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Results for "

chemical inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Autophagy (1) Bacterial (3) Biochemical Assay Reagents (1) Calcium Channel (1) Drug Intermediate (1) ERK (1) GSK-3 (1) Histamine Receptor (2) Histone Demethylase (1) Monocarboxylate Transporter (1) mTOR (1) Potassium Channel (1) Reactive Oxygen Species (ROS) (3) Reference Standards (2) SGLT (1) Sodium Channel (1) TRP Channel (1)
By Research Areas:	Cancer (5) Endocrinology (2) Infection (3) Metabolic Disease (2) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112082

BAY885	ERK	Cancer
BAY885, a chemical probe, is a highly potent and selective ERK5 inhibitor with an IC₅₀ of 35 nM. BAY885 shows weak inhibition on others kinases .

HY-132301

MSC-4381 MCT4-IN-1	Monocarboxylate Transporter	Cancer
MSC-4381 (MCT4-IN-1), a chemical probe, is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC₅₀ of 77 nM and a K_i of 11 nM. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research . MSC-4381 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-101189

JNJ-39758979	Histamine Receptor	Neurological Disease Endocrinology
JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine H₄ receptor antagonist with K_is of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H₄ receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .

HY-125629

Primordazine B	Others	Others
Primordazine B is a small molecule compound identified by chemical screening in zebrafish embryos with the activity of selectively destroying Primordial Germ Cells (PGCs). Primordazine B inhibits a process called Poly(A)-tail Independent Non-canonical Translation (PAINT) without inhibition of polyadenylate tail dependent typical translation (PAT). Primordazine B can be used to study translational control of cells in specific physiological or pathological states, such as gene expression regulation during cell dormancy, viral infection, or stress conditions .

HY-101122

LX2761	SGLT	Metabolic Disease
LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC₅₀s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract .

HY-W674002

1-Adamantylphosphaethyne 1-(2-Phosphaethynyl)adamantane	Apoptosis
1-Adamantylphosphaethyne (1-(2-Phosphaethynyl)adamantane) is a compound with potential biological activity and can be used as a catalyst in organic synthesis. 1-Adamantylphosphaethyne has shown the ability to induce cell apoptosis in compound development, which helps in anti-tumor inhibition. 1-Adamantylphosphaethyne can also be used as an efficient reaction intermediate to promote the progress of various chemical reactions.

HY-136818

DA 4643 dihydrochloride	Histamine Receptor	Endocrinology
DA 4643 (hydrochloride) is an H2 receptor antagonist with the chemical name 2-guanidino-4 (3-methylaminomethyleneiminophenyl) thiazole dihydrochloride. It has a weak interaction with cytochrome P-450 and has a less inhibitory effect on P-450 than cimetidine and tiotidine. DA 4643 (hydrochloride) is able to inhibit both enzymatic and non-enzymatic lipid peroxidation reactions. This inhibition may not be achieved by inhibiting agent metabolizing enzymes, but rather due to the antioxidant properties of the compound itself. Compared with other H2 receptor antagonists such as cimetidine, ranitidine and tiotidine, DA 4643 (hydrochloride) shows a unique effect in lipid peroxidation inhibition. These properties make DA 4643 (hydrochloride) a potential H2 receptor antagonist with multiple mechanisms of action.

HY-N11431

ent-Toddalolactone	Others	Cancer
ent-Toddalolactone is a natural compound with anti-inflammatory and anticancer activities. Ent-Toddalolactone has shown inhibitory effects on phosphodiesterase-4 (PDE4) in vitro and is a potential drug target for inhibiting asthma and chronic obstructive pulmonary disease. The activity of ent-Toddalolactone is related to its unique chemical structure, and some of its derivatives showed IC₅₀ values below 10 μM in inhibition experiments, showing high biological activity .

HY-W015752R

5-Methoxyresorcinol (Standard)	Reference Standards Drug Intermediate	Others
5-Methoxyresorcinol (Standard) is an analytical standard for 5-Methoxyresorcinol (HY-W015752). This product is intended for research and analytical applications. 5-Methoxyresorcinol is a model molecule for the A ring of flavonoids, specifically mimicking the chemical behavior of the resorcinol-type A ring in catechins. 5-Methoxyresorcinol exhibits very low tocopherol regeneration activity. 5-Methoxyresorcinol shows little inhibition of cholesteryl ester transfer protein (CETP).

HY-12596

JNJ-26489112	Calcium Channel Sodium Channel Potassium Channel	Neurological Disease
JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na ⁺ channels and N-type Ca ²⁺ channels, and is effective as a K ⁺ channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC₅₀=35 μM) and CA-I (18 μM) .

HY-N7059

Lactobionic acid	Bacterial Reactive Oxygen Species (ROS)	Infection
Lactobionic acid is a bionic acid that can be naturally found in the Caspian Sea yogurt and chemically constituted of a gluconic acid bonded to a galactose. Lactobionic acid has antioxidant, antimicrobial, chelating, stabilizer, acidulant, and moisturizing properties. Lactobionic acid can be obtained by electrolytic methods, microbial fermentation or biocatalytic approaches. Lactobionic acid can be used in foodstuffs, to produce new functional products and against food-borne pathogens. Lactobionic acid inhibits DNA repair and protein synthesis, induction of oxidative stress and inhibition of metabolic pathways against MRSA .

HY-N7059A

Lactobionic acid calcium dihydrate	Biochemical Assay Reagents Bacterial Reactive Oxygen Species (ROS)	Infection
Lactobionic acid calcium dihydrate is a biomimetic acid found in Caspian yogurt, chemically composed of gluconic acid bonded to galactose. Lactobionic acid calcium dihydrate has antioxidant, antimicrobial, chelating, stabilizer, acidulant and humectant properties. Lactobionic acid calcium dihydrate can be obtained by electrolytic methods, microbial fermentation or biocatalytic approaches. Lactobionic acid calcium dihydrate can be used in foodstuffs, to produce new functional products and against food-borne pathogens. Lactobionic acid calcium dihydrate inhibits DNA repair and protein synthesis, induction of oxidative stress and inhibition of metabolic pathways against MRSA .

HY-N7536

Voacangine	TRP Channel	Others
Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC₅₀=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC₅₀=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC₅₀=9 μM) and it shows noncompetitive inhibition against icilin (IC₅₀=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .

HY-N7059R

Lactobionic acid (Standard)	Reference Standards Bacterial Reactive Oxygen Species (ROS)	Infection
Lactobionic acid (Standard) is an analytical standard for lactobionic acid. This product is intended for use in research and analytical applications. Lactobionic acid is a bionic acid that can be naturally found in the Caspian Sea yogurt and chemically constituted of a gluconic acid bonded to a galactose. Lactobionic acid has antioxidant, antimicrobial, chelating, stabilizer, acidulant, and moisturizing properties. Lactobionic acid can be obtained by electrolytic methods, microbial fermentation or biocatalytic approaches. Lactobionic acid can be used in foodstuffs, to produce new functional products and against food-borne pathogens. Lactobionic acid inhibits DNA repair and protein synthesis, induction of oxidative stress and inhibition of metabolic pathways against MRSA .

HY-172118

SGC-CDKL5/GSK3	GSK-3	Neurological Disease
CDKL5/GSK3-IN-1 (Compound 2) is a potent and selectivity chemical probe for CDKL5/GSK3.CDKL5/GSK3-IN-1 has potent inhibition of CDKL5 and GSK3α/β, with IC₅₀ values of 4.6, 24 and 9.5 nM for CDKL5, GSK3β and GSK3α, respectively, in the NanoBRET assay. CDKL5/GSK3-IN-1 can be used for the research of CNS diseases .

HY-111373

RapaLink-1 10+ Cited Publications	mTOR Autophagy	Cancer
RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity .

HY-15313B

CBB1007 hydrochloride	Histone Demethylase	Metabolic Disease Cancer
CBB1007 hydrochloride is a reversible and selective LSD1 inhibitor with an IC₅₀ of 5.27 µM for human LSD1. CBB1007 hydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 hydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 hydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .

Cat. No.	Product Name

HY-L036P

Covalent Screening Library Plus	5,913 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery. MCE covalent inhibitor library contains 5,913 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc. MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

Covalent Screening Library Plus

5,913 compounds

Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.

MCE covalent inhibitor library contains 5,913 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

HY-L036

Covalent Screening Library	1,443 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery. MCE covalent inhibitor library contains 1,443 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

Covalent Screening Library

1,443 compounds

MCE covalent inhibitor library contains 1,443 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

HY-L044

Nucleotide Compound Library	593 compounds
Nucleoside and nucleotide analogues are synthetic, chemically modified compounds that have been developed to mimic their physiological counterparts in order to exploit cellular metabolism and subsequently be incorporated into DNA and RNA to inhibit cellular division and viral replication. In addition to their incorporation into nucleic acids, nucleoside and nucleotide analogues can interact with and inhibit essential enzymes such as human and viral polymerases (that is, DNA-dependent DNA polymerases, RNA-dependent DNA polymerases or RNA-dependent RNA polymerases), kinases, ribonucleotide reductase, DNA methyltransferases, purine and pyrimidine nucleoside phosphorylase and thymidylate synthase. These actions of nucleoside and nucleotide analogues have potential therapeutic benefits — for example, in the inhibition of cancer cell growth, the inhibition of viral replication as well as other indications. MCE offers a unique collection of 593 nucleotide compounds including nucleotide, nucleoside and their structural analogues. MCE Nucleotide Compound Library is a useful tool to discover anti-cancer and antiviral drugs for high throughput screening (HTS) and high content screening (HCS).

Nucleotide Compound Library

593 compounds

Nucleoside and nucleotide analogues are synthetic, chemically modified compounds that have been developed to mimic their physiological counterparts in order to exploit cellular metabolism and subsequently be incorporated into DNA and RNA to inhibit cellular division and viral replication. In addition to their incorporation into nucleic acids, nucleoside and nucleotide analogues can interact with and inhibit essential enzymes such as human and viral polymerases (that is, DNA-dependent DNA polymerases, RNA-dependent DNA polymerases or RNA-dependent RNA polymerases), kinases, ribonucleotide reductase, DNA methyltransferases, purine and pyrimidine nucleoside phosphorylase and thymidylate synthase. These actions of nucleoside and nucleotide analogues have potential therapeutic benefits — for example, in the inhibition of cancer cell growth, the inhibition of viral replication as well as other indications.

MCE offers a unique collection of 593 nucleotide compounds including nucleotide, nucleoside and their structural analogues. MCE Nucleotide Compound Library is a useful tool to discover anti-cancer and antiviral drugs for high throughput screening (HTS) and high content screening (HCS).

HY-L193

PBCRBS Traditional Chinese Medicine Compound Library	1,021 compounds
Since ancient times, promoting blood circulation for removing blood stasis (PBCRBS) has been one of the most popular research contents in the area of traditional Chinese medicine (TCM) and integrated medicine. Rhizoma, Persicae Semen, Carthami Flos, Curcumae Longae Rhizoma and so on are common TCM with PBCRBS characteristic. Studies have shown that the mechanism of action of PBCRBS TCM is to promote blood circulation (improving cardiovascular and cerebrovascular functions, physical and chemical properties of blood, platelet and coagulation system and other physiological functions) and remove blood stasis (anti-myocardial ischemia, cerebral ischemia, inhibition of platelet aggregation, anti-coagulation, anti-thrombosis, etc.). Not only that, PBCRBS TCM has anti-infection, inhibit inflammation, regulate immune function, inhibit immune response, inhibit abnormal tissue proliferation and other functions. Therefore, PBCRBS TCM has high research value in all- field disease research fields. MCE can supply 1,021 monomer component from more than a hundred sources of PBCRBS TCM, which can be used in TCM studies, drug development and mechanism-based studies.

PBCRBS Traditional Chinese Medicine Compound Library

1,021 compounds

Since ancient times, promoting blood circulation for removing blood stasis (PBCRBS) has been one of the most popular research contents in the area of traditional Chinese medicine (TCM) and integrated medicine. Rhizoma, Persicae Semen, Carthami Flos, Curcumae Longae Rhizoma and so on are common TCM with PBCRBS characteristic. Studies have shown that the mechanism of action of PBCRBS TCM is to promote blood circulation (improving cardiovascular and cerebrovascular functions, physical and chemical properties of blood, platelet and coagulation system and other physiological functions) and remove blood stasis (anti-myocardial ischemia, cerebral ischemia, inhibition of platelet aggregation, anti-coagulation, anti-thrombosis, etc.). Not only that, PBCRBS TCM has anti-infection, inhibit inflammation, regulate immune function, inhibit immune response, inhibit abnormal tissue proliferation and other functions. Therefore, PBCRBS TCM has high research value in all- field disease research fields.

MCE can supply 1,021 monomer component from more than a hundred sources of PBCRBS TCM, which can be used in TCM studies, drug development and mechanism-based studies.

Cat. No.	Product Name	Type

HY-N7059A

Lactobionic acid calcium dihydrate	Cell Assay Reagents
Lactobionic acid calcium dihydrate is a biomimetic acid found in Caspian yogurt, chemically composed of gluconic acid bonded to galactose. Lactobionic acid calcium dihydrate has antioxidant, antimicrobial, chelating, stabilizer, acidulant and humectant properties. Lactobionic acid calcium dihydrate can be obtained by electrolytic methods, microbial fermentation or biocatalytic approaches. Lactobionic acid calcium dihydrate can be used in foodstuffs, to produce new functional products and against food-borne pathogens. Lactobionic acid calcium dihydrate inhibits DNA repair and protein synthesis, induction of oxidative stress and inhibition of metabolic pathways against MRSA .

Lactobionic acid calcium dihydrate

Cell Assay Reagents

Lactobionic acid calcium dihydrate is a biomimetic acid found in Caspian yogurt, chemically composed of gluconic acid bonded to galactose. Lactobionic acid calcium dihydrate has antioxidant, antimicrobial, chelating, stabilizer, acidulant and humectant properties. Lactobionic acid calcium dihydrate can be obtained by electrolytic methods, microbial fermentation or biocatalytic approaches. Lactobionic acid calcium dihydrate can be used in foodstuffs, to produce new functional products and against food-borne pathogens. Lactobionic acid calcium dihydrate inhibits DNA repair and protein synthesis, induction of oxidative stress and inhibition of metabolic pathways against MRSA .

Cat. No.	Product Name	Category	Target	Chemical Structure