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By Targets:	Cyclin G-associated Kinase (GAK) (1) Cytochrome P450 (1) Dengue Virus (1) DNA-PK (2) Drug Metabolite (1) Endogenous Metabolite (1) Ephrin Receptor (1) Farnesyl Transferase (1) Fluorescent Dye (1) Fungal (1) Potassium Channel (1) VEGFR (1)
By Research Areas:	Cancer (5) Cardiovascular Disease (2) Infection (3) Neurological Disease (1)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-156404

PM-1	Fluorescent Dye	Others
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .

HY-158090

Triptolide palmitate	Others	Cancer
Triptolide palmitate is the derivative of Triptolide (HY-32735). Triptolide palmitate exhibits cytotoxicity against cancer cell MCF-7 and A549, with IC₅₀ of 7.5 and 6.4 μM. Triptolide palmitate exhibits a half-time T_1/2 of 50.4 min in Sprague Dawley rats. Triptolide palmitate can be utilizd as drug carrier .

HY-158122

Lys(CO-C3-p-I-Ph)-O-tBu	DNA-PK	Cancer
Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with ¹¹¹In, it can be used as DOTA chelating agent and imaging agent. Or labeled with ²²⁵Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .

HY-129708

LU 2443	Drug Metabolite	Neurological Disease
LU 2443 is an orally active antiepileptic mesoionic. LU 2443 is extensively absorbed, in the maximum 18% are eliminated unabsorbed in rats. The half-time of the activity in plasma is 13.17 h .

HY-172423

Darlifarnib	Farnesyl Transferase	Cancer
Darlifarnib (Compound (S)-058) is the inhibitor for farnesyl transferase and geranylgeranyltransferase with IC₅₀ ≤ 10 nM and ＞ 1000 nM. Darlifarnib exhibits good metabolic stability in human and mouse liver microsomes with the half-life time ＞ 100 min .

HY-169119

Antifungal agent 114	Cytochrome P450 Fungal	Infection
Antifungal agent 114 (Compound 19g) is an inhibitor for Cytochrome P450, that inhibits CYP1A2, CYP2C9, CYP2C19 CYP2D6 and CYP3A4 at 10 μM. Antifungal agent 114 exhibits antifungal activity against Cryptococcus neoformans, Candida and Aspergillus, with MIC <0.0625 μg/mL. Antifungal agent 114 exhibits good metabolic stability in human liver microsomes with a half-time of 107 minutes .

HY-14308

GS-9851 PSI-7851	Endogenous Metabolite	Infection
GS-9851 (PSI-7851) is an HCV nonstructural protein 5B (NS5B) inhibitor with potential activity for the treatment of HCV infection. GS-9851 showed good tolerability in patients with initial HCV genotype 1 infection. GS-9851 is rapidly cleared from the body with a half-life of approximately 1 hour. The maximum concentration of GS-9851 and the increase in the area under the compound concentration-time curve were not dose-proportional, especially at the highest dose .

HY-159174

EPHA2/A4/GAK-IN-1	Ephrin Receptor Cyclin G-associated Kinase (GAK) Dengue Virus	Infection
EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with K_D values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. EPHA2/GAK-IN-1 shows an extrapolated half-life time of 4.6 h in a microsomal stability assay. EPHA2/GAK-IN-1 shows antiviral activity and prevents dengue virus infection of Huh7 liver cells .

HY-163403

VEGFR-2-IN-43	VEGFR	Cardiovascular Disease Cancer
VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC₅₀ of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .

HY-121183

Aprikalim RP 52891	Potassium Channel	Cardiovascular Disease
Aprikalim (RP 52891), a potassium channel opener (KCO), activates ATP-sensitive K+ (KATP) channels in guinea pig ventricular myocytes. Using patch-clamp techniques, it was found that aprikalim enhances KATP channel activity more effectively in Mg-NDP solution compared to standard solutions. In Mg-NDP solution, aprikalim reduced the sensitivity of KATP channels to ATP, increasing the concentration of ATP required to inhibit channel activity by half (K1) from 56 μM to 180 μM. However, this effect diminished over time. Aprikalim's ability to activate KATP channels in Mg-NDP solution suggests potential therapeutic implications in modulating cardiac excitability and may relate to changes in channel protein enzymatic activity under experimental conditions .

HY-158118

Lys(CO-C3-p-I-Ph)-OMe	DNA-PK	Cancer
Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with ¹¹¹In, it can be used as DOTA chelating agent and imaging agent. Or labeled with ²²⁵Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .

Cat. No.	Product Name

HY-L021M

Natural Product and Natural Product-Like Compound Library	0 compounds
From the discovery of traditional Chinese medicine to modern antibiotics, natural products have played an important role in the drug development process. A review of all FDA-approved drugs shows that natural products and natural product-like compounds account for more than one-third of all approved drugs. Nearly half of that came from mammals, a quarter from microbes, and a quarter from plants. Over time, the proportion of microbial natural products and natural product derivatives in approved drugs has increased. Natural products have natural advantages in drug development and can be used as lead compounds in drug discovery for drug identification and mechanism research. MCE provides a unique collection of 0 natural compounds and natural product-like compounds that contain saccharides and glycosides, phenylpropanoids, quinones, flavonoids, terpenoids and glycosides, steroids, alkaloid, phenols, acids and aldehydes. Natural product and natural product-like compounds library is a useful tool for drug discovery that can be used for high-throughput screening (HTS) and high-content screening (HCS).

Natural Product and Natural Product-Like Compound Library

0 compounds

From the discovery of traditional Chinese medicine to modern antibiotics, natural products have played an important role in the drug development process. A review of all FDA-approved drugs shows that natural products and natural product-like compounds account for more than one-third of all approved drugs. Nearly half of that came from mammals, a quarter from microbes, and a quarter from plants. Over time, the proportion of microbial natural products and natural product derivatives in approved drugs has increased. Natural products have natural advantages in drug development and can be used as lead compounds in drug discovery for drug identification and mechanism research.

MCE provides a unique collection of 0 natural compounds and natural product-like compounds that contain saccharides and glycosides, phenylpropanoids, quinones, flavonoids, terpenoids and glycosides, steroids, alkaloid, phenols, acids and aldehydes. Natural product and natural product-like compounds library is a useful tool for drug discovery that can be used for high-throughput screening (HTS) and high-content screening (HCS).

Cat. No.	Product Name	Type

HY-156404

PM-1	Dyes
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .

PM-1

Dyes

PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .

Cat. No.	Product Name		Classification

HY-159174

EPHA2/A4/GAK-IN-1		Azide
EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with K_D values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. EPHA2/GAK-IN-1 shows an extrapolated half-life time of 4.6 h in a microsomal stability assay. EPHA2/GAK-IN-1 shows antiviral activity and prevents dengue virus infection of Huh7 liver cells .

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