Catalog No.
Product Name
Application
Product Information
Citations
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Autophagy Inducer
Loperamide hydrochloride is an opioid receptor agonist that functions primarily as an autophagy inducer. This compound selectively inhibits human intestinal carboxylesterases (hiCE), contributing to its anti-diarrheal properties. Its unique mechanism of action makes Loperamide hydrochloride a valuable reagent for studies related to gastrointestinal motility and autophagy modulation in various biological contexts. -
GPX4 Targeting AUTAC
GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader designed to selectively induce degradation of GPX4 through autophagy. By promoting the ubiquitination of GPX4 via E3 ligase TRAF6, it enhances the interaction with p62, facilitating the autophagy-dependent degradation process. GPX4-AUTAC has been shown to significantly induce ferroptosis and exhibit notable anti-cancer activity in breast cancer cells, breast cancer-derived organoids, and in the MDA-MB-231 tumor xenograft model. Additionally, it demonstrates potent synergistic effects when used in combination with drugs such as Sulfasalazine or traditional chemotherapy agents like Paclitaxel or Cisplatin. -
Apoptosis/Autophagy Inducer
Formosanin C is a diosgenin saponin that functions primarily as an apoptosis and autophagy inducer. It exhibits notable anti-tumor activities through mechanisms such as blocking the cell cycle, inhibiting metastasis, and promoting ferroptosis. Additionally, Formosanin C can suppress the NF-κB signaling pathway, providing anti-inflammatory effects while enhancing immune cell activity. This compound is relevant for research in anti-inflammatory, antifungal, and anti-cancer applications, particularly concerning lung, liver, breast, and colorectal cancers. -
Autophagy Inducer
(E,E)-Bisdemethoxycurcumin is an autophagy inducer derived from curcumin, exhibiting significant anti-inflammatory and anticancer properties. This compound has been shown to enhance cellular autophagy processes, making it a valuable tool for research into cancer biology and potential therapeutic strategies. Its ability to modulate inflammatory pathways also positions it as a candidate for studies relating to chronic inflammatory diseases. -
CXCR Inhibitor
Corydalmine, a CXCR inhibitor, demonstrates significant antifungal activity by inhibiting spore germination in various plant pathogenic and saprophytic fungi. Additionally, it serves as an oral analgesic agent, exhibiting potent analgesic effects. Corydalmine has been shown to alleviate Vincristine-induced neuropathic pain in murine models through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, making it a valuable tool for pain research and therapeutic applications. -
CXCR Inhibitor
Corydalmine hydrochloride is a potent CXCR inhibitor that demonstrates significant biological activity by inhibiting spore germination in certain plant pathogenic and saprophytic fungi. Additionally, it exhibits notable analgesic properties, effectively alleviating Vincristine-induced neuropathic pain in murine models. This effect is mediated through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, highlighting its potential applications in pain management research and fungal inhibition studies. -
Autophagy Enhancer
Corynoxine is a tetracyclic oxindole alkaloid derived from Uncaria rhynchophylla, acting primarily as an autophagy enhancer. It promotes the clearance of alpha-synuclein through the Akt/mTOR signaling pathway, making it a valuable tool for investigating neurodegenerative diseases and related cellular mechanisms. Its ability to modulate autophagy positions Corynoxine as a significant research reagent for studies focused on cellular stress responses and neuroprotection. -
Autophagy Inducer
Diazoxide is an ATP-sensitive potassium channel activator that induces autophagy through modulation of cellular ion balance. This compound demonstrates potential therapeutic effects in conditions related to hyperinsulinism. It is commonly utilized in research applications focusing on autophagy pathways and metabolic regulation. -
REV-ERB/Autophagy Inhibitor
ARN5187 trihydrochloride is a selective REV-ERBβ ligand that functions as an autophagy inhibitor. It exerts dual inhibitory effects on REV-ERB-mediated transcription and autophagy processes, demonstrating significant lysosomotropic properties. Additionally, ARN5187 trihydrochloride can induce apoptosis, making it a valuable tool for research in cellular metabolism and programmed cell death. Its biological activity positions it as a critical reagent for studies investigating the interplay between autophagy and transcriptional regulation. -
Autophagy Inducer
Physalin B is a potent autophagy inducer derived from Cape gooseberry, known for its steroidal properties. It has been shown to induce cell cycle arrest and promote apoptosis in breast cancer cells by modulating the p53-dependent apoptotic pathway. Additionally, Physalin B inhibits the ubiquitin-proteasome pathway and elicits an incomplete autophagic response in human colon cancer cells in vitro, making it a valuable tool for cancer research and the study of autophagic mechanisms. -
E3 ubiquitin ligase RNF5 Inhibitor
RNF5 inhibitor inh-02 is a selective inhibitor of the E3 ubiquitin ligase RNF5/RMA1, demonstrating significant biological activity by restoring F508del-CFTR function in F508del-CFTR-expressing immortalized cell lines (CFBE41o⁻, EC50 = 2.6 μM; FRT, EC50 = 2.2 μM). This compound promotes autophagy through increased LC3IIB expression and enhanced autophagic vacuole formation by reducing ATG4B ubiquitylation. RNF5 inhibitor inh-02 is valuable for research into cystic fibrosis and related cellular mechanisms. -
RNF5 Agonist
RNF5 Agonist 1 is a potent activator of RNF5, enhancing its biological function. This compound significantly increases the ubiquitylation of ATG4B in F508del-CFTR-expressing CFBE41o- cells, indicating its potential utility in studies of protein degradation pathways and cystic fibrosis research. RNF5 Agonist 1 serves as a valuable tool for investigating the role of RNF5 in cellular processes and therapeutic interventions. -
ULK1 Inhibitor
ULK-101 is a highly selective inhibitor of ULK1, demonstrating an IC50 of 1.6 nM for ULK1 and 30 nM for ULK2. This compound effectively suppresses autophagy processes, making it valuable for cancer research, particularly in studies focused on nutrient stress sensitivity in cancer cells. ULK-101 is suitable for applications requiring modulation of autophagy and exploration of related signaling pathways. -
ULK Inhibitor/ATG13 Degrader
SBP-1750 is a potent ULK1/2 inhibitor and an effective degrader of ATG13. It demonstrates strong inhibition of ULK1 and ULK2 with IC50 values of 8 nM and 50 nM, respectively, while inducing ATG13 degradation with an EC50 of 114 nM. By inhibiting autophagy, SBP-1750 can promote cell death in cancer cells, making it a valuable tool for research in cancer biology, particularly in the study of pancreatic cancer. -
ULK1 Kinase Inhibitor
ULK-100 is a potent and selective inhibitor of ULK1 kinase, exhibiting an IC50 value of 1.6 nM. This compound demonstrates significant biological activity in modulating autophagy processes, making it a valuable tool for research into autophagy-related diseases, such as KRAS-mutant lung cancer and glioblastoma. Its specificity for ULK1 allows for targeted studies in cancer biology and therapeutic development. -
ULK1 Inhibitor
SR-17398 is a selective inhibitor of Unc-51-Like Kinase 1 (ULK1), exhibiting an IC50 value of 22.4 μM. Inhibition of ULK1 by SR-17398 has been shown to impact autophagy and cellular metabolism, making it a valuable tool for researchers studying these processes. This compound is applicable in research investigating the role of ULK1 in various diseases, including cancer and neurodegeneration. -
AUTAC
HaloAUTAC tt15 is an autophagy-targeting chimera (AUTAC) designed to selectively induce the degradation of Halo Tag-conjugated proteins through autophagy. This compound effectively promotes the clearance of unwanted proteins and can be utilized in studies exploring cellular homeostasis, protein turnover, and the roles of autophagy in various diseases. Its ability to target specific proteins makes it a valuable tool for researchers investigating autophagic pathways and protein quality control mechanisms. -
Tag-linker Conjugate of AUTAC
FBnG-(Cys-acetamide)-CH2-PEG3-CH2-CH2-CH2-NH2 is a tag-linker conjugate of AUTAC designed to facilitate targeted protein degradation. This compound integrates a p-fluorobenzylguanine (FBnG) tag with a glycol spacer, enabling effective K63-linked polyubiquitination. It demonstrates significant biological activity by promoting the degradation of mitochondrial proteins in HeLa cells, making it a valuable tool for researchers studying mitochondrial dynamics and protein homeostasis. -
AUTAC Control
YT 6-2 is an autophagy-targeting ligand (ATL) that targets p62/SQSTM1, functioning as a control for the AUTAC mechanism. This compound plays a crucial role in enhancing the degradation of the androgen receptor (AR), leading to a reduction in nuclear AR levels and subsequent downregulation of AR target gene expression, including AR-v7. Additionally, YT 6-2 demonstrates efficacy against common AR mutants, making it a valuable tool for research in prostate cancer (PCa) therapies and the study of AR pathway modulation. -
AUTAC Autophagy Tag
Cys-C-cGMP is an autophagy tag designed for AUTACs that facilitates the selective degradation of target proteins through autophagy. It enhances K63-linked ubiquitination of mitochondria in HeLa cells, thereby promoting cellular quality control and elimination of damaged organelles. This compound is valuable for studying autophagy-related pathways and the development of targeted protein degradation strategies. -
AUTAC Ligand
TSPO ligand-3 serves as a ligand for AUTAC2, which features a p-fluorobenzylguanine (FBnG) moiety alongside a synthetic FKBP ligand (SLF). This compound exhibits notable biological activity by significantly silencing FKBP12 in HeLa cells. Research applications include studying targeted protein degradation and investigating the mechanistic pathways of autophagy-related and intracellular degradation processes. -
LC3 Ligand
TH152 is a reversible pan ligand targeting LC3/GABARAP, exhibiting a dissociation constant (KD) of 2 µM. This compound plays a critical role in autophagy regulation, making it valuable for studies investigating autophagic processes and cellular homeostasis. TH152 can be utilized in research delineating the roles of LC3/GABARAP in various biological systems and disease models. -
PAD4 Inhibitor
JBI-589 is a non-covalent inhibitor selectively targeting the PAD4 isoform. This compound effectively reduces CXCR2 expression and inhibits neutrophil chemotaxis, making it instrumental in the study of inflammatory processes. JBI-589 demonstrates potential in diminishing primary tumors and metastases while enhancing the efficacy of checkpoint inhibitors. It is suitable for various applications in cancer research. -
RDC-related Molecule
NOTA-NHS ester is a chelating agent that allows for the creation of radiolabeled compounds, specifically through coupling with T140 to form NOTA-T140. This compound can then be radiolabeled with Al[18F], enabling visualization of tumor uptake that correlates with CXCR4 expression levels. Al[18F]NOTA-T140 is particularly valuable for PET imaging studies of tumors. Additionally, NOTA-NHS ester serves as a versatile tool for fluorescent labeling in various biological applications. -
CXCR4 Targeting Peptide
Pentixafor is a synthetic peptide that targets the CXCR4 receptor, playing a critical role in various cellular processes, including cell migration and signaling. This compound can be labeled with 68Gallium (68Ga), enabling its application in positron emission tomography (PET) imaging for assessing CXCR4 expression in vivo. Additionally, Pentixafor serves as a vital component in the development of Radionuclide-Drug Conjugates (RDCs) for targeted cancer therapies. -
Endoradiotherapeutic vector
Anditixafortide is a CXCR4-targeting peptide derivative that functions as an endoradiotherapeutic vector. This reagent is primarily utilized in the synthesis and research of Radionuclide-Drug Conjugates (RDCs), leveraging its ability to selectively target CXCR4-expressing cells. Its application is significant in the field of targeted cancer therapies, facilitating precise delivery of therapeutic radionuclides to tumor sites. -
Liposome
DOTA Conjugated JM#21 derivative 7 is a CXCR4-targeting peptide conjugated with DOTA, designed for the synthesis of radioligands. When radiolabeled as 177Lu-DOTA, it demonstrates superior targeting of CXCR4-expressing tumors while exhibiting minimal uptake in non-targeted organs, except for the kidneys. This compound is ideal for research applications involving Radionuclide-Drug Conjugates (RDCs), facilitating advancements in targeted radiotherapy. -
LRRK2 Inhibitor
Lu AF58786 is a selective inhibitor of LRRK2, demonstrating potent activity with an IC50 of 12 nM. It effectively inhibits both the LRRK2 G2019S and LRRK2 A2016T mutations, with IC50 values of 19 nM and 93 nM, respectively. Additionally, Lu AF58786 prevents the phosphorylation of LRRK2, Rab10, and Rab12 in human peripheral blood mononuclear cells. This compound is suitable for research applications focused on Parkinson's disease. -
PROTAC LRRK2 Degrader
PROTAC LRRK2 Degrader-4 is a potent PROTAC designed to target and degrade LRRK2 with a DC50 of 0.79 nM. It exhibits significant biological activity, making it a valuable tool for research into Parkinson's disease and associated inflammatory pathways. This compound enables studies into the modulation of LRRK2 levels, thereby facilitating deeper understanding of its role in neurodegeneration and inflammation. -
LRRK2 PROTAC Degrader
PROTAC LRRK2 Degrader-1 is a targeted protein degrader that selectively engages leucine-rich repeat kinase 2 (LRRK2), exhibiting an IC50 value of less than 10 nM. This compound is designed for the study of LRRK2-mediated pathways and offers significant potential for advancing research on Parkinson's disease. Its ability to induce targeted degradation makes it a valuable tool for investigating therapeutic strategies in neurodegenerative disorders associated with LRRK2 dysregulation. -
LRRK2 PROTAC Degarder
JH-XII-03-02 is a potent and selective LRRK2 PROTAC degrader. It induces targeted degradation of LRRK2 protein, making it a valuable tool for investigating the role of LRRK2 in Parkinson's disease. This compound is suitable for research applications focused on elucidating LRRK2 function and exploring therapeutic strategies for neurodegenerative disorders. -
LRRK2 Inhibitor
EB-42486 is a potent and highly selective inhibitor of the G2019S mutant variant of LRRK2, exhibiting an IC50 of less than 0.2 nM. This compound demonstrates significant biological activity in cellular models, making it a valuable tool for investigating the role of LRRK2 in Parkinson's disease. Researchers can utilize EB-42486 to explore potential therapeutic strategies aimed at modulating LRRK2 activity in neurodegenerative disorders. -
LRRK2 Kinase Inhibitor
LRRK2-IN-7 is a potent and selective inhibitor of the LRRK2 kinase, exhibiting an IC50 of 0.9 nM. This compound demonstrates over 1000-fold selectivity against other kinases, ion channels, and cytochrome P450 enzymes. Due to its ability to penetrate the central nervous system (CNS), LRRK2-IN-7 is valuable for studies related to neurodegenerative diseases and the physiological roles of LRRK2 in cellular signaling pathways. -
LRRK2 Inhibitor
MK-1468 is a selective LRRK2 inhibitor known for its oral bioavailability and ability to cross the blood-brain barrier. This compound has demonstrated significant potential in studying the pathophysiology of Parkinson's disease, making it a valuable tool for researchers investigating therapeutic mechanisms and interventions in neurodegenerative disorders related to LRRK2 activity. -
LRRK2 Inhibitor
GNE-7915 tosylate is a potent and selective inhibitor of LRRK2, exhibiting an IC50 of 9 nM. This compound demonstrates effective brain penetration, making it a valuable tool for studying LRRK2-related pathways in neurological diseases. Its specificity allows for targeted research into the role of LRRK2 in conditions such as Parkinson's disease and other neurodegenerative disorders. -
LRRK2 Inhibitor
LRRK2-IN-2 is a potent and selective inhibitor of the Leucine-rich repeat kinase 2 (LRRK2) with an IC50 of less than 0.6 nM. This orally active compound demonstrates excellent brain penetration, making it valuable for studies focused on Parkinson’s disease. Its specificity and efficacy support a range of neurobiological research applications related to LRRK2's role in neurodegeneration. -
LRRK2 Inhibitor
LRRK2-IN-3 is a potent and selective inhibitor of LRRK2, exhibiting an IC50 of 2.6 nM in human peripheral blood mononuclear cells (PBMCs). This orally active compound demonstrates effective brain penetration, making it an invaluable tool for studying LRRK2's role in neurodegenerative disorders. Its application in Parkinson's disease research allows for deeper insights into disease mechanisms and therapeutic strategies targeting LRRK2 pathways. -
LRRK2 Inhibitor
LRRK2-IN-16 is a selective inhibitor of the LRRK2 kinase with an IC50 value of less than 5 μM. This compound is valuable for investigating neurodegenerative and autoimmune disorders, providing insights into the role of LRRK2 in these pathologies. Its use in research can enhance understanding of disease mechanisms and aid in the development of therapeutic strategies targeting LRRK2. -
G2019S-LRRK2 Kinase Inhibitor
LRRK2-IN-10 is a potent and mutation-selective inhibitor targeting the G2019S variant of LRRK2 kinase. It exhibits IC50 values of 11 nM and 5.2 nM for phosphorylated sites pS935 and pS1292, respectively, demonstrating its effectiveness in modulating LRRK2 activity. This compound is particularly valuable for research related to Parkinson’s disease, offering insights into the mechanisms of G2019S-LRRK2 in neurological contexts. -
LRRK2 Inhibitor
CZC-54252 hydrochloride is a potent and selective inhibitor of LRRK2, exhibiting IC50 values of 1.28 nM for wild-type and 1.85 nM for the G2019S mutant variant. This compound effectively attenuates G2019S LRRK2-induced neuronal injury, with an EC50 of approximately 1 nM, showcasing its neuroprotective properties. CZC-54252 hydrochloride is valuable for research applications focused on neurodegenerative diseases associated with LRRK2 modulation. -
LRRK2 Inhibitor
SRI-31255 is an orally active inhibitor of Leucine-rich repeat kinase 2 (LRRK2), exhibiting IC50 values of 520 nM and 427 nM for human wild-type and G2019S mutant forms, respectively. By binding to the ATP-binding pocket of LRRK2, SRI-31255 effectively inhibits kinase activity, providing neuroprotective effects. This compound is a valuable tool for research aimed at developing LRRK2-targeted therapies for Parkinson's disease. -
LRRK2 Inhibitor
LRRK2-IN-14 is a potent LRRK2 inhibitor with a remarkable IC50 of 6.3 nM specifically targeting the LRRK2(G2019S) mutation. This compound exhibits significant inhibitory activity against hERG with an IC50 of 22 μM. Notably, LRRK2-IN-14 demonstrates permeability across the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases related to LRRK2 dysregulation. Its pharmacological profile positions it as a promising candidate for research applications in Parkinson's disease and other related disorders. -
LRRK2 Inhibitor
LRRK2-IN-6 is a selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with potent activity demonstrated by IC50 values of 4.6 μM for GS LRRK2 and 49 μM for wild-type LRRK2. This compound effectively inhibits autophosphorylation at Ser1292 and Ser925, key sites associated with LRRK2 activity. LRRK2-IN-6's ability to cross the blood-brain barrier makes it a valuable tool for research in neurodegenerative diseases linked to LRRK2 dysregulation. -
LRRK2 Inhibitor
SRI-29132 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2). It exhibits significant activity in modulating LRRK2-related pathways, making it a valuable tool for investigating the pathophysiology of Parkinson's disease and the development of potential therapeutic strategies. Research utilizing SRI-29132 can provide insights into the role of LRRK2 in neurodegenerative processes and neuronal signaling. -
PROTAC LRRK2 Degrader
PROTAC LRRK2 Degrader-3 primarily targets the LRRK2 protein through a PROTAC mechanism, exhibiting a DC50 of 0.17 nM. This compound effectively promotes the degradation of LRRK2, making it a valuable tool for research in Parkinson’s disease and inflammation. Its unique structure comprises a specific LRRK2 ligand, a Cereblon ligand, and an optimized linker, facilitating targeted therapeutic investigations. -
LRRK2 Inhibitor
LRRK2-IN-20 is a selective inhibitor of the leucine-rich repeat kinase 2 (LRRK2), exhibiting a pIC50 of 0.7921 nM. This compound is primarily utilized in the study of Parkinson's disease, enabling researchers to explore LRRK2's role in disease pathology and therapeutic interventions. Its potent inhibition provides a valuable tool for investigating the underlying mechanisms of neurodegeneration and potential treatment strategies. -
LRRK2 Inhibitor
LRRK2-IN-4 is a potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2), exhibiting an IC50 of 2.6 nM. This compound demonstrates good central nervous system penetration and oral bioavailability, making it a valuable tool for studying LRRK2's role in cellular signaling. LRRK2-IN-4 is particularly relevant for research into Parkinson’s disease, providing a means to explore therapeutic strategies targeting this kinase in related pathophysiological contexts. -
LRRK2 Inhibitor
PF-06455943 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2) with an IC50 of 3 nM. This compound also functions as a PET radioligand, making it valuable for imaging studies. PF-06455943 is primarily utilized in research investigating ADME/neuro pharmacokinetics and offers insights into pathophysiological mechanisms associated with Parkinson's disease (PD). -
LRRK2 Inhibitor
LRRK2-IN-5 is a selective inhibitor of the leucine-rich repeat kinase 2 (LRRK2), demonstrating potent inhibitory activity with IC50 values of 1.2 μM for GS LRRK2 and 16 μM for wild-type LRRK2. This compound effectively inhibits LRRK2 autophosphorylation at the Ser1292 and Ser925 sites, making it a valuable tool for studying LRRK2's role in various neurological disorders. Additionally, LRRK2-IN-5 is capable of crossing the blood-brain barrier, facilitating its application in central nervous system research. -
LRRK2 Kinase Inhibitor
(R,R)-LRRK2-IN-7 is a selective LRRK2 kinase inhibitor, exhibiting a potent inhibitory activity with an IC50 of 0.9 nM. This compound demonstrates over 1000-fold selectivity against various other kinases, ion channels, and CYP enzymes, making it a valuable tool for studies involving LRRK2-associated pathologies. Its ability to penetrate the central nervous system (CNS) enhances its relevance for research applications in neurodegenerative diseases.
