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Results for "

catalytically active

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Angiotensin-converting Enzyme (ACE) (1) Apoptosis (3) Autophagy (2) Beta-secretase (1) Biochemical Assay Reagents (3) Btk (1) c-Met/HGFR (1) Cholinesterase (ChE) (3) DNA/RNA Synthesis (1) Endogenous Metabolite (3) FAAH (1) Fluorescent Dye (1) Fungal (1) HDAC (2) Histone Methyltransferase (2) MDM-2/p53 (2) Parasite (1) Phosphatase (1) Phosphodiesterase (PDE) (1) PKA (1) PKC (1) Reverse Transcriptase (1)
By Research Areas:	Cancer (10) Cardiovascular Disease (2) Endocrinology (1) Infection (3) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (5)
Click Chemistry:	Alkynes (2)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-E70017

Peptidase, microorganism Erepsin; Peptidase (IMPa)	Others	Others
Peptidase (IMPa) (Erepsin) is catalytically active enzyme that cleaves peptide bonds in proteins and peptides by hydrolysis .

HY-E70069

Endo S2, Streptococcus pyogenes	Others	Others
Endo-β-N-acetylglucosaminidase (Endo S2) is a key enzyme involved in the processing of free oligosaccharides in the cytosol. Endo-β-N-acetylglucosaminidase catalyzes hydrolysis of N-linked oligosaccharides .

HY-109143

Elsubrutinib 1 Publications Verification ABBV-105	Btk	Inflammation/Immunology
Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC₅₀ of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease .

HY-115383

Roflupram 1 Publications Verification	Phosphodiesterase (PDE)	Neurological Disease Inflammation/Immunology
Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC₅₀ of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors .

HY-153967

BLU0588 1 Publications Verification	PKA	Cancer
BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC₅₀ of 1 nM and dissociation constant (K_d) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research .

HY-E70021

UDP-Glc 4-epimerase (GalE)	Others	Others
UDP-Glc 4-epimerase (GalE) is catalytically active enzyme. UDP-Glc 4-epimerase (GalE) catalyzes the reversible conversion of abundantly available UDP-glucose to UDP-galactose .

HY-157527

hAChE-IN-7	Cholinesterase (ChE) Beta-secretase	Neurological Disease
hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC₅₀=69.8 nM) and hBuChE (IC₅₀=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC₅₀=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .

HY-E70039

alpha-2-3,6,8-Sialidosidase (SpNanA)	Others	Others
alpha-2-3,6,8-Sialidosidase (SpNanA) catalyses hydrolysis of alpha-(2->3)-, alpha-(2->6)-, alpha-(2->8)- glycosidic linkages of terminal sialic acid residues in oligosaccharides, glycoproteins, glycolipids, colominic acid and synthetic substrates .

HY-171036

GAPDH-IN-1	Endogenous Metabolite	Metabolic Disease
GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor (IC₅₀ of 39.31 μM for GAPDH enzymatic activity). GAPDH-IN-1 forms a covalent adduct with an aspartic acid in the active site to displace NAD ⁺, a cofactor of the enzyme, with concomitant enhancement of the cysteine-reactive probe reaction with the catalytic cysteine .

HY-E70066

UDP-sugar pyrophosphorylase (AtUSP)	Others	Others
UDP-sugar pyrophosphorylase (AtUSP) is a broad substrate enzyme that synthesizes nucleotide sugars. UDP-sugar pyrophosphorylase catalyzes the conversion of various monosaccharide 1-phosphates to the respective UDP-sugars in the salvage pathway .

HY-P5489

IGRP(206-214)	Phosphatase	Others
IGRP(206-214) is a biological active peptide. (This peptide corresponds to residues 206–214 of murine islet-specific glucose-6-phosphatase catalytic subunit–related protein (IGRP). This peptide is T cells specific for proinsulin and IGRP induces diabetes in non-obese diabetic (NOD) mice.)

HY-P10808

RSRGVFF	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
RSRGVFF (FOXP3 inhibitor P60) is a mixed-type angiotensin-converting enzyme (ACE) inhibitor with blood-brain barrier permeability, boasting an IC₅₀ value of 5.01 μM . RSRGVFF is capable of binding to both active and non-active sites of ACE and its substrate HHL complex, thus reducing the catalytic activity of ACE. RSRGVFF can be further utilized for research on lowering hypertension .

HY-150728

AChE-IN-22	Cholinesterase (ChE)	Neurological Disease
AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC₅₀ values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease .

HY-10572A

(R)-Efavirenz (R)-DMP 266; (R)-EFV; (R)-L-743726	Reverse Transcriptase	Infection
(R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .

HY-W728451

URB694	FAAH	Cardiovascular Disease Neurological Disease
URB694 is a carbamate FAAH inhibitor that irreversibly carbamoylate the nucleophile catalytic serine in FAAH active site. URB694 exhibits antidepressant-like activity and cardioprotective effects. URB694 can be used to prepare ¹¹C-Carbonyl-URB694 for in vivo positron emission tomography (PET) imaging studies of the brain FAAH .

HY-149484

AChE/BChE-IN-15	Cholinesterase (ChE)	Neurological Disease
AChE/BChE-IN-15 (Compound 6d) is an AChE/BChE inhibitor, with IC₅₀s of 20 nM and 220 nM respectively. AChE/BChE-IN-15 binds to both catalytic anionic site (CAS) and peripheral anionic site (PAS) in the active sites of AChE and BChE. AChE/BChE-IN-15 can be used for research of Alzheimer’s disease .

HY-125384

ARN14686	Fluorescent Dye	Inflammation/Immunology
ARN14686 is an activity-based protein profiling (ABPP) probe. ARN14686 inhibits hNAAA with high potency (IC₅₀=0.006 μM). ARN14686 interacts with NAAA via covalent binding to the N-terminal cysteine. ARN14686 binds only to the catalytically active form of NAAA, and may serve therefore as an efficient activity-based probe .

HY-158335

DXR-IN-1	Parasite	Infection
DXR-IN-1 (Compound 13E) is an inhibitor of 1-deoxy-D-ketose 5-phosphate reductoisomerase (DXR). DXR-IN-1 is highly selective for P. falciparum DXR (IC₅₀=0.030 μM). DXR-IN-1 inhibits the growth of P. falciparum by binding to the active site of DXR and blocking its catalytic activity .

HY-P10422

Multi-Leu peptide ML-peptide, Multi-Leucine (ML)-peptide	Autophagy	Cancer
Multi-Leu peptide (ML-peptide) is a potent inhibitor of PACE4 (K_i=22 nM). Multi-Leu peptide can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide can be used to study the specific mechanism of PACE4 in the development of prostate cancer .

HY-E70016

Terminal deoxyribonucleotidyltransferase TdT	DNA/RNA Synthesis	Others Cancer
Terminal deoxyribonucleotidyltransferase (TdT) catalyses the condensation of deoxyribonucleotide triphosphates onto the 3' hydroxyl ends of DNA strands and adds N-regions to gene segment junctions during V(D)J recombination. Terminal deoxyribonucleotidyltransferase is expressed in immature, pre-B, pre-T lymphoid cells, and acute lymphoblastic leukemia/lymphoma cells .

HY-132913

Cyclopropenone probe 1	Biochemical Assay Reagents	Cancer
Cyclopropenone probe 1 can specifically and efficiently modify a triple-negative breast cancer driver, glutathione S-transferase pi-1 (GSTP1), by covalently binding at the catalytic active site. Cyclopropenone probe 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-124308

PS315	PKC	Cancer
PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKC_ζ (IC₅₀=10 μM) and PKC_η (IC₅₀=30 μM). PS315 has anti-cancer activity .

HY-162488

Laccase-IN-3	Fungal	Infection
Laccase-IN-3 (Compound 2b) is a laccase inhibitor (IC₅₀ = 1.02= μM) with significant antifungal activity. Laccase-IN-3 shows superior inhibitory effect on Botryosphaeria dothidea (EC₅₀ = 0.17 mg/L). Laccase-IN-3 effectively blocks the catalytic function of laccase by binding to its active center. Laccase-IN-3 also disrupts pathogen cell membrane integrity and increases ROS .

HY-11107

PHA-665752 Maximum Cited Publications 13 Publications Verification	c-Met/HGFR Autophagy Apoptosis	Cancer
PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (K_i=4 nM; IC₅₀=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity .

HY-167920

Glutathione sulfonate S-Sulfoglutathione	Endogenous Metabolite	Cancer
Glutathione sulfonate (S-Sulfoglutathione) is a multifunctional bioactive compound that inhibits angiogenesis and tumor growth. Glutathione sulfonate is a competitive inhibitor of glutathione S-transferase and is involved in the detoxification process and the binding of a variety of exogenous and endogenous compounds. Glutathione sulfonate acts in the substrate binding site of Escherichia coli glutathione S-transferase, affecting the catalytic mechanism. The structural characteristics of Glutathione sulfonate contribute to its inhibitory effect by hydrogen bonding in the active center of the enzyme .

HY-24312

AD-mix-α	Biochemical Assay Reagents	Others
AD-mix-α is a mixture of organic compounds, commonly used to distinguish and identify asymmetric carbon atoms in chiral compounds. It consists of compounds containing catalytically active metals and chiral ligands. AD-mix-α is widely used in various organic synthesis reactions, such as hydrogenation, addition, and carbonylation reactions, to increase yield and reduce the formation of side reaction products. Although it has no direct application in the medical field, it plays an important role in the pharmaceutical industry and chemical research.

HY-W033831

Rhodium(II) triphenylacetate dimer Rh2(TPA)4	Endogenous Metabolite Biochemical Assay Reagents
Rhodium(II) triphenylacetate dimer (Rh2(TPA)4) is an important catalyst with high C–H activation reaction activity. Rhodium(II) triphenylacetate dimer is widely used in organic synthesis to achieve the construction of complex molecules. Rhodium(II) triphenylacetate dimer can also be used to catalyze the synthesis of certain biologically active molecules and improve the preparation efficiency of compounds. Rhodium(II) triphenylacetate dimer exhibits excellent selectivity and reaction rate in catalytic reactions.

HY-164144

EPZ033294	Histone Methyltransferase	Cancer
EPZ033294 is an inhibitor of SYMD2 (IC₅₀ is 3.9 nM). SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC₅₀ of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T .

HY-110196

(S)-PFI-2 hydrochloride	Histone Methyltransferase	Others
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2 .

HY-16138

Ivaltinostat CG-200745	HDAC MDM-2/p53 Apoptosis	Cancer
Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects .

HY-16138A

Ivaltinostat formic CG-200745 formic	HDAC MDM-2/p53 Apoptosis	Inflammation/Immunology Endocrinology Cancer
Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat formic induces apoptosis and has anti-tumour effects .

Cat. No.	Product Name

HY-L175

Inflammasomes related Compound Library	92 compounds
Inflammasomes are classic pattern recognition receptors for natural immune responses. Inflammasomes are polymeric protein complexes that regulate inflammatory responses and pyrolytic cell death, thereby exerting the host's defense against microorganisms. Inflammasomes sensors are associated with adapter proteins, activating inflammatory caspase-1, releasing inflammatory cytokines and inducing cell death, endowing the host with defense against pathogens. NLRP1, NLRP3, NLRC4, AIM2, and pyrin are considered typical inflammasomes because they convert cysteine asparaginase-1 into catalytically active capsaicin-1. In addition to infectious diseases, the importance of inflammasomes is also related to various clinical diseases, such as autoimmune diseases, neurodegeneration and metabolic disorders, and the development of cancer. Therefore, it is necessary to strictly regulate the activation and function of inflammasomes to avoid accidental host tissue damage while inducing pathogens to kill the inflammatory response. MCE designs a unique collection of 92 inflammasomes related compounds. It is a good tool to be used for research on Inflammation, cancer and other diseases.

Inflammasomes related Compound Library

92 compounds

Inflammasomes are classic pattern recognition receptors for natural immune responses. Inflammasomes are polymeric protein complexes that regulate inflammatory responses and pyrolytic cell death, thereby exerting the host's defense against microorganisms. Inflammasomes sensors are associated with adapter proteins, activating inflammatory caspase-1, releasing inflammatory cytokines and inducing cell death, endowing the host with defense against pathogens. NLRP1, NLRP3, NLRC4, AIM2, and pyrin are considered typical inflammasomes because they convert cysteine asparaginase-1 into catalytically active capsaicin-1. In addition to infectious diseases, the importance of inflammasomes is also related to various clinical diseases, such as autoimmune diseases, neurodegeneration and metabolic disorders, and the development of cancer. Therefore, it is necessary to strictly regulate the activation and function of inflammasomes to avoid accidental host tissue damage while inducing pathogens to kill the inflammatory response.

MCE designs a unique collection of 92 inflammasomes related compounds. It is a good tool to be used for research on Inflammation, cancer and other diseases.

Cat. No.	Product Name	Type

HY-24312

AD-mix-α	Biochemical Assay Reagents
AD-mix-α is a mixture of organic compounds, commonly used to distinguish and identify asymmetric carbon atoms in chiral compounds. It consists of compounds containing catalytically active metals and chiral ligands. AD-mix-α is widely used in various organic synthesis reactions, such as hydrogenation, addition, and carbonylation reactions, to increase yield and reduce the formation of side reaction products. Although it has no direct application in the medical field, it plays an important role in the pharmaceutical industry and chemical research.

AD-mix-α

Biochemical Assay Reagents

AD-mix-α is a mixture of organic compounds, commonly used to distinguish and identify asymmetric carbon atoms in chiral compounds. It consists of compounds containing catalytically active metals and chiral ligands. AD-mix-α is widely used in various organic synthesis reactions, such as hydrogenation, addition, and carbonylation reactions, to increase yield and reduce the formation of side reaction products. Although it has no direct application in the medical field, it plays an important role in the pharmaceutical industry and chemical research.

Cat. No.	Product Name	Target	Research Area

HY-P5489

IGRP(206-214)	Phosphatase	Others
IGRP(206-214) is a biological active peptide. (This peptide corresponds to residues 206–214 of murine islet-specific glucose-6-phosphatase catalytic subunit–related protein (IGRP). This peptide is T cells specific for proinsulin and IGRP induces diabetes in non-obese diabetic (NOD) mice.)

HY-P5427

EAC3I	Peptides	Others
EAC3I is a biological active peptide. (The autocamtide-3 derived inhibitory peptide (EAC3I) sequence (KKALHRQEAVDAL) mimics the autoinhibitory region of the CaMKII regulatory domain (residues 278–290) and acts by competitively binding to the catalytic site.)

HY-P10808

RSRGVFF	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
RSRGVFF (FOXP3 inhibitor P60) is a mixed-type angiotensin-converting enzyme (ACE) inhibitor with blood-brain barrier permeability, boasting an IC₅₀ value of 5.01 μM . RSRGVFF is capable of binding to both active and non-active sites of ACE and its substrate HHL complex, thus reducing the catalytic activity of ACE. RSRGVFF can be further utilized for research on lowering hypertension .

HY-P10422

Multi-Leu peptide ML-peptide, Multi-Leucine (ML)-peptide	Autophagy	Cancer
Multi-Leu peptide (ML-peptide) is a potent inhibitor of PACE4 (K_i=22 nM). Multi-Leu peptide can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide can be used to study the specific mechanism of PACE4 in the development of prostate cancer .

Cat. No.	Product Name		Classification

HY-125384

ARN14686		Alkynes
ARN14686 is an activity-based protein profiling (ABPP) probe. ARN14686 inhibits hNAAA with high potency (IC₅₀=0.006 μM). ARN14686 interacts with NAAA via covalent binding to the N-terminal cysteine. ARN14686 binds only to the catalytically active form of NAAA, and may serve therefore as an efficient activity-based probe .

HY-132913

Cyclopropenone probe 1		Alkynes
Cyclopropenone probe 1 can specifically and efficiently modify a triple-negative breast cancer driver, glutathione S-transferase pi-1 (GSTP1), by covalently binding at the catalytic active site. Cyclopropenone probe 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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