Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
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. -
CXCR4 Antagonist
Mavorixafor trihydrochloride is a potent and selective antagonist of the CXCR4 receptor, exhibiting an IC50 of 13 nM in inhibiting CXCR4 125I-SDF binding. This compound has demonstrated significant antiviral activity by inhibiting the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs, with IC50 values of 1 nM and 9 nM, respectively. Mavorixafor trihydrochloride is applicable in research studying WHIM syndrome and various CXCR4-related biological processes. -
CCR7 and CXCR2 Antagonist
Cosalane is a dual antagonist of the chemokine receptors CCR7 (IC50 = 2.43 μM) and CXCR2 (IC50 = 0.66 μM). This compound effectively inhibits HIV replication across a variety of strains, including HIV-1, HIV-2, Rauscher murine leukemia virus, as well as herpes simplex viruses HSV-1 and HSV-2, and human cytomegalovirus. Cosalane disrupts the interaction between gp120 and CD4, inhibiting signaling downstream of CCR7 in response to its ligands CCL19 and CCL21. Research applications include studies on HIV and the potential modulation of acute graft-versus-host disease in allogeneic hematopoietic stem cell transplantation. -
CXCR4 Antagonist
TC14012 is a peptidomimetic antagonist targeting the chemokine receptor CXCR4, exhibiting a high level of selectivity with an IC50 of 19.3 nM. In addition, TC14012 acts as a potent agonist for CXCR7, demonstrating an EC50 of 350 nM in β-arrestin 2 recruitment assays. This compound is utilized in research focused on HIV and cancer therapy, showcasing its potential in modulating chemokine signaling pathways. -
CXCR4 Antagonist
FC131 TFA is a potent CXCR4 antagonist that effectively inhibits the binding of [125I]-SDF-1 to CXCR4, demonstrating an IC50 value of 4.5 nM. This compound exhibits significant anti-HIV activity, making it a valuable tool for research in HIV treatment and other CXCR4-related studies. Its ability to disrupt CXCR4 signaling can be explored in various biological contexts, including cancer metastasis and immune response regulation. -
CXCR4 Antagonist
AMD 3465 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of both the 12G5 monoclonal antibody and CXCL12AF647 to CXCR4, demonstrating IC50 values of 0.75 nM and 18 nM in SupT1 cells, respectively. Additionally, AMD 3465 significantly impedes the replication of X4-tropic HIV strains, with IC50 values ranging from 1 to 10 nM, while showing no activity against CCR5-using (R5) viruses. This compound is suitable for research applications focusing on HIV treatment and CXCR4-related signaling pathways. -
CXCR4 Antagonist
KRH-3955 hydrochloride is a potent CXCR4 antagonist that effectively inhibits the binding of SDF-1α to CXCR4 with an IC50 of 0.61 nM. This compound demonstrates strong selectivity and efficacy against X4 HIV-1, with an EC50 ranging from 0.3 to 1.0 nM. KRH-3955 hydrochloride is suitable for research applications focused on HIV-1 pathogenesis and CXCR4-related signaling pathways. -
CXCR4 Antagonist
FC131 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of [125I]-SDF-1 to CXCR4 with an IC50 value of 4.5 nM. Due to its mechanism of action, FC131 demonstrates significant anti-HIV activity, making it a valuable tool for research into HIV pathogenesis and potential therapeutic interventions. -
Stable Isotope
Plerixafor-d4 is a deuterated derivative of Plerixafor, a selective antagonist of the CXCR4 receptor with an IC50 of 44 nM. This compound serves as an immunostimulant and is known for its ability to mobilize hematopoietic stem cells (HSCs). Additionally, Plerixafor has demonstrated efficacy in inhibiting HIV-1 and HIV-2 replication, with an EC50 ranging from 1 to 10 nM. Plerixafor-d4 is useful in research applications requiring stable isotopes for tracking and quantification purposes. -
HIV-1 Entry Inhibitor
RPR103611 is a derivative of betulinic acid that functions as a potent HIV-1 entry inhibitor. It displays IC50 values of 80 nM for CCR5-tropic virus YU2, 0.27 nM for CXCR4-tropic virus NL4-3, and 0.17 nM for dual tropic virus 89.6. This compound is valuable for research focused on the mechanisms of HIV-1 entry and the development of antiviral therapies. -
CXCR4 Antagonist
CXCR4 antagonist 7 is a potent CXCR4 antagonist with an IC50 of 9.3 nM. It effectively inhibits CXCR4 receptor activity, making it a valuable tool in the investigation of HIV infection, inflammatory diseases, cancer, and WHIM syndrome. This compound provides essential insights into the roles of CXCR4 signaling in various pathological conditions. -
CXCR Inhibitor
AMD 3329 octahydrobromide is a potent CXCR4 inhibitor that effectively reduces HIV-1 and HIV-2 viral replication. It demonstrates exceptional antiviral activity with EC50 values of 0.8 nM and 1.6 nM, surpassing the efficacy of related compounds. Additionally, AMD 3329 significantly obstructs the binding of specific CXCR4 monoclonal antibodies and inhibits SDF-1 alpha-induced Ca(2+) influx. This compound also disrupts virus-induced syncytium formation, with an EC50 of 12 nM, making it a valuable tool for HIV research and therapeutic development. -
CXCR6 Antagonist
ML339 is a selective antagonist of the CXCR6 receptor, displaying an IC50 of 140 nM. It inhibits β-arrestin recruitment and the cAMP signaling pathway induced by CXCL16 in human CXCR6, with IC50 values of 0.3 μM and 1.4 μM, respectively. While exhibiting reduced efficacy against mouse CXCR6 with an IC50 of 18 μM, ML339 demonstrates no significant inhibition of CXCR5, CXCR4, or the apelin receptor (APJ), with IC50 values exceeding 79 μM. This compound shows promise for advancing research focused on prostate cancer. -
CXCR Inhibitor
ALX 40-4C is a small peptide inhibitor targeting the chemokine receptor CXCR4. It effectively prevents the binding of SDF-1 to CXCR4 with a Ki of 1 μM, thereby inhibiting the replication of X4 strains of HIV-1. Additionally, ALX 40-4C Trifluoroacetate serves as an antagonist of the APJ receptor, exhibiting an IC50 value of 2.9 μM. This dual activity makes ALX 40-4C a valuable tool for research in HIV-1 studies and chemokine receptor signaling pathways. -
CXCR Receptor Inhibitor
SCH-900875 is a selective inhibitor of the CXCR3 receptor, known for its oral bioavailability and ability to penetrate the blood-brain barrier. By binding to CXCR3, it effectively prevents the interaction of ligands CXCL9, CXCL10, and CXCL11, thereby inhibiting downstream G protein and β-arrestin signaling pathways, which reduces inflammatory cell migration. This compound holds potential for investigating various autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis, as well as inflammatory conditions like psoriasis and inflammatory bowel disease. -
CXCR7 Antagonist
CXCR7 antagonist-1 functions as a CXCR7 antagonist by inhibiting the binding of the SDF-1 (CXCL12) and I-TAC (CXCL11) chemokines to the CXCR7 receptor. This inhibition plays a critical role in suppressing tumor cell proliferation and tumor growth, thereby providing potential therapeutic applications in cancer treatment. Additionally, CXCR7 antagonist-1 may be beneficial in the study and management of various inflammatory diseases and other pathologies associated with the CXCR7 pathway. -
CXCR7 Antagonist
CXCR7 antagonist-1 hydrochloride functions as an antagonist to the CXCR7 receptor, effectively inhibiting the binding of the SDF-1 chemokine (CXCL12) and I-TAC (CXCL11). This compound demonstrates significant potential in research related to tumor cell proliferation and formation, as well as in inflammatory diseases and other pathologies associated with CXCR7 signaling. Its ability to modulate chemokine receptor activity makes it a valuable tool for exploring therapeutic strategies in cancer and inflammation. -
CXCR2/CCR7 Antagonist
CXCR2/CCR7 antagonist-1 is a potent dual antagonist of the chemokine receptors CXCR2 and CCR7, exhibiting IC50 values of 0.0046 μM and 0.0014 μM, respectively. This compound serves as a valuable tool in the investigation of cancer metastasis and the mechanisms underlying autoimmune diseases, facilitating the study of therapeutic strategies targeting these pathways. Its efficacy in inhibiting both receptors makes it suitable for a range of biochemical and pharmacological research applications. -
CCR6/CXCR2 Antagonist
SQA1 is a squaramide derivative that functions as a CCR6 and CXCR2 antagonist, displaying a dissociation constant (Kd) of 250 nM. It effectively occupies the intracellular pocket, overlapping with the G protein binding site, which helps stabilize the closed conformation of the receptor. This compound is useful in research applications targeting chemokine receptor signaling pathways and their roles in inflammatory responses and immune cell trafficking. -
CCR5/CXCR3 Inhibitor
CCR5/CXCR3-IN-1 is a potent inhibitor of the chemokine receptors CXCR3 and CCR5. This compound effectively suppresses the chemotaxis of transformed cells expressing CCR5 and CXCR3, while exhibiting no inhibitory effect on CXCR4-expressing transfected cells. CCR5/CXCR3-IN-1 is valuable for research into chronic arthritic rheumatism and other conditions where modulation of these receptors is crucial. -
CXCR Antagonist
ACT-1004-1239 is a selective antagonist of the CXCR7 receptor, exhibiting a potent inhibitory effect with an IC50 value of 3.2 nM. This compound is primarily utilized in research focused on chemokine signaling pathways and is relevant in studies investigating disorders related to the immune system and cancer. Its oral bioactivity makes it an attractive candidate for in vivo investigations targeting CXCR7-mediated pathways. -
CXCR4 Receptor Agonist
NUCC-390 dihydrochloride is a selective small-molecule agonist of the CXCR4 receptor. It promotes the internalization of CXCR4 receptors and exhibits effects that are opposite to those of conventional CXCR4 antagonists. This compound has demonstrated the potential to enhance nerve recovery following neurodegeneration in vivo, making it a valuable tool for research in neurobiology and therapeutic applications targeting nerve regeneration. -
CXCR3 Antagonist
ACT-777991 is a selective antagonist of the CXCR3 receptor, demonstrating oral bioavailability. This compound effectively inhibits the migration of activated T cells in response to CXCL11, making it a useful tool for studying immune responses and inflammatory conditions. Its stability in microsomes and hepatocytes across various animal models further supports its potential applications in pharmacological research related to autoimmune diseases and cancer immunotherapy. -
ACKR7 Agonist
VUF11207 fumarate is a selective agonist of the ACKR7 receptor (formerly known as CXCR7). This compound effectively inhibits CXCL12-induced osteoclastogenesis and bone resorption by preventing ERK phosphorylation. VUF11207 fumarate is valuable for research targeting bone metabolism and related pathologies, making it a key tool for studying the role of ACKR7 in bone homeostasis and signaling pathways. -
CXCR3 Agonist
PS372424 hydrochloride is a selective agonist of the CXCR3 receptor, a key player in immune response modulation. This compound exhibits anti-inflammatory properties by inhibiting human T-cell migration, making it valuable for research into inflammatory diseases, particularly in models of arthritic inflammation. Its ability to target CXCR3 offers insight into the therapeutic potential for treating conditions characterized by dysregulated T-cell activity. -
CXCR2/1 Antagonist
SX-517 is a dual antagonist of CXCR2 and CXCR1, featuring a boronic acid structure. It effectively inhibits CXCL1-induced calcium flux with an IC50 of 38 nM and disrupts CXCL8-induced [(35)S]GTPγS binding, showing an IC50 of 60 nM, while also preventing ERK1/2 phosphorylation. This compound demonstrates significant anti-inflammatory properties in both humanized polymorphonuclear (PMN) cells and murine models, making it a valuable tool for research into inflammation-related pathways. -
Isomer
(Rac)-Reparixin is an isomer of Reparixin and serves as a useful experimental control in research settings. Reparixin functions as a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2, exhibiting inhibitory constants (IC50) of 1 nM and 100 nM, respectively. This compound is valuable for studies focusing on inflammation, cancer biology, and other pathways mediated by chemokine signaling. -
Dual CXCR1/2 Antagonist
Ladarixin sodium is a dual antagonist of CXCR1 and CXCR2, exhibiting an allosteric non-competitive mechanism. This compound demonstrates significant anti-inflammatory activity, making it relevant for research in chronic obstructive pulmonary disease (COPD) and asthma. Its ability to inhibit CXCR1 and CXCR2 pathways positions Ladarixin sodium as a valuable tool for exploring therapeutic strategies in respiratory inflammatory conditions. -
CXCR2 Antagonist
CXCR2-IN-2 is a selective antagonist of the CXCR2 receptor, demonstrating high potency with an IC50 of 5.2 nM in a β-arrestin assay and 1 nM in the CXCR2 Tango assay. This compound exhibits significant selectivity, being approximately 730-fold more selective for CXCR2 over CXCR1 and greater than 1900-fold over other chemokine receptors. Additionally, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood with an IC50 of 0.04 μM, making it a valuable tool for research into inflammatory processes and associated therapeutic applications. -
CXCR Modulator
CXCR7 modulator 2 is a selective modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), exhibiting an affinity with a Ki value of 13 nM. This compound plays a critical role in research applications focusing on chemokine signaling pathways and their involvement in various physiological and pathological processes. It is particularly useful in studies related to cancer metastasis, inflammation, and cardiovascular diseases, making it a valuable tool for understanding CXCR7's biological functions. -
CXCR2 Antagonist
CXCR2 antagonist 8 is a potent and selective antagonist of the CXCR2 receptor, involved in inflammatory responses and immune cell migration. This compound has demonstrated significant activity in models of insulin resistance, making it a valuable tool for investigating metabolic disorders and related signaling pathways. Researchers can utilize CXCR2 antagonist 8 for studies aimed at elucidating the role of CXCR2 in various disease states. -
CXCR4 Receptor Agonist
NUCC-390 is a selective small-molecule agonist of the CXCR4 receptor. This compound induces internalization of CXCR4 receptors, thereby modulating signaling pathways distinct from antagonists. Research indicates that NUCC-390 promotes functional recovery of nerve tissue following neurodegeneration, making it a valuable tool for applications related to neurobiology and regenerative medicine. -
CXCR4 Antagonist
EPI-X4 is a selective antagonist of the C-X-C motif chemokine receptor 4 (CXCR4), exhibiting an IC50 of 8.6 μM. This compound effectively inhibits CXCL12-mediated signaling and reduces chemokine-driven migration and invasion in leukemia cells. Additionally, EPI-X4 demonstrates anti-inflammatory properties in mouse models and displays antiviral activity against CXCR4-tropic HIV, making it a valuable tool for research in cancer, inflammation, and virology. -
CXCR3 Antagonist
ACT-660602 is an orally active antagonist of the chemokine receptor CXCR3, demonstrating an IC50 value of 204 nM. This compound effectively inhibits T-cell migration, making it a valuable tool in the study of immune response. ACT-660602 has shown efficacy in models of acute lung injury and is relevant for research focused on autoimmune diseases and related inflammatory conditions.
