Permeability enhancer

By Targets:	Bacterial (1) Biochemical Assay Reagents (2) Caspase (1) Drug Metabolite (1) Endogenous Metabolite (2) Fungal (1) IAP (1) MMP (1) PKC (2) Reactive Oxygen Species (2) ROCK (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (3) Endocrinology (1) Infection (2) Inflammation/Immunology (3) Metabolic Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-Y1893

Solutol HS-15 Maximum Cited Publications 11 Publications Verification Polyethylene glycol 12-hydroxystearate	Biochemical Assay Reagents	Others
Solutol HS-15, a Macrogol 15 hydroxy stearate, is a permeability enhancer .

HY-100973A

Adenosine 5′-diphosphoribose sodium 2 Publications Verification ADP ribose sodium
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	Inflammation/Immunology
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 .

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-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-W141881

N-Lauroylsarcosine	Biochemical Assay Reagents	Others
N-lauroylsarcosine is an anionic surfactant, and can be used as a permeation enhancer. The mixture of N-lauroylsarcosine in 25-50% ethanol acts synergistically to increase skin permeability, which may be useful for transdermal drug delivery research .

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-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-141894

5-Ph-IAA-AM	Others	Others
5-Ph-IAA-AM is an eggshell-permeable 5-Ph-IAA analog. 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-15292

S107 1 Publications Verification	Others	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-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-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 3 Publications Verification N-Acetylcysteine ethyl ester; NACET	Reactive Oxygen Species	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-145452

5-Octyl-α-ketoglutarate 5-Octyl 2-oxopentanedioate	Others	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 .

Cat. No.	Product Name

HY-L036P

Covalent Screening Library Plus	2996 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 2996 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

2996 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 2996 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	1676 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 1676 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

1676 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 1676 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

10+ Cited Publications

Polyethylene glycol 12-hydroxystearate
Co-solvents

Solutol HS-15, a Macrogol 15 hydroxy stearate, is a permeability enhancer .

Solutol HS-15 10+ Cited Publications Polyethylene glycol 12-hydroxystearate	Co-solvents
Solutol HS-15, a Macrogol 15 hydroxy stearate, is a permeability enhancer .

Cat. No.	Product Name	Target	Research Area

HY-107380A

PGlu-3-methyl-His-Pro-NH2 TFA A-42872 TFA	Peptides	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	Inflammation/Immunology
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-W141881

N-Lauroylsarcosine	Biochemical Assay Reagents	Others
N-lauroylsarcosine is an anionic surfactant, and can be used as a permeation enhancer. The mixture of N-lauroylsarcosine in 25-50% ethanol acts synergistically to increase skin permeability, which may be useful for transdermal drug delivery research .

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)	Peptides	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 .

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-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 .

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.

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.

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