Cytidine diphosphate is a nucleoside diphosphate that acts as a carrier for phosphorylcholine, diacylglycerol, and other molecules during phospholipid synthesis.

63-38-7
DC72911 CHBO4 Featured

CHBO4 is a potent, reversible, competitive, and selective hMAO-B inhibitor with an IC50 value of 0.031 μM in CHBO subseries and an Ki value of 0.010 ± 0.005 μM. CHBO4 reduce cell damage by scavenging intracellular reactive oxygen species (ROS). CHBO4 can be used for Parkinson's Disease (PD) research.

98991-32-3
DC72914 UE2343

UE2343 (UE-2343, Xanamem) is a potent, orally bioavailable, brain penetrant 11β-HSD1 inhibitor with IC50 of 24 nM in cell-free assays, with no activity for isozyme 11β-HSD2.

1346013-80-6
DC73703 VP15 hydrochloride

VP15 hydrochloride (VP-15 HCl) is a BBB-penetrant, orally active, multitarget directed ligand against acetylcholine and monoamine oxidase enzymes with IC50 of 0.04 and 0.37 uM for AChE and MAO-B, respectively, >600-fold selectivity over BuChE.

DC73704 AD-5591 Featured

AD-5591 (AD5591) is a potent, selective, new generation small molecule ALDH2 activator, has the improved biological activities and pharmacological properties compared to Alda-1. AD-5591 (100  μM) significantly increases the enzymatic activity of recombinant WT and mutant human ALDH2 proteins. AD-5591 is the active form of AD-9308.

1804942-45-7
DC73705 AD-9308 Featured

AD-9308 is a water-soluble, orally bioavailable, potent, and highly selective ALDH2 activator, AD-9308 is a valine ester prodrug of a potent and selective small molecule ALDH2 activator AD-5591.

1804942-56-0
DC73706 ER-001135935

ER-001135935 is a potent selective inhibitor of aldehyde dehydrogenase family 1 member A3 (ALDH1A3) with IC50 of 64 nM, Ki value of 106 nM.

DC73707 KOTX1

KOTX1 is a potent, selective and reversible ALDH1A3 inhibitor with IC50 of 5.14 nM by Aldefluor assay in A375 cells.

1788963-83-6
DC73708 LEI-945

LEI-945 (LEI 945) is a first-in-class probe that enables profiling retinaldehyde dehydrogenases (ALDHs) in cancer cells.

2582758-03-8
DC73709 NCT-507

NCT-507 (NCT507) is a potent, selective, orally available ALDH1A1 inhibitor with IC50 of 7 nM (hALDH1A1), exhibits high specificity over other ALDH isozymes and unrelated dehydrogenases.

DC73710 STA-55

STA-55 is a broad-spectrum activity-based probe of aldehyde dehydrogenase family, can be used to identify therapy resistance biomarkers in cancer and to validate target engagement of ALDH drug candidates.

2451093-96-0
DC73711 BAY1128688

BAY1128688 is a potent, steroidal aldo-keto reductase 1C3 (AKR1C3) inhibitor with potential for endometriosis.

1428988-21-9
DC73712 Imirestat

Imirestat (AL-1576) is a potent aldose reductase inhibitor with IC50 of 8.5 nM for rat lens aldose reductase, with similar IC50 value for the human placental enzyme, shows high affinity for AKR1A1 and AKR1B1 with Ki of 47 and 46 nM respectively.

89391-50-4
DC73713 DG013A

DG013A (DG 013A) is tripeptide mimetic chemical probe (inhibitor) of ERAP1 with IC50 of 0.19 uM, 15-fold selectivity over ERAP2, potently inhibits aminopeptidase N (APN) with IC50 of 3.7 nM.

2007955-07-7
DC73714 AZD0011

AZD0011 (AZD-0011) a novel peptidic boronic acid prodrug of AZD0011-PL, highly potent and orally available Arginase (ARG) inhibitor with IC50 of 404/308 nM for ARG1/2, respectively.

2374807-41-5
DC73715 AZD0011-PL

AZD0011-PL is a highly potent Arginase (ARG) inhibitor with IC50 of 7/15 nM for ARG1/2, respectively.

2374807-39-1
DC73716 ALLM

ALLM (Ac-Leu-Leu-Met-CHO) is a potent, cell-permeable calpain inhibitor with Ki of 0.6 and 100 nM for calpain L and calpain B, respectively.

136632-32-1
DC73717 NA-184

NA-184 is a potent, selective calpain-2 inhibitor with Ki of 50 nM (human calpain-2) and IC50 of 134 nM (mouse calpain-2).

2688119-39-1
DC73718 Dutacatib

Dutacatib (AFG495) is potent, selective and non-covalent cathepsin K inhibitor with IC50 of 3-6 nM (human CatK), shows excellent selectivity profile versus human cathepsins L and S.

501000-36-8
DC73719 MK-1256

MK-1256 (MK1256) is a potent, selective cathepsin K (Cat K) inhibitor with IC50 of 0.62 nM, >1100-fold selectivity over Cat B, L, S, C, H, Z, and V, 110-fold over Cat F.

919109-76-5
DC73720 Z-Tyr-Ala-CHN2

Z-Tyr-Ala-CHN2 is a potent cathepsin L inhibitor with EC50 of <50 nM, has broad-spectrum coronavirus antiviral activity.

114515-99-0
DC73721 BMS-737

BMS-737 (BMS737) is a potent, , selective, non-steroidal, reversible inhibitor of CYP17 lyase, 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase.

1356053-63-8
DC73722 DLCI-1

DLCI-1 is a potent and selective CYP2A6 inhibitor with IC50 of 17 nM, 15-765-fold selectivity other major hepatic CYP enzymes.

2244569-14-8
DC73723 DLCI-1 dihydrochloride

DLCI-1 dihydrochloride is a potent and selective CYP2A6 inhibitor with IC50 of 17 nM, 15-765-fold selectivity other major hepatic CYP enzymes.

2244569-15-9
DC73724 ODM-208

ODM-208 (ODM208) is a potent, selective, orally bioavailable CYP11A1 inhibitor, inhibits the biosynthesis of pregnenolone with IC50 of 15 nM in NCI-H295R cells.

2231294-96-3
DC73725 ODM-209

ODM-209 (ODM209) is a potent, selective, orally bioavailable inhibitor of CYP11A1 (cholesterol side-chain cleavage enzyme) with potential antineoplastic activity, inhibits the biosynthesis of pregnenolone.

2231294-95-2
DC73726 TPP-IOA

TPP-IOA is a specific inhibitor of cytochrome c (cyt c) peroxidase activity, inhibits peroxidase activity of cardiolipin-induced cytochrome c peroxidase activity with IC50 of 5 uM.

1423018-61-4
DC73727 AZD7687

AZD7687 (AZD-7687) is a potent, selective DGAT1 inhibitor with IC50 of 80 nM (hDGAT1), >400-fold selectivity over hACAT1.

1166827-44-6
DC73728 TP-020

TP-020 is a potent, selective, orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.

1800025-30-2
DC73729 AX8819

AX8819 is a potent, specific DPP-2 inhibitor with IC50 of 0.88 nM, highly selective for DPP II over all of the other DPP enzymes.

928161-33-5
DC73730 ICeD-1

ICeD-1 is a potent DPP9 inhibitor capable of killing HIV-1 infected peripheral blood mononuclear cells, activates the caspase recruitment domain family member 8 (CARD8) inflammasome.

752977-19-8
DC73731 TEI-8362

TEI-8362 is a potent, selective inhibitor of human neutrophil elastase (HNE) with Ki value of 1.38 nM and IC50 of 1.9 nM.

180154-57-8
DC73732 ARN15381

ARN15381 is a potent, multitarget FAAH inhibitor/D3 partial agonist with low nanomolar range activity, decreases nicotine self-administration in male rats.

2650065-24-8
DC73733 UCM1341

UCM1341 (UCM 1341) is a bivalent ligand with melatonin receptor agonist (hMT1/hMT2, pKi=9.11/8.77) and fatty acid amide hydrolase (FAAH) inhibitory activity (rFAAH IC5=0.85 nM).

2244611-73-0
DC73734 Fasnall benzenesulfonate

Fasnall benzenesulfonate is a potent, selective fatty acid synthase (FASN) inhibitor with IC50 of 3.71 uM for purified human FASN isolated from the BT474 cell line.

2187367-11-7
DC73735 FASstatin

FASstatin (FASNi-8) is an orally bioavailable small-molecule inhibitor of fatty acid synthase (FASN), directly binds FASN with SPR KD of 16 uM, potentiates TRIM56-mediated FASN ubiquitination.

1047504-12-0
DC73736 NJNU-0069

NJNU-0069 is a specific small-molecule inducer of major histocompatibility complex class II (MHC-II), directly binds to the MAT domain of FASN (Kd=32.1 uM).

DC73737 NJNU-0069-003

NJNU-0069-003 is a specific small-molecule inducer of major histocompatibility complex class II (MHC-II), directly binds to the MAT domain of FASN with Kd of 7.98 uM.

DC73738 GKA23

GKA23 is a potent, small molecule glucokinase (GK) activator with EC50 of 152 nM for glucokinase activation in 5 mM glucose, increases glucose uptake in primary rat hepatocytes with EC50 of 201 nM.

1138675-60-1
DC73739 GKM-001

GKM-001 is a potent, liver-selective small molecule activator of glucokinase (GKA), demonstrates glucose lowering effect without hypoglycemia in normal and type II diabetes mellitus (T2DM).

1092375-28-4
DC73740 TMG-123

TMG-123 (TMG123) is a potent small molecule activator of glucokinase (GK) with EC50 of 0.35 and 0.32 uM for human liver and pancreas GK, respectively.

1193394-53-4
DC73741 MZ-101 Featured

MZ-101 is a potent, selective inhibitor of glycogen synthase 1 (GYS1) with IC50 of 41 nM (human GYS1), with no inhibition against GYS2.

2839908-40-4
DC73743 SRK2128

SRK2128 (SRK 2128) is a highly potent HMG-CoA reductase degrader with EC50 of 84 nM, potently induce degradation of HMG-CoA reductase.

2601455-20-1
DC73744 ADAM9i

ADAM9i is a specific small molecule inhibitor of ADAM9 protein with binding KD of 5.9 uM and enzyme IC50 of 5.2 uM, promotes the selective degradation of KRAS and sensitizes pancreatic cancers to chemotherapy.

860786-85-2
DC73745 AZD1236

AZD1236 is a potent, selective MMP-9 and MMP-12 inhibitor with IC50 of 4.5 and 6.1 nM respectively, >10-fold selectivity to MMP-2 and MMP-13 and >350-fold selectivity to other MMPs.

459814-89-2
DC73746 BAY-9835 Featured

BAY-9835 is the first orally bioavailable ADAMTS7 inhibitor with IC50 of 6 nM, which is selective against a range of off-targets and metalloproteases except for ADAMTS12.

2644738-11-2
DC73747 CID 3117694

CID 3117694 is a selective, non-competitive inhibitor of ADAM10 with IC50 of 1.1 uM, does not inhibit ADAM17.

331636-31-8
DC73748 IPR-179

IPR-179 (ACT-03) is a potent, BBB-permeable, selective gelatinase (MMP2 and MMP9) inhibitor with IC50 of 656 nM and 310 nM, respectively.

2098556-70-6
DC73749 JTP-96193

JTP-96193 (JTP96193) is a potent, selective TNF-α converting enzyme (TACE/ADAM17) inhibitor with IC50 of 5.4 nM, >1800-fold selectivity against ADAM10.

1016257-48-9
DC73750 MMP118

MMP118 is a potent, selective and orally bioavailable matrix metalloproteinase-12 (MMP-12) inhibitor with IC50 of 1.0 nM (hMMP-12), 1980- and 154-fold selectivity over MMP-13 and MMP-8 respectively.

1080637-90-6
DC73751 MMP408

MMP408 (MMP 408) is a potent, selective matrix metalloprotease 12 (MMP-12) inhibitor with IC50 of 2.0 nM (human MMP-12), 60-fold selectivity over MMP-13.

1258003-93-8
DC73752 TAPI-0

TAPI-0 is a potent, selective inhibitor of TNFalpha converting enzyme (TACE, ADAM7) with IC50 of 100 nM.

163958-73-4
DC73753 TP0628103

TP0628103 is a highly potent, selective matrix metalloproteinase-7 (MMP-7) inhibitor with IC50 of 0.17 nM and 4.1 nM for human and mouse MMP-7, respectively.

2865102-08-3
DC73754 AKU-005

AKU-005 is a potent, dual MAGL/FAAH inhibitor with IC50 of 589 and 309 pM for MAGL in rat and mouse brain membrane respectively, inhibits rat and human FAAH with IC50 of 63 and 389 nM.

1515855-85-2
DC73755 GLX481304

GLX481304 is a specific small molecule inhibitor of Nox2 and Nox4 with IC50 values of 1.25 uM, shows negligible effects on Nox1.

701224-63-7
DC73756 LMH001

LMH001 is a small chemical compound blocking phosphorylated p47phox interaction with p22phox, inhibits effectively angiotensin II (AngII)-induced endothelial Nox2 activation and superoxide production (IC50=0.25 uM).

1427434-81-8
DC73757 NCATS-SM7270

NCATS-SM7270 is a specific small molecule NADPH oxidase 2 (NOX2) inhibitor with IC50 of 2.1 uM (Polymorphonuclear leukocytes, PMN), inhibits NOX2 in primary human and mouse granulocytes.

DC73758 TIPTP

TIPTP is a highly potent and selective inhibitor of p22phox, inhibits the p22phox-Rubicon interaction with IC50 of 0.1 uM, and suppresses ROS-mediated inflammation.

2413675-03-1
DC73759 A4276

A4276 is a novel orally bioavailable NAMPT inhibitor with IC50 of 492 nM for inhibiting NAMPT enzymatic activity, shows high selectivity for NAPRT-deficient lung cancer cell lines.

896661-48-6
DC73760 MM201

MM201 is a novel potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with IC50 of 74.3 nM in in vitro biochemical assays.

2109584-00-9
DC73761 NAMPT activator (NAT) Featured

NAMPT activator (NAT) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 500 nM.

831243-31-3
DC73763 CC-11050

Dovramilast (CC-11050) is a potent and orally active phosphodiesterase 4 (PDE4) inhibitor, CC-11050 is a promising candidate for host directed therapy of patients with pulmonary TB.

340019-69-4
DC73764 CRD733 Featured

CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.

917089-10-2
DC73765 Gemlapodect

Gemlapodect (NOE-105) is a potent, selective PDE10A inhibitor with a potential therapeutic effect for the treatment of COFD.

1380329-87-2
DC73766 MCI-030

MCI-030 (ADT 061) is a potent, selective PDE10 inhibitor, inhibits recombinant PDE10 using cGMP as a substrate with IC50 of 0.3 uM.

2700025-84-7
DC73767 ME3183

ME3183 is a potent, selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 2.33, 1.28 and 1.63 nM for PDE4B1, PDE4A1A and PDE4D2 respectively.

2231329-25-0
DC73768 PF-2545920 hydrochloride

A potent and selective PDE10A inhibitor with IC50 of 0.37 nM.

DC73769 TOP-N53

TOP-N53 is a dual-acting nitric oxide (NO) donor and selective PDE5 inhibitor, potently inhibits PDE5 with IC50 of 1.6 nM.

2098499-23-9
DC73770 TPN171

TPN171 (TPN-171) is a highly potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 0.62 nM, 32-fold selectivity over PDE6.

1229018-87-4
DC73771 Yonkenafil

Yonkenafil is a potent, selective PDE5 inhibitor with IC50 of 2.0 nM.

804518-63-6
DC73772 ABD298

ABD298 is a potent, selective ABHD13 inhibitor, inhibits HEK293T cells expressing recombinant mouse ABHD13 with IC50 of 0.98 uM.

DC73773 KT-203

KT-203 (KT203) is a potent, selective inhibitor of α/β-hydrolase domain 6 (ABHD6) with IC50 of 3.9 nM in 2-AG hydrolysis assays.

1402612-64-9
DC73774 VU533

VU533 is a small molecule activator of N-acyl-phosphatidylethanolamine hydrolyzing phospholipase D (NAPE-PLD) with EC50 of 0.3 uM, enhances efferocytosis by macrophages.

923417-09-8
DC73775 VU534

VU534 is a small molecule activator of N-acyl-phosphatidylethanolamine hydrolyzing phospholipase D (NAPE-PLD) with EC50 of 0.3 uM, enhances efferocytosis by macrophages.

923509-20-0
DC73776 IPR-3011

IPR3011 is a small-molecule uPAR-uPA protein-protein interaction inhibitor with Ki of 2.4 uM.

1031631-29-4
DC73777 WX-293

WX-293 is a highly selective small-molecule inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 2.4 uM.

282718-42-7
DC73778 WX-340

WX-340 is a highly specific and selective, peptidic cyclic competitive inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 12 and 170 nM for human and mouse uPA, respectively, inhibit 10 Units of human uPA with IC50 of 90 nM.

DC73779 GSK-199

GSK-199 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 250 nM in FP binding assay (0.2 mM Ca), 200 nM in PAD4 NH3 release inhibition assay.

1549810-81-2
DC73780 JBI-589

JBI-589 (JBI589) is potent, selective, orally active PAD4 small molecule inhibitor, reduces CXCR2 expression and blocks neutrophil chemotaxis.

2308504-22-3
DC73781 ML325

ML325 (ML 325) is a potent, irreversible pan-protein arginine deiminase (PAD) inhibitor with IC50 of 70 nM, 200 nM 170 nM, and 240 nM for PAD1, 2, 3, and 4 in vitro respectively.

110144-34-8
DC73782 ATUX-1215

ATUX-1215 is a direct, orally active small molecule activator of protein phosphatase 2A (PP2A), suppresses bleomycin-induced fibrosis in vivo.

2910930-01-5
DC73783 ATUX-792

ATUX-792 is a small molecule activator of protein phosphatase 2A (PP2A), decreases survival, proliferation, and motility of neuroblastoma in vitro and tumor growth in vivo.

2088956-21-0
DC73784 CNBCA

CNBCA is a selective, competitive inhibitor of Src homology phosphotyrosyl phosphatase 2 (SHP2) with IC50 of 0.87 uM, effectively suppresses breast cancer cell phenotypes.

DC73785 DS-1211

DS-1211 (DS1211) is a potent, selecitve inhibitor of tissue-nonspecific alkaline phosphatase (TNAP) with IC50 of 3.4 nM.

2062664-81-5
DC73786 HN252

HN252 is a potent protein phosphatase 1B (PPM1B) inhibitor with Ki of 0.52 uM and IC50 of 0.76 uM, shows no inhibition against topoisomerases in vitro.

DC73787 JAB-3068

JAB-3068 (JAB3068) is a potent, selective and orally bioavailable allosteric inhibitor of SHP2.

2169223-48-5
DC73788 K161

K161 is a potent, pan-SHIP1/2 inhibitor with IC50 of 1.5- 6 uM and 6.5-13 uM, respectively.

2396446-12-9
DC73789 K306

K306 is a specific, small molecule agonist of SH2-containing 5' inositol phosphatase 1 (SHIP1) with EC50 of 119 nM, 10-fold higher selectivity over SHIP2.

1184987-29-8
DC73790 NGD61181

NGD61181 is a pyrazole-based SHIP2 inhibitor, has micromolar binding affinity and inhibitory activity, does not contain a phosphatase “warhead,” binds the active site of SHIP2.

1266401-14-2
DC73791 NSC49L

NSC49L (NSC30049) is a small molecule agonist (activator) of protein phosphatase 2A (PP2A), specifically stimulates PP2A-Cα activity with Kact of 14 nM, downregulates the AKT1/mTOR/4EBP1-axis, and inhibits p21 translation.

64401-41-8
DC73792 NSC74429 Featured

NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.

7255-94-9
DC73793 SBI-221

SBI-221 is a small molecule inhihitor of SHP2-E76K mutant with IC50 of 2.1 uM and 7.4 uM for SHP2-E76K and SHP2-WT in isothermal CETSA assays, respectively.

1840947-78-5
DC73794 SBI-668

SBI-668 is a selective inhihitor of SHP2-E76K mutant with IC50 of 2.1 uM in isothermal CETSA assays, 7-fold selectivity over SHP2-WT (IC50=15 uM).

DC73795 Sanofi-14h

Sanofi-14h is a selective inhibitor of the AGC family kinase SGK3, blocks DMXAA-stimulated IRF3-promoter activity with IC50 of 1.73 uM, inhibits IFNβ production under STING stimulation.

1426214-64-3
DC73796 (R)-SW203668

(R)-SW203668 (SCD inhibitor (R)-27) is a potent, tumor-specific, irreversible stearoyl CoA desaturase (SCD) inhibitor with high sensitity to H2122 cell (IC50=11 nM).

1673558-51-4
DC73797 TPT-004

TPT-004 is a highly potent, selective tryptophan hydroxylase (TPH) with IC50 of 77 nM and 16 nM for TPH1 and TPH2, respectively.

DC74592 DL-Thiorphan

Thiorphan (DL-3-Mercapto-2-benzylpropanoylglycine) is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM. It is also a potent inhibitor of enkephalinase, with antinociceptive activity.

76721-89-6
DC74593 ACT001(DMAMCL)

ACT001(DMAMCL, dimethylaminomicheliolide) is a PAI-1 inhibitor and exerts antitumor effects on neuroblastoma (NB) both in vitro and in vivo. It also exerts synergistic effects in combination with cisplatin through the inhibition of the PAI-1/PI3K/AKT pathway.

1403357-81-2
DC74620 OATD-02

OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study.

2146132-73-0
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