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Catalog No.
Product Name
Application
Product Information
Citations
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Apoptosis Inducer/Autophagy Inhibitor
Kumatakenin is a potent apoptosis inducer and autophagy inhibitor that targets ATG5 with a Kd value of 2.94 μM. It effectively enhances the activity of caspases 3, 8, and 9, leading to caspase-dependent apoptosis in ovarian cancer cells while modulating chemokines and pro-oncogenic factors. Kumatakenin also reduces M2 macrophage polarization, inhibits tumor progression in esophageal cancer by targeting FASN, and interacts with Eno3 to mitigate ferroptosis and alleviate intestinal inflammation. This compound is valuable for studies in ovarian cancer, esophageal cancer, depression, and colitis research. -
ULK1 Inhibitor
XST-14 is a potent and selective inhibitor of ULK1, demonstrating an IC50 of 26.6 nM. This compound effectively inhibits autophagy by decreasing the phosphorylation of ULK1 downstream substrates. XST-14 has been shown to induce apoptosis in hepatocellular carcinoma (HCC) cells, providing significant antitumor effects and contributing to ongoing cancer research and therapeutic studies. -
LRRK2 Inhibitor
LRRK2-IN-8 is a selective inhibitor of the leucine-rich repeat kinase 2 (LRRK2), effectively targeting both wild-type LRRK2 and the G2019S mutant with IC50 values under 10 nM. Additionally, this compound demonstrates inhibitory activity against TYK2 and NUAK1 with IC50 values ranging from 10 to 100 nM. LRRK2-IN-8 is valuable for research focused on neurodegenerative diseases linked to LRRK2, as well as studies aimed at exploring the functionality of TYK2 and NUAK1 in various cellular processes. -
LRRK2/NUAK1/TYK2 Inhibitor
LRRK2/NUAK1/TYK2-IN-1 is a potent inhibitor of LRRK2, NUAK1, and TYK2, exhibiting IC50 values under 10 nM for LRRK2 (Wt), LRRK2 (G2019), TYK2, and NUAK1. This compound is valuable for research in autoimmune diseases, providing insights into the mechanisms of inflammation and immune response modulation. Its high selectivity and efficacy make it a crucial tool for studying the roles of these kinases in various biological pathways. -
ULK1 Inhibitor
ULK1-IN-2 is a potent inhibitor of ULK1, a key regulator of autophagy. This compound exhibits significant cytotoxic effects against cancer cell lines, demonstrating an IC50 of 1.94 μM in A549 cells. ULK1-IN-2 not only induces apoptosis but also effectively inhibits autophagy, making it a valuable tool for research applications in non-small cell lung cancer (NSCLC) studies. -
Autophagy Inhibitor
Autophagy-IN-1 is a selective autophagy and mitophagy inhibitor that operates by enhancing autophagic flux while obstructing the fusion of autophagosomes and lysosomes in cancer cells. This compound demonstrates significant biological activity by inducing apoptosis and facilitating cell cycle arrest. Research applications include investigating its effects on tumor growth, particularly in colorectal cancer models, as evidenced by its ability to inhibit tumor growth in an HCT116 xenograft mouse model with minimal toxicity. -
Autophagy Inducer, NLRP3 Inhibitor
Britannin is an autophagy inducer and NLRP3 inflammasome inhibitor with an IC50 of 3.630 μM. It exhibits significant anti-inflammatory effects by disrupting the interaction between NLRP3 and NEK7, effectively preventing NLRP3 activation and assembly. Additionally, Britannin shows antitumor properties by inhibiting tumor cell proliferation through interference with the interaction of HIF-1α and Myc, leading to reduced PD-L1 expression and enhanced activity of cytotoxic T lymphocytes. This compound also promotes apoptosis and autophagy in liver cancer cells via activation of ROS-regulated AMPK, making it a valuable tool for research in anti-inflammatory and oncology studies. -
ULK1/2 inhibitor
DCC-3116 is an orally active inhibitor of ULK1/2 that suppresses autophagy in lung cancer cells. By targeting ULK1/2, DCC-3116 inhibits KRAS^G12C-driven signaling pathways, leading to reduced cell proliferation and demonstrating anti-tumor activity in KRAS-mutant lung cancer models. -
Autophagy inhibitor
Liensinine diperchlorate is a major isoquinoline alkaloid extracted from the seed embryo of *Nelumbo nucifera* Gaertn. It inhibits late-stage autophagy and mitophagy by blocking the fusion of autophagosomes with lysosomes. Liensinine diperchlorate exhibits a broad spectrum of biological activities, including anti-arrhythmic, antihypertensive, anti-pulmonary fibrosis effects, and vascular smooth muscle relaxation, making it a valuable compound for research in cardiovascular and pulmonary diseases, as well as autophagy-related disorders. -
TAK1 inhibitor
HS-276 is an orally bioavailable, potent, and highly selective inhibitor of transforming growth factor-β–activated kinase 1 (TAK1), with a Kᵢ of 2.5 nM. It exhibits strong inhibition of TAK1 and moderate activity against a panel of other kinases, including CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with respective IC₅₀ values ranging from 8.25 to 5585 nM. HS-276 is a valuable tool for investigating TAK1-mediated signaling pathways and holds therapeutic potential for inflammatory conditions such as rheumatoid arthritis (RA). -
PI3K-AKT Inhibitor
Alborixin is a potent inhibitor of the PI3K-AKT signaling pathway that promotes autophagy. It facilitates the clearance of intracellular and extracellular amyloid-β by upregulating key autophagy-related proteins such as BECN1, ATG5, and ATG7, while enhancing lysosomal activity. This mechanism yields a reduction in amyloid-β-mediated neurotoxicity, positioning Alborixin as a valuable tool for research related to Alzheimer's disease and other neurodegenerative conditions. -
CXCR4 Inhibitor
Hit 14 is a selective inhibitor of C-X-C chemokine receptor type 4 (CXCR4), demonstrating an IC50 value of 254 nM. This compound effectively inhibits the migration and invasion of MDA-MB-231 cells, highlighting its potential in cancer research. Furthermore, Hit 14 modulates Akt phosphorylation and exhibits anti-inflammatory properties, demonstrating efficacy in reducing ear swelling and damage in mouse models. Its diverse biological activities make it a valuable tool for studies related to cancer metastasis and inflammation. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
ELR+CXCL-CXCR1/2 Inhibitor
CXCL-CXCR1/2-IN-1 is an orally active inhibitor of the ELR+CXCL-CXCR1/2 signaling pathway, exhibiting an EC50 of 42.7 nM for the CXCR2 receptor. This compound demonstrates significant anticancer and antiangiogenic properties, making it a valuable tool for research into tumor progression and vascularization. Its ability to target these pathways underscores its potential application in cancer biology and therapeutic development. -
CXCR4 Inhibitor
CXCR4-IN-3 is a potent inhibitor of the CXCR4 receptor, demonstrating an IC50 of 3.2 nM. It exhibits significant antichemotactic effects, with an inhibition rate of 79.19±2.33%. This compound also displays anti-inflammatory properties, making it a valuable tool for research into inflammatory bowel disease (IBD) and related inflammatory conditions. -
CXCR4 Inhibitor
Peptide R is a cyclic peptide that functions as a specific antagonist of the CXCR4 receptor. It demonstrates significant efficacy in remodeling tumor stroma, making it a valuable tool for tumor research. Its ability to modulate the tumor microenvironment highlights its potential applications in cancer therapy and investigation into tumor progression mechanisms. -
CXCR4 Inhibitor
CXCR4-IN-1 is a selective inhibitor of the CXCR4 chemokine receptor, with an IC50 of 20 nM. This compound exhibits potential biological activity in modulating cellular responses associated with cancer progression, HIV infection, diabetic retinopathy, and inflammatory conditions. CXCR4-IN-1 is suitable for use in research applications focused on these disease processes, providing valuable insights into therapeutic targeting of the CXCR4 signaling pathway. -
CXCR2 Inhibitor
NVP CXCR2 20 is a selective inhibitor of the CXCR2 receptor, primarily involved in modulating pain pathways. It exhibits significant analgesic and antinociceptive effects, effectively reducing mechanical and thermal hypersensitivity in rat models of chronic constriction injury (CCI). Additionally, NVP CXCR2 20 diminishes CXCL3-induced hypersensitivity in naive mice and lowers CXCL3 protein levels in the spinal cord and dorsal root ganglia of CCI-exposed rats. This compound is valuable for research into neuropathic pain and chronic obstructive pulmonary disease (COPD). -
CXCL12 Inhibitor
4-Amino-D-phenylalanine is a potent CXCL12 inhibitor that targets the CXCR4 receptor. With an IC50 value of 0.1 μM, it effectively inhibits the binding of CXCL12 to its receptor. This compound is valuable for research applications focused on understanding CXCR4-related pathways and their implications in cancer, inflammation, and various other diseases. -
CXCR4 Inhibitor
vMIP-II (1-21) is a selective inhibitor of the chemokine receptor CXCR4. By competing with 125I-SDF-1R for binding sites, vMIP-II (1-21) effectively disrupts CXCR4 signaling, with an IC50 value of 190 nM. This compound is useful for research applications involving the study of chemokine receptors and their role in various biological processes, such as immune response and cancer metastasis. -
CXCR4 Inhibitor
TN14003 is a selective inhibitor of the CXCR4 receptor. It demonstrates significant antitumor activity by disrupting CXCR4-mediated signaling pathways, which are implicated in cancer cell survival, proliferation, and metastasis. This compound is primarily utilized in research focused on cancer treatment and understanding the role of the CXCR4 chemokine receptor in tumor progression. -
CXCR Inhibitor
AMD-3329 is a selective CXCR4 inhibitor that targets the chemokine receptor involved in HIV-1 and HIV-2 entry into host cells. By obstructing CXCR4, AMD-3329 effectively inhibits viral replication, making it a valuable tool in HIV research. This compound is suitable for studies focused on developing therapeutic strategies against X4-tropic HIV strains and understanding the mechanisms of viral entry and infection. -
HIV Inhibitor
KRH-3955 is a potent CXCR4 antagonist that demonstrates significant anti-HIV-1 activity, particularly against X4 strains. It effectively inhibits the replication of various X4 HIV-1 clinical isolates and is active against recombinant strains with resistance mutations in reverse transcriptase, protease, and tyrosinase. KRH-3955 disrupts the binding of SDF-1alpha to CXCR4, thereby interfering with calcium signaling through this receptor, along with inhibiting antibody binding to CXCR4. With an oral bioavailability of 25.6% in rats, KRH-3955 has shown efficacy in vivo, making it a valuable tool for HIV research. -
HIF Inhibitor
Arylsulfonamide 64B is a potent inhibitor of hypoxia-inducible factor (HIF). This compound effectively suppresses hypoxia/HIF-mediated expression of key oncogenes such as c-Met and CXCR4, thereby demonstrating significant anti-tumor activity. Arylsulfonamide 64B is particularly relevant for research focused on uveal melanoma, as it has been shown to reduce primary tumor growth and metastasis in mouse models. -
PPT1 Inhibitor
Ezurpimtrostat (hydrochloride) is a potent and selective PPT1 inhibitor with multiple biological activities. It disrupts lysosomal function, modulates autophagy, and induces apoptosis, making it a valuable tool in cancer research and immunology. This compound has demonstrated efficacy in reducing inflammatory markers such as IFN-α and CRP, as well as in lowering viral loads of SARS-CoV-2. Ezurpimtrostat is suitable for investigating conditions such as systemic lupus erythematosus, hepatocellular carcinoma, fibrosis, and other related disorders. -
CCR5/CXCR4 Chemotaxis Inhibitor
Catenarin, an anthraquinone compound, serves as an inhibitor of CCR5 and CXCR4-mediated chemotaxis. It effectively reduces the phosphorylation of mitogen-activated protein kinases (p38 and JNK) and their upstream kinases (MKK6 and MKK7), as well as calcium mobilization. Catenarin demonstrates anti-inflammatory properties and inhibits leukocyte migration, contributing to its potential in diabetes research. Additionally, it exhibits significant antibacterial activity against Gram-positive bacteria and has been shown to prevent type 1 diabetes in nonobese diabetic mice. -
CXCR5 Inhibitor
YU241279 is a selective inhibitor of CXCR5, targeting the CXCL13-mediated signaling pathways. It effectively inhibits Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells, leading to reduced proliferation of lymphoma cells. In preclinical studies, YU241279 demonstrated a significant reduction in tumor burden within the peripheral blood and bone marrow of mice with lymphoma. This compound is suitable for research into angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma.
