Endogenous Metabolite

Cat. No.

A73021

CAS No.

182821-29-0

Endopeptidase-IN-1

Endopeptidase-IN-1 is a potent inhibitor of endopeptidase activity, targeting endogenous metabolites to regulate proteolytic processes. Its biological activity is crucial for research focused on protein processing, cellular signaling pathways, and the modulation of metabolic diseases. This compound is a valuable tool for investigating the role of endopeptidases in physiological and pathological conditions.

Cat. No.

A73023

CAS No.

780736-74-5

YM-75440

YM-75440 is an orally active inhibitor of squalene synthase, a key enzyme in the cholesterol biosynthesis pathway. This compound demonstrates significant biological activity in modulating lipid metabolism, making it useful for research on metabolic disorders and cardiovascular diseases. Its ability to inhibit squalene synthesis positions YM-75440 as a valuable tool for studying cholesterol-related pathways and potential therapeutic interventions.

Cat. No.

A73039

CAS No.

100715-13-7

ts-SA

ts-SA is a potent carbonic anhydrase (CA) inhibitor that demonstrates inhibitory activity against seven human CA homologues. It effectively binds to the Zn(II) ion in the enzyme's active site in its deprotonated form, with its organic structure extending into the enzyme cavity, facilitating interactions with amino acid residues and water molecules. With low nanomolar inhibitory activity, ts-SA serves as a multi-target CA inhibitor, making it valuable for research applications in enzymatic regulation and metabolic studies.

Cat. No.

A73042

CAS No.

2020015-37-4

DY3002

DY3002 is a highly selective and potent EGFR inhibitor specifically designed to target T790M-mutated variants associated with non-small cell lung cancer. This compound demonstrates a remarkable inhibitory effect on EGFR T790M mutants with an IC50 of 0.71 nM, while exhibiting significantly reduced activity against wild-type EGFR (IC50 = 448.7 nM). In cellular assays, DY3002 shows an IC50 of 0.037 μM against H1975 cells, indicating enhanced biological efficacy. Additionally, DY3002 maintains an extraordinary selectivity index (SI = 632.0) and does not induce hyperglycemia, making it a promising candidate for further research in overcoming drug resistance in cancer therapy.

Cat. No.

A73062

CAS No.

1619884-75-1

MAO-B-IN-35

MAO-B-IN-35 is a potent, selective, reversible inhibitor of monoamine oxidase B (MAO-B). Demonstrating strong inhibitory activity, this compound has significant potential for research applications related to neurodegenerative disorders and the modulation of monoamine neurotransmitter levels. Its design allows for efficient synthesis and superior physicochemical properties, making it a valuable tool for studying MAO-B's role in various biological processes.

Cat. No.

A73075

CAS No.

109376-83-2

ML-7

ML-7 is a myosin light chain kinase inhibitor that primarily targets the regulation of superoxide anion (O2(-)) release in human neutrophils. This compound effectively inhibits extracellular O2(-) release from stimulated cells while leaving intracellular O2(-) production unaffected. Additionally, ML-7 has been shown to modulate neutrophil activity independently of myosin light chain kinase and offers protective effects on cardiac function during ischemia/reperfusion injury. Its unique properties make it valuable for research in inflammation and cardiac protection mechanisms.

Cat. No.

A73108

CAS No.

924764-38-5

NPD7155

NPD7155 is a purine-based competitive inhibitor of the enzyme MTH1, which plays a crucial role in the detoxification of oxidized purine metabolites. This compound demonstrates significant cytotoxic activity against cancer cells by promoting oxidative stress and disrupting metabolic pathways. NPD7155 is valuable for research into the mechanisms of cancer cell metabolism and the development of targeted cancer therapies.

Cat. No.

A73138

CAS No.

423744-59-6

STF-038533

STF-038533 is an inhibitor of the cAMP response element-binding protein (CREB), primarily targeting its transcriptional activity. This compound effectively suppresses the expression of CREB target genes, thereby modulating cellular signaling pathways. STF-038533 is invaluable for research into diseases associated with aberrant CREB activity, offering insights into therapeutic strategies for CREB-related disorders.

Cat. No.

A73143

CAS No.

1370023-80-5

Deleobuvir sodium

Synonyms: BI 207127 sodium

Deleobuvir sodium is a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase, targeting viral replication. This compound exhibits significant anti-hepatitis C virus activity, making it a valuable tool for research into hepatitis C treatment. Its use facilitates the study of viral mechanisms and the development of therapeutic strategies aimed at combating hepatitis C infection.

Cat. No.

A73152

CAS No.

22781-23-3

Bendiocarb

Bendiocarb is a carbamate compound that primarily acts as an inhibitor of the enzyme acetylcholinesterase. This inhibition results in increased levels of acetylcholine, which plays a crucial role in neurotransmission and muscle contraction. Bendiocarb is utilized in research applications focusing on neurobiology and the study of cholinergic systems, as well as in the examination of potential neurotoxic effects.

Cat. No.

A73154

CAS No.

1011465-90-9

H-0106 dihydrochloride

H-0106 dihydrochloride is a selective inhibitor of Rho-associated kinase (ROCK), primarily targeting the modulation of intraocular pressure (IOP). This compound exhibits significant IOP-lowering activity, as demonstrated in primate models. Research indicates that while H-0106 dihydrochloride effectively inhibits the ROCK enzyme, the relationship between ROCK inhibition and IOP reduction may not be straightforward, warranting further investigation into its mechanisms of action in ocular health.

Cat. No.

A73163

CAS No.

191791-65-8

(Rac)-Eflucimibe

Synonyms: (Rac)-F 12511

(Rac)-Eflucimibe is an ACAT inhibitor that modulates endogenous hypercholesterolemia. It demonstrates significant potency and efficacy as an anti-hypercholesterol agent in various animal models of hypercholesterolemia. This compound is useful for investigating cholesterol metabolism and understanding the mechanisms of cholesterol regulation in biological systems.

Cat. No.

A73171

CAS No.

1310694-75-7

DBPR110

DBPR110 is a potent inhibitor of nonstructural protein 5A (NS5A), specifically targeting hepatitis C virus (HCV) replication. It demonstrates significant antiviral activity with an EC50 of 3.9 ± 0.9 pM against HCV1b replicon reporter expression, and a selectivity index exceeding 12,800,000. Additionally, DBPR110 reduces HCV2a replicon activity with an EC50 of 228.8 pM and a selectivity index of over 173,130. This compound exhibits synergistic effects when used in combination with interferon alpha (IFN-α) and other antiviral agents, suggesting its potential as a viable small molecule therapeutic for HCV treatment.

Cat. No.

A73189

CAS No.

194979-70-9

(S)-CPP sodium

(S)-CPP sodium is an inhibitor of the branched-chain α-ketoacid dehydrogenase complex (BCKDC) kinase, also known as BDK. By negatively regulating BCKDC activity, (S)-CPP effectively activates the complex and significantly reduces plasma concentrations of branched-chain amino acids such as leucine, isoleucine, and valine in wild-type mice. This agent is useful for research applications investigating metabolic pathways and the regulation of amino acid levels in physiological and pathological contexts.

Cat. No.

A73198

CAS No.

1212-37-9

Neostigmine iodide

Neostigmine iodide is a reversible inhibitor of acetylcholinesterase, enhancing muscle tone and function. This compound is primarily utilized in the management of myasthenia gravis, aiming to improve muscle strength in affected patients. Additionally, Neostigmine iodide is employed in anesthetic procedures to counteract the effects of nondepolarizing muscle relaxants, such as rocuronium, thereby facilitating recovery from anesthesia.

Cat. No.

A73200

CAS No.

2025320-97-0

Lifirafenib hydrochloride

Synonyms: BGB-283 hydrochloride

Lifirafenib hydrochloride is a reversible inhibitor of the B-RAFV600E mutation, exhibiting significant antitumor activity in solid tumors, including melanoma, thyroid cancer, and low-grade serous ovarian cancer. This compound demonstrates selective cytotoxicity by preferentially targeting cancer cells harboring B-RAFV600E and EGFR mutations or amplifications. In preclinical studies, Lifirafenib has been shown to inhibit tumor growth in a dose-dependent manner, resulting in partial and complete tumor regression in animal models, making it a valuable tool for cancer research applications.

Cat. No.

A73208

CAS No.

81050-71-7

Chlorambucyl-proline

Chlorambucyl-proline is an amino acid derivative exhibiting inhibitory activity against bovine pulmonary vasoconstrictor enzyme. This compound functions as an irreversible inhibitor by forming ester bonds with the enzyme's aspartic or glutamic acid residues, leading to permanent enzyme inactivation. The rate of inactivation by chlorambucyl-proline is influenced by pH, with increased activity observed in the 5-8 range, making it a valuable tool for studying enzymatic regulation and function in physiological pH environments.

Cat. No.

A73212

CAS No.

56767-76-1

Flurbiprofen sodium

Synonyms: dl-Flurbiprofen sodium

Flurbiprofen sodium is a nonsteroidal anti-inflammatory drug (NSAID) targeting inflammatory pathways through the inhibition of carbonic anhydrase. It exhibits significant anti-inflammatory and analgesic properties, making it useful in the treatment of periodontal disease by reducing bone resorption. Additionally, Flurbiprofen sodium can be formulated into biodegradable microspheres for effective compound delivery, particularly within periodontal pockets, with the release kinetics influenced by the concentration of the polymer and polyvinyl alcohol used in its preparation. This compound is valuable for research into periodontal therapies and inflammation-related studies.

Cat. No.

A73231

CAS No.

919010-22-3

Pfn1-IN-2

Pfn1-IN-2 is a selective inhibitor of Profilin1 (Pfn1), designed to disrupt the interaction between Pfn1 and actin filaments. This compound effectively decreases the levels of filamentous (F) actin within cells, leading to diminished migration and proliferation of endothelial cells. Pfn1-IN-2 demonstrates significant inhibition of endothelial cell angiogenic capabilities in both in vitro and in vivo research settings, making it a valuable tool for studies in angiogenesis and cellular dynamics.

Cat. No.

A73239

CAS No.

3431-16-1

VEC6

Synonyms: NSC 11435

VEC6 (NSC 11435) is an inhibitor of the VEZF1-DNA interaction, demonstrating significant activity in modulating vascular responses during ischemic retinopathy. It effectively reduces pathological angiogenesis while promoting lymphangiogenesis by influencing the expression of distinct gene sets in endothelial cells. VEC6 inhibits VEZF1-mediated transcriptional activity, thereby impacting endothelial cell proliferation and sprouting. This compound serves as a valuable tool for studying the molecular mechanisms of angiogenesis and lymphangiogenesis in various research applications.

Cat. No.

A73240

CAS No.

1392224-59-7

MyomiRs-IN-1

MyomiRs-IN-1 is a specific inhibitor targeting endogenous metabolites involved in muscle cell differentiation. It effectively downregulates myoD protein translation in C2C12 cells without altering myoD mRNA levels, thereby affecting the expression of muscle differentiation markers. By modulating the regulatory pathway between miR-221/222 and myoD, MyomiRs-IN-1 is a valuable tool for researchers investigating muscle development and associated disorders.

Cat. No.

A73241

CAS No.

111783-54-1

A 62176 hydrochloride

A 62176 hydrochloride is a potent inhibitor of DNA topoisomerase II, demonstrating significant activity in disrupting purine synthesis in cancer cells. By interacting with G-quadruplex structures, A 62176 hydrochloride reduces c-MYC mRNA expression and displaces nucleosomes from the non-template strand of rDNA. This mechanism leads to DNA damage that necessitates repair via BRCA1/2-mediated homologous recombination and DNA-PK-mediated non-homologous end-joining pathways, highlighting its potential applications in cancer research and therapeutic development.

Cat. No.

A73250

CAS No.

1604034-78-7

IRAK4-IN-29

IRAK4-IN-29 is a selective inhibitor of the interleukin-1 receptor-associated kinase 4 (IRAK4), demonstrating low nanomolar activity. This compound effectively disrupts TLR-mediated signaling pathways and exhibits significant inhibition of cytokine production in response to LPS and R848 stimulation. In vivo studies reveal that IRAK4-IN-29 can suppress LPS-induced TNFα, mirroring the phenotype observed in IRAK4 gene-deficient mice. Furthermore, IRAK4-IN-29 possesses favorable medicinal chemistry characteristics, including microsomal stability and solubility, indicating its potential for clinical applications in inflammatory diseases.

Cat. No.

A73287

CAS No.

380877-02-1

MMV667492

MMV667492 is a potent inhibitor of the cytoskeletal protein Ezrin, effectively targeting its function in cellular processes. This compound demonstrates significant anti-invasion activity in osteosarcoma cells, hindering their metastatic potential. In addition to its in vitro efficacy, MMV667492 induces distinct morphological defects in zebrafish embryos, aligning with Ezrin inhibition mechanisms. Furthermore, it reduces lung metastasis in osteosarcoma models characterized by elevated Ezrin expression, making it a valuable tool for studying tumor biology and metastasis.

Cat. No.

A73291

CAS No.

865531-74-4

PTC-510 free base

PTC-510 Free Base is a selective inhibitor of hypoxia-induced VEGF expression in tumor cells. It effectively reduces endogenous VEGF production under hypoxic conditions, demonstrating significant activity in controlling tumor growth while minimizing associated toxicity. This compound offers a novel therapeutic approach to overcome the limitations of existing anti-VEGF therapies, making it a valuable tool for cancer research and therapeutic development.