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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
LRRK2 Inhibitor
LY2023-001 is a selective inhibitor of the G2019S mutation in LRRK2, exhibiting a potent inhibitory activity with an IC50 of 12.9 nM. This compound interacts with critical residues, forming stable hydrogen bonds with Glu1948 and Ala1950 in the G2019S LRRK2 protein. It serves as a valuable tool for investigating the role of LRRK2 signaling in neurodegenerative disorders, facilitating research in cellular models and drug development for Parkinson's disease. -
LRRK2 Inhibitor
LRRK2-IN-12 is a potent inhibitor of LRRK2, effectively targeting G2019S (IC50=0.45 nM) and wild-type LRRK2 (IC50=1.1 nM), with a similar affinity for the wild-type enzyme in the presence of ADP (IC50=0.46 nM). This compound is valuable for research into neurodegenerative diseases, particularly in investigating the role of LRRK2 in Alzheimer's Disease. Its high specificity and low nanomolar activity make it an essential tool for exploring LRRK2-related pathways and therapeutic interventions. -
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. -
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. -
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. -
CXCR4 Inhibitor
MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. -
Mitochondrial respiratory chain inhibitor
Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain. -
LRRK2 kinase inhibitor
GSK2578215A is a potent leucine-rich repeat kinase 2 (LRRK2) inhibitor (IC50 values are 8.9 and 10.1 nM respectively for LRRK2[G2019S] mutant and wild-type LRRK2 respectively). -
LRRK2 Inhibitor III
HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2. -
15-LO inhibitor
PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis. -
Protein translocation Inhibitor
Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange. -
JAK1/2 inhibitor
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3. -
LRRK2 inhibitor
LRRK2-IN-1 inhibits both G2019S mutant and wild-type LRRK2 kinase activity with IC50 values of 6 and 13 nM respectively. -
JAK inhibitor
Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.
