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Results for "

Permeability enhancer

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amylases (1) Amyloid-β (1) Antibiotic (1) Apoptosis (7) Autophagy (2) Bacterial (3) Bcl-2 Family (1) Biochemical Assay Reagents (4) Calcium Channel (1) Caspase (3) Claudin (1) DNA/RNA Synthesis (1) Drug Derivative (1) Drug Metabolite (1) E1/E2/E3 Enzyme (1) Endogenous Metabolite (7) ERK (1) Fungal (1) GABA Receptor (1) Glycosidase (1) Histone Acetyltransferase (1) Histone Methyltransferase (1) HSP (1) IAP (1) Interleukin Related (2) Isotope-Labeled Compounds (2) Liposome (1) mAChR (1) MMP (1) PACAP Receptor (1) PARP (1) PKA (2) PKC (2) PROTACs (1) Reactive Oxygen Species (ROS) (2) Reference Standards (3) ROCK (1) TNF Receptor (2) TRP Channel (2) TSH Receptor (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (4) Endocrinology (3) Infection (6) Inflammation/Immunology (6) Metabolic Disease (9) Neurological Disease (7)
Oligonucleotides:	Polymers (2)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-107380A

PGlu-3-methyl-His-Pro-NH2 TFA A-42872 TFA	TSH Receptor	Endocrinology
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole .

HY-Y1893

Solutol HS-15 15+ Cited Publications Polyethylene glycol 12-hydroxystearate	Biochemical Assay Reagents	Others
Solutol HS-15, a Macrogol 15 hydroxy stearate, is a permeability enhancer .

HY-W009326

Laurocapram	Biochemical Assay Reagents	Infection
Laurocapram is a chemical penetration enhancer that increases the permeability of compounds through the skin and mucous membranes, thereby improving their local or systemic efficacy. Laurocapram improves the skin permeability of a variety of hydrophilic and lipophilic compounds .

HY-100973A

Adenosine 5′-diphosphoribose sodium 5 Publications Verification ADP ribose sodium	TRP Channel Autophagy	Metabolic Disease Endocrinology Cancer
Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD ⁺) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca ²⁺-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy .

HY-134124

Glutathione ethyl ester	Reactive Oxygen Species (ROS)	Metabolic Disease
Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .

HY-162038

RXP03	MMP	Others
RXP03 is a MMPs inhibitor with the K_i of 20 nM, 2.5 nM, 10 nM, 5nM and 105 nM for MMP-2, MMP-8, MMP-9, MMP-11, MMP-14, respectively .

HY-W009326S

Laurocapram-15N	Isotope-Labeled Compounds	Infection
Laurocapram-15N is a deuterated labeled Laurocapram . Laurocapram is a chemical penetration enhancer that increases the permeability of compounds through the skin and mucous membranes, thereby improving their local or systemic efficacy. Laurocapram improves the skin permeability of a variety of hydrophilic and lipophilic compounds .

HY-127139

Eicosapentaenoyl Chloride Eicosapentaenoic acid Chloride; EPA Chloride	Endogenous Metabolite	Metabolic Disease
Eicosapentaenoyl chloride is a derivative of eicosapentaenoic acid. It has been used in the synthesis of fatty acid conjugates to enhance lipophilicity and cell permeability of bioactive compounds such as (–)-epigallocatechin gallate and salicylic acid.

HY-169732

Gadoquatrane	Biochemical Assay Reagents	Others
Gadoquatrane is a highly stable gadolinium-based MRI contrast agent that enhances soft tissue imaging by altering the local magnetic field, with low permeability and high biological safety .

HY-P5877

ɛPKC(85–92),Myristoylated	PKC	Inflammation/Immunology
PKC(85–92),Myristoylated is a cell permeable myristic acid conjugated PKC peptide activator that enhances NO release in cultured human umbilical vein endothelial cells (HUVECs) .

HY-100973AR

Adenosine 5′-diphosphoribose sodium (Standard) ADP ribose sodium (Standard)	Reference Standards TRP Channel Autophagy	Metabolic Disease Endocrinology Cancer
Adenosine 5′-diphosphoribose (sodium) (Standard) is the analytical standard of Adenosine 5′-diphosphoribose (sodium). This product is intended for research and analytical applications. Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD+) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca2+-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy .

HY-12372

Sanggenon G	IAP Caspase	Cancer
Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspase activation .

HY-W112651

2,4,6-Triphenylaniline	Glycosidase Amylases	Metabolic Disease
2,4,6-Triphenylaniline has anti-diabetic activity and can be encapsulated in nano-emulsions (NE) to enhance stability and permeability. The NE loaded with 2,4,6-Triphenylaniline inhibits α-glucosidase and α-amylase .

HY-167702

(Rac)-Acetoxyvalerenic acid	GABA Receptor	Neurological Disease
(Rac)-Acetoxyvalerenic acid is a derivative of valerenic acid that acts as a GABA (A) receptor modulator, potentially providing sedative and sleep-enhancing effects. (Rac)-Acetoxyvalerenic acid exhibits slower permeability across the blood-brain barrier compared to diazepam, indicating that its transport may rely on an unidentified pathway rather than transcellular passive diffusion.

HY-P5986

mSIRK (L9A)	ERK	Others
mSIRK (L9A) is a cell-permeable, N-myristoylated G-Protein Binding Peptide (mSIRK). mSIRK (L9A) contains a single point mutation (Leu9 to Ala). mSIRK (L9A) cannot enhance ERK1/2 phosphorylation. mSIRK (L9A) can be used as a control peptide .

HY-W923366

Magnesium ionophore III ETH 4030	Biochemical Assay Reagents Endogenous Metabolite
Magnesium ionophore III (ETH 4030) is an ionophore that has the activity of regulating the intracellular magnesium concentration. Magnesium ionophore III can promote the permeability of cell membranes to magnesium ions and enhance cell functions and metabolic activities. Magnesium ionophore III is also used to study the importance of magnesium ions in biological processes and its effects on cell physiology.

HY-149614

Laccase-IN-1	Endogenous Metabolite Fungal	Infection
Laccase-IN-1 (compound 4b) is an orally active inhibitor of laccase, with the IC₅₀ of 11.3 μM. Laccase-IN-1displays protective and curative effects on apple fruits infected by B. dothidea. Laccase-IN-1 enhances the cell membrane permeability, destroys the mycelial surface morphology and the cell ultrastructure, and reduces the ergosterol and exopolysaccharide contents of B. dothidea .

HY-15292

S107 1 Publications Verification	Calcium Channel	Cardiovascular Disease
S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca ²⁺ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold .

HY-135969

Glycol chitosan 3 Publications Verification	Bacterial	Infection
Glycol chitosan is a chitosan derivative with ethylene glycol branches. Glycol chitosan enhances membrane permeability and leadkage in Glycine max Harosoy 63W cells. Glycol chitosan is biocompatible and biodegradable . Glycol chitosan inhibits E. coli, S. aureus and S. enteritidis growths with MIC values of 4 μg/mL, 32 μg/mL and <0.5 μg/mL, respectively .

HY-101999

EM20-25	Bcl-2 Family Caspase Apoptosis	Cancer
EM20-25 is an inhibitor for Bcl-2, which interferes with the interaction between BCL-2 and BAX, activates caspase-9 and thus induces the apoptosis. EM20-25 affects the mitochondrial function, causes the open of permeability transition pore (PTP). EM20-25 enhances the sensitivity of cells to Staurosporine (HY-15141), and enhances the killing effect of BCL-2-expressing leukemia cells to Chlorambucil (HY-13593) and Fludarabine (HY-B0069) .

HY-P1380A

Difopein TFA	Apoptosis	Cancer
Difopein TFA, a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein TFA is not cell permeable. Difopein TFA leads to induction of apoptosis and enhances the ability of Cisplatin (HY-17394) to kill cells .

HY-116585

C6 D-Threo Ceramide (d18:1/6:0)	Liposome Interleukin Related	Neurological Disease
C6 D-Threo Ceramide (d18:1/6:0) is a bioactive sphingolipid and cell-permeable analog of ceramides. C6 D-Threo Ceramide (d18:1/6:0) enhances IL-4 production induced by Phorbol 12-myristate 13-acetate (HY-18739) in EL4 T cells .

HY-125639

(rac)-AR-13503 (rac)-AR-13324 M1 metabolite	PKC ROCK	Cardiovascular Disease
(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice .

HY-134495

N-Acetyl-L-cysteine ethyl ester 5+ Cited Publications N-Acetylcysteine ethyl ester; NACET	Reactive Oxygen Species (ROS)	Metabolic Disease
N-Acetyl-L-cysteine ethyl ester is an esterified form of N-acetyl-L-cysteine (NAC). N-Acetyl-L-cysteine ethyl ester exhibits enhanced cell permeability, and produce NAC and cysteine. N-Acetyl-L-cysteine ethyl ester increases circulating hydrogen sulfide (H₂S) and can be used as an H₂S producer. N-Acetyl-L-cysteine ethyl ester has the potential to substitute NAC as a mucolytic agent, and as a GSH-related antioxidant .

HY-113456S

Leukotriene D4-d5	Drug Metabolite Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology
Leukotriene D4-d₅ is the deuterium labeled Leukotriene D4. Leukotriene D4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) produced by the metabolism of LTC4 by γ-glutamyl transpeptidase. Leukotriene D4 is the first cysteinyl-leukotriene metabolite of LTC4. Leukotriene D4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute hypersensitivity.

HY-148033

Trimethyl chitosan N,N,N-Trimethylchitosan	Drug Derivative	Others
Trimethyl chitosan (N,N,N-Trimethylchitosan) is a multifunctional polymer and a derivative of Chitosan (HY-B2144A). Trimethyl chitosan targets the absorption enhancing proteins of tight junctions of intestinal and mucosal epithelial cells, induces tight junction protein rearrangement, and increases intercellular permeability. Trimethyl chitosan can stimulate the activity of promoting transmembrane transport of hydrophilic drugs (such as peptides and proteins) and can be used for drug delivery and synthesis of nanoparticles .

HY-141894

5-Ph-IAA-AM	Histone Acetyltransferase	Metabolic Disease
5-Ph-IAA-AM is an eggshell-permeable 5-Ph-IAA (HY-134653) analog which contains an acetoxymethyl (AM) group. 5-Ph-IAA-AM affords an enhanced protein degradation in laid embryos. 5-Ph-IAA-AM can be used to disclosure the roles of proteins in C. elegans, in particular those that are involved in embryogenesis and development, through temporally controlled protein degradation .

HY-I0746

3-Aminobenzoic acid m-Aminobenzoic acid; 3ABA	Endogenous Metabolite	Neurological Disease Inflammation/Immunology
3-Aminobenzoic acid (3-ABA) is an orally active anti-inflammatory agent targeting the tight junction (TJ) regulatory pathways in intestinal epithelial cells. 3-Aminobenzoic acid improves intestinal inflammation by enhancing intestinal barrier integrity and reducing epithelial permeability. It can be used in studies related to improving gut health. Additionally, 3-Aminobenzoic acid analogs can act as γ-aminobutyric acid transaminase (GABA-AT) inhibitors, exhibiting anticonvulsant effects .

HY-145452

5-Octyl-α-ketoglutarate 5-Octyl 2-oxopentanedioate	E1/E2/E3 Enzyme Histone Methyltransferase	Cancer
5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation .

HY-19542

C6 Ceramide 3 Publications Verification C6-Cer; N-Hexanoylsphingosine	Apoptosis	Cancer
C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .

HY-B0764B

Bucladesine Dibutyryl cAMP; DBcAMP	PKA	Neurological Disease
Bucladesine (DBcAMP) is a membrane permeable selective activator that activates cyclic adenosine phosphate dependent protein kinase A (PKA). The main regulatory mechanism of Bucladesine involves the cAMP/PKA signaling pathway. When Bucladesine activates PKA, it can promote a variety of cellular processes, including neurodevelopment, growth and plasticity. In particular, the cAMP/PKA signaling pathway plays a key role in the expression of long-term enhancement (LTP) and long-term inhibition (LTD), as well as in the formation of long-term memory in the hippocampus. Bucladesine can be used to study memory formation and neuroplasticity .

HY-168258

Antibiofilm agent-13	Bacterial	Infection
Antibiofilm agent-13 (compound 14b) is a potent antibacterial agent that displays a broad-spectrum antimicrobial activity. Antibiofilm agent-13 could disintegrate the integrity of bacterial cell membranes by destroying transmembrane potential and enhancing membrane permeability, and causing the generation of intracellular ROS and the leakage of DNA and proteins, ultimately leading to bacterial death. Antibiofilm agent-13 inhibits both Gram-positive bacteria (MIC of 0.5-1 μg/mL) and Gram-negative bacteria (MIC of 1-32 μg/mL) .

HY-14562

TBPB	mAChR Amyloid-β	Neurological Disease Inflammation/Immunology
TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC₅₀=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis) .

HY-P3483

Maxadilan	PACAP Receptor Caspase Apoptosis PKA Interleukin Related TNF Receptor	Cardiovascular Disease Neurological Disease
Maxadilan is a specific irreversible PAC1 receptor agonist and a potent vasodilator peptide present in the salivary glands of sand flies. Maxadilan exhibits anti-apoptotic activity in hADSCs. Maxadilan inhibits pro-inflammatory cytokines (TNF-α) and enhances anti-inflammatory mediators (IL-10). Maxadilan can activate leukocytes and inhibit vascular permeability through PAC1 receptors. Maxadilan promotes neural differentiation of human adipose-derived stem cells. Maxadilan can be used to study endotoxin shock, atherosclerosis, and neurodegenerative diseases ^{[1] [2] [3] [4] [5]}.

HY-137371

Lactonic sophorolipid	Bacterial Apoptosis Antibiotic	Infection Cancer
Lactonic sophorolipid is an apoptosis inducer and antimicrobial surfactant with antitumor activity. Lactonic sophorolipid regulates Bax/Bcl-gene expression through caspase-3/9 and induces apoptosis in tumor cells. Lactonic sophorolipid can disrupt cell membrane permeability and exert antibacterial effects (MIC for oral pathogens is 100-400 μg/mL). Lactonic sophorolipid promotes mitochondrial membrane potential depolarization, activates the intrinsic apoptotic pathway, and can synergize with antibiotics to enhance the antibacterial effect. Lactonic sophorolipid can be used in liver cancer research and the development of oral hygiene antibacterial agents[1][2][3].

HY-I0746R

3-Aminobenzoic acid (Standard) m-Aminobenzoic acid (Standard); 3ABA (Standard)	Reference Standards Endogenous Metabolite	Neurological Disease Inflammation/Immunology
3-Aminobenzoic acid (Standard) is the analytical standard of 3-Aminobenzoic acid. This product is intended for research and analytical applications. 3-Aminobenzoic acid (3-ABA) is an orally active anti-inflammatory agent targeting the tight junction (TJ) regulatory pathways in intestinal epithelial cells. 3-Aminobenzoic acid improves intestinal inflammation by enhancing intestinal barrier integrity and reducing epithelial permeability. It can be used in studies related to improving gut health. Additionally, 3-Aminobenzoic acid analogs can act as γ-aminobutyric acid transaminase (GABA-AT) inhibitors, exhibiting anticonvulsant effects .

HY-N1516R

Ganoderenic acid D (Standard)	Reference Standards Apoptosis	Cancer
3-Aminobenzoic acid (Standard) is the analytical standard of 3-Aminobenzoic acid. This product is intended for research and analytical applications. 3-Aminobenzoic acid (3-ABA) is an orally active anti-inflammatory agent targeting the tight junction (TJ) regulatory pathways in intestinal epithelial cells. 3-Aminobenzoic acid improves intestinal inflammation by enhancing intestinal barrier integrity and reducing epithelial permeability. It can be used in studies related to improving gut health. Additionally, 3-Aminobenzoic acid analogs can act as γ-aminobutyric acid transaminase (GABA-AT) inhibitors, exhibiting anticonvulsant effects .

HY-173437

CW-2	PROTACs PARP DNA/RNA Synthesis	Cancer
CW-2 is a PARP1 PROTAC degrader. CW-2 has potent antiproliferative effects against MDA-MB-231 cells (IC₅₀ = 0.72 μM) and CDDP-resistant cells (A549/CDDP: IC₅₀ = 3.52 μM). CW-2 has synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts antitumor effects by inducing DNA damage, impairing DNA repair, and activating mitochondria-dependent apoptosis (Pink: PARP1 ligand (HY-173441); Blue: E3 CRBN ligand (HY-173439); Black: linker (HY-173440)) .

HY-W010514

trans-Cyclohexane-1,2-diol	Endogenous Metabolite	Metabolic Disease
trans-Cyclohexane-1,2-diol (TCHD) is a transient dilator of the nuclear pore complex (NPC). By interacting with the hydrophobic core (FG nucleoporin) of the NPC, trans-Cyclohexane-1,2-diol can disrupt the NPC structure and reversibly increase the permeability of the nuclear pore, allowing macromolecules larger than 40 kDa (such as plasmid DNA) to enter the cell nucleus by passive diffusion, thereby enhancing the nuclear import efficiency of non-viral vectors. trans-Cyclohexane-1,2-diol can improve the efficiency of in vitro electrotransfection or lipid-mediated gene transfection, especially significantly increasing gene expression in differentiated airway epithelial cells .

HY-N2468

Xylobiose 1,4-β-D-Xylobiose; 1,4-D-Xylobiose	TNF Receptor Claudin HSP	Metabolic Disease Inflammation/Immunology
Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is an orally active Claudin 2/CLDN2 inhibitor and HSP27 inducer. Xylobiose works by regulating intestinal barrier function and glucose and lipid metabolism-related signaling pathways. Xylobiose inhibits CLDN2 expression to reduce intestinal permeability, induces HSP27 to enhance cell protection, and regulates the miR-122a/miR-33a axis to inhibit liver lipid synthesis and improve insulin resistance. Xylobiose can strengthen intestinal barrier integrity, reduce blood sugar and blood lipid levels, and reduce oxidative stress and inflammatory response. Xylobiose can be used in the study of type 2 diabetes and metabolic syndrome .

HY-W766368

C6 Ceramide-13C2,d2 C6-Cer-¹³C₂,d₂; N-Hexanoylsphingosine-¹³C₂,d₂	Isotope-Labeled Compounds Apoptosis	Cancer
C6 Ceramide- ¹³C₂,d₂ (C6-Cer- ¹³C₂,d₂) is the deuterium labeled and ¹³C-labeled C6 Ceramide (HY-19542). C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .

Cat. No.	Product Name

HY-L036P

Covalent Screening Library Plus	5,794 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 5,794 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

5,794 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 5,794 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	1,430 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 1,430 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

1,430 compounds

MCE covalent inhibitor library contains 1,430 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.

Cat. No.	Product Name	Type

HY-Y1893

Solutol HS-15 15+ Cited Publications Polyethylene glycol 12-hydroxystearate	Co-solvents
Solutol HS-15, a Macrogol 15 hydroxy stearate, is a permeability enhancer .

HY-135969

Glycol chitosan 3 Publications Verification	Drug Delivery
Glycol chitosan is a chitosan derivative with ethylene glycol branches. Glycol chitosan enhances membrane permeability and leadkage in Glycine max Harosoy 63W cells. Glycol chitosan is biocompatible and biodegradable . Glycol chitosan inhibits E. coli, S. aureus and S. enteritidis growths with MIC values of 4 μg/mL, 32 μg/mL and <0.5 μg/mL, respectively .

HY-148033

Trimethyl chitosan

N,N,N-Trimethylchitosan

Drug Delivery

Trimethyl chitosan (N,N,N-Trimethylchitosan) is a multifunctional polymer and a derivative of Chitosan (HY-B2144A). Trimethyl chitosan targets the absorption enhancing proteins of tight junctions of intestinal and mucosal epithelial cells, induces tight junction protein rearrangement, and increases intercellular permeability. Trimethyl chitosan can stimulate the activity of promoting transmembrane transport of hydrophilic drugs (such as peptides and proteins) and can be used for drug delivery and synthesis of nanoparticles .

Cat. No.	Product Name	Target	Research Area

HY-107380A

PGlu-3-methyl-His-Pro-NH2 TFA A-42872 TFA	TSH Receptor	Endocrinology
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole .

HY-134124

Glutathione ethyl ester	Reactive Oxygen Species (ROS)	Metabolic Disease
Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .

HY-P1380A

Difopein TFA	Apoptosis	Cancer
Difopein TFA, a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein TFA is not cell permeable. Difopein TFA leads to induction of apoptosis and enhances the ability of Cisplatin (HY-17394) to kill cells .

HY-P5877

ɛPKC(85–92),Myristoylated	PKC	Inflammation/Immunology
PKC(85–92),Myristoylated is a cell permeable myristic acid conjugated PKC peptide activator that enhances NO release in cultured human umbilical vein endothelial cells (HUVECs) .

HY-P5986

mSIRK (L9A)	ERK	Others
mSIRK (L9A) is a cell-permeable, N-myristoylated G-Protein Binding Peptide (mSIRK). mSIRK (L9A) contains a single point mutation (Leu9 to Ala). mSIRK (L9A) cannot enhance ERK1/2 phosphorylation. mSIRK (L9A) can be used as a control peptide .

HY-P3483

Maxadilan	PACAP Receptor Caspase Apoptosis PKA Interleukin Related TNF Receptor	Cardiovascular Disease Neurological Disease
Maxadilan is a specific irreversible PAC1 receptor agonist and a potent vasodilator peptide present in the salivary glands of sand flies. Maxadilan exhibits anti-apoptotic activity in hADSCs. Maxadilan inhibits pro-inflammatory cytokines (TNF-α) and enhances anti-inflammatory mediators (IL-10). Maxadilan can activate leukocytes and inhibit vascular permeability through PAC1 receptors. Maxadilan promotes neural differentiation of human adipose-derived stem cells. Maxadilan can be used to study endotoxin shock, atherosclerosis, and neurodegenerative diseases ^{[1] [2] [3] [4] [5]}.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-12372

Sanggenon G	Structural Classification Flavonoids Flavonones Source classification Morus alba L. Plants Moraceae	IAP Caspase
Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspase activation .

HY-W010514

trans-Cyclohexane-1,2-diol	Structural Classification Natural Products Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
trans-Cyclohexane-1,2-diol (TCHD) is a transient dilator of the nuclear pore complex (NPC). By interacting with the hydrophobic core (FG nucleoporin) of the NPC, trans-Cyclohexane-1,2-diol can disrupt the NPC structure and reversibly increase the permeability of the nuclear pore, allowing macromolecules larger than 40 kDa (such as plasmid DNA) to enter the cell nucleus by passive diffusion, thereby enhancing the nuclear import efficiency of non-viral vectors. trans-Cyclohexane-1,2-diol can improve the efficiency of in vitro electrotransfection or lipid-mediated gene transfection, especially significantly increasing gene expression in differentiated airway epithelial cells .

HY-N2468

Xylobiose 1,4-β-D-Xylobiose; 1,4-D-Xylobiose	Structural Classification Zea mays L. Polysaccharides Classification of Application Fields Gramineae Source classification Other Diseases Plants Disease Research Fields Saccharides	TNF Receptor Claudin HSP
Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is an orally active Claudin 2/CLDN2 inhibitor and HSP27 inducer. Xylobiose works by regulating intestinal barrier function and glucose and lipid metabolism-related signaling pathways. Xylobiose inhibits CLDN2 expression to reduce intestinal permeability, induces HSP27 to enhance cell protection, and regulates the miR-122a/miR-33a axis to inhibit liver lipid synthesis and improve insulin resistance. Xylobiose can strengthen intestinal barrier integrity, reduce blood sugar and blood lipid levels, and reduce oxidative stress and inflammatory response. Xylobiose can be used in the study of type 2 diabetes and metabolic syndrome .

HY-149614

Laccase-IN-1	Infection Structural Classification Natural Products Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields	Endogenous Metabolite Fungal
Laccase-IN-1 (compound 4b) is an orally active inhibitor of laccase, with the IC₅₀ of 11.3 μM. Laccase-IN-1displays protective and curative effects on apple fruits infected by B. dothidea. Laccase-IN-1 enhances the cell membrane permeability, destroys the mycelial surface morphology and the cell ultrastructure, and reduces the ergosterol and exopolysaccharide contents of B. dothidea .

HY-N1516R

Ganoderenic acid D (Standard)	Triterpenes Structural Classification Microorganisms Terpenoids Polyporaceae Source classification Ganoderma lucidum (Leyss. Ex Fr.) Karst. Plants	Reference Standards Apoptosis
3-Aminobenzoic acid (Standard) is the analytical standard of 3-Aminobenzoic acid. This product is intended for research and analytical applications. 3-Aminobenzoic acid (3-ABA) is an orally active anti-inflammatory agent targeting the tight junction (TJ) regulatory pathways in intestinal epithelial cells. 3-Aminobenzoic acid improves intestinal inflammation by enhancing intestinal barrier integrity and reducing epithelial permeability. It can be used in studies related to improving gut health. Additionally, 3-Aminobenzoic acid analogs can act as γ-aminobutyric acid transaminase (GABA-AT) inhibitors, exhibiting anticonvulsant effects .

Cat. No.	Product Name	Chemical Structure

HY-113456S

Leukotriene D4-d5

Leukotriene D4-d₅ is the deuterium labeled Leukotriene D4. Leukotriene D4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) produced by the metabolism of LTC4 by γ-glutamyl transpeptidase. Leukotriene D4 is the first cysteinyl-leukotriene metabolite of LTC4. Leukotriene D4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute hypersensitivity.

HY-W009326S

Laurocapram-15N
Laurocapram-15N is a deuterated labeled Laurocapram . Laurocapram is a chemical penetration enhancer that increases the permeability of compounds through the skin and mucous membranes, thereby improving their local or systemic efficacy. Laurocapram improves the skin permeability of a variety of hydrophilic and lipophilic compounds .

HY-W766368

C6 Ceramide-13C2,d2

C6 Ceramide- ¹³C₂,d₂ (C6-Cer- ¹³C₂,d₂) is the deuterium labeled and ¹³C-labeled C6 Ceramide (HY-19542). C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .

Cat. No.	Product Name		Classification

HY-135969

Glycol chitosan 3 Publications Verification		Polymers
Glycol chitosan is a chitosan derivative with ethylene glycol branches. Glycol chitosan enhances membrane permeability and leadkage in Glycine max Harosoy 63W cells. Glycol chitosan is biocompatible and biodegradable . Glycol chitosan inhibits E. coli, S. aureus and S. enteritidis growths with MIC values of 4 μg/mL, 32 μg/mL and <0.5 μg/mL, respectively .

HY-148033

Trimethyl chitosan N,N,N-Trimethylchitosan		Polymers
Trimethyl chitosan (N,N,N-Trimethylchitosan) is a multifunctional polymer and a derivative of Chitosan (HY-B2144A). Trimethyl chitosan targets the absorption enhancing proteins of tight junctions of intestinal and mucosal epithelial cells, induces tight junction protein rearrangement, and increases intercellular permeability. Trimethyl chitosan can stimulate the activity of promoting transmembrane transport of hydrophilic drugs (such as peptides and proteins) and can be used for drug delivery and synthesis of nanoparticles .

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