GPCR/G Protein

Items 4751-4800 of 5455

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  1. ICMT Inhibitor

    ICMT-IN-38 is a selective inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.049 μM. This compound is valuable for investigating the role of ICMT in post-translational modifications and its implications in various biological processes. Research applications include studies on cancer biology and cellular signaling pathways, where modulation of ICMT activity may reveal novel therapeutic targets.
  2. ICMT Inhibitor

    ICMT-IN-43 is a potent inhibitor of the isoprenylcysteine carboxyl methyltransferase (ICMT) enzyme, with an IC50 value of 0.04 μM. This compound is instrumental in studying the role of protein methylation in various cellular processes and signaling pathways. ICMT-IN-43 can be utilized in research focused on cancer biology, neurodegenerative diseases, and other pathologies linked to post-translational modifications.
  3. ICMT Inhibitor

    ICMT-IN-39 is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 of 0.031 μM. This compound effectively disrupts the methylation process of isoprenylated proteins, providing valuable insights into cellular signaling pathways. ICMT-IN-39 is applicable in research focused on the roles of protein modification in various diseases, including cancer and neurodegenerative disorders.
  4. ICMT Inhibitor

    ICMT-IN-32 is a selective inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), showcasing an IC50 value of 0.777 μM. This compound is utilized in biochemical research to examine the role of ICMT in post-translational modifications of proteins. Its inhibitory properties make it valuable for studying signaling pathways and cellular processes related to protein farnesylation.
  5. ICMT Inhibitor

    ICMT-IN-23 is a selective inhibitor of Isoprenylcysteine carboxylmethyltransferase (ICMT), exhibiting an IC50 value of 0.123 μM. This compound plays a crucial role in studying post-translational modifications involved in protein function and stability. ICMT-IN-23 is valuable for research applications focusing on signal transduction, protein interaction studies, and the development of novel therapeutic strategies targeting ICMT.
  6. ICMT Inhibitor

    ICMT-IN-10 is a selective inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), with an IC50 value of 0.184 μM. This compound effectively disrupts the methylation of isoprenylated proteins, thereby playing a critical role in various signaling pathways. ICMT-IN-10 is valuable for studying the biological implications of ICMT in cancer research and potentially in other diseases associated with aberrant protein methylation.
  7. ICMT Inhibitor

    ICMT-IN-25 is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), with an IC50 value of 0.025 μM. This compound is significant in biochemical research focused on post-translational modifications, particularly in the study of protein localization and function mediated by ICMT. Its application extends to the investigation of cancer biology and other diseases where ICMT plays a crucial role in regulating protein activity.
  8. ICMT Inhibitor

    ICMT-IN-53 is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.96 μM. This compound demonstrates significant antiproliferative activity, effectively inhibiting the growth of MDA-MB-231 and PC3 cancer cell lines with IC50 values of 5.14 μM and 5.88 μM, respectively. ICMT-IN-53's PAMPA permeability makes it suitable for various biological research applications, particularly in the study of cancer cell proliferation and signaling pathways.
  9. ICMT Inhibitor

    ICMT-IN-48 is a competitive inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), with a Km of 13 μM for the prenylated methyl acceptor, the enzyme's initial substrate. This compound effectively inhibits ICMT activity, demonstrating IC50 values of 3.5 μM at 1×Km S-adenosylmethionine (SAM) and 2.3 μM at 10×Km SAM. ICMT-IN-48 is valuable for studying the role of ICMT in cellular signaling and post-translational regulation related to prenylated proteins in various biological systems.
  10. ICMT Inhibitor

    ICMT-IN-45 is a selective inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 of 0.132 μM. This compound disrupts the post-translational modification of proteins, thereby influencing signaling pathways associated with cancer and other diseases. ICMT-IN-45 is useful in research applications aimed at understanding ICMT-related biological processes and evaluating the potential therapeutic effects of ICMT inhibition.
  11. ICMT Inhibitor

    ICMT-IN-2 is a potent inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.168 μM. This compound effectively disrupts protein prenylation processes, making it a valuable tool for investigating the role of ICMT in various biological systems. ICMT-IN-2 has applications in studying signal transduction pathways and potential therapeutic interventions in diseases associated with aberrant protein modifications.
  12. ICMT Inhibitor

    ICMT-IN-14 is a selective inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.025 μM. This compound plays a critical role in the modulation of post-translational modifications of proteins associated with oncogenic signaling pathways. ICMT-IN-14 is ideal for research applications focused on protein methylation dynamics and the investigation of cancer biology.
  13. ICMT Inhibitor

    ICMT-IN-47 is a specific inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), with an IC50 value of 0.76 μM. This compound effectively disrupts ICMT activity, which is critical in the post-translational modification of proteins involved in various signaling pathways. ICMT-IN-47 can be utilized in research applications focused on cancer biology, signaling mechanisms, and studies targeting prenylated proteins.
  14. ICMT Inhibitor

    ICMT-IN-19 is a specific inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.026 μM. This compound effectively blocks ICMT activity, impacting post-translational modifications of proteins that can influence various cellular processes. ICMT-IN-19 is suitable for research applications focusing on protein processing, signal transduction, and cancer biology.
  15. ICMT Inhibitor

    ICMT-IN-22 is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.63 μM. This compound is instrumental in research applications related to lipid modification pathways, playing a crucial role in understanding post-translational modifications of proteins. Its use can facilitate studies on cellular signaling, protein stability, and the implications of ICMT activity in various diseases.
  16. ICMT Inhibitor

    ICMT-IN-49 is a potent inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), demonstrating an IC50 of 0.12 μM. This compound plays a critical role in modulating cellular processes by regulating protein methylation and is valuable in studies targeting protein function and signaling pathways. Research applications include investigations into cancer biology, neurodegenerative diseases, and other conditions where ICMT activity is implicated.
  17. ICMT Inhibitor

    ICMT-IN-42 is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.054 μM. This compound is valuable for research into the role of ICMT in post-translational modifications and protein function regulation. It is suitable for studies investigating cancer biology, signal transduction, and therapeutic development targeting ICMT pathways.
  18. ICMT Inhibitor

    ICMT-IN-9 is an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), with an IC50 of 0.16 μM. This compound selectively targets ICMT, playing a significant role in regulating post-translational modifications of proteins that are essential for various cellular processes. ICMT-IN-9 can be utilized in research applications focused on cancer biology, signal transduction, and the study of protein interactions influenced by methylation.
  19. ICMT Inhibitor

    ICMT-IN-3 is a potent inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT) with an IC50 value of 0.015 μM. This compound is crucial for studying protein modification processes, particularly in the context of signal transduction and cellular regulation. It serves as a valuable tool for investigating the role of ICMT in various biological pathways and its potential implications in disease mechanisms.
  20. ICMT Inhibitor

    ICMT-IN-4 is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), with an IC50 value of 0.27 μM. This compound plays a crucial role in the modulation of protein prenylation, impacting various cellular processes. It is valuable for research applications aimed at investigating the role of ICMT in signaling pathways and disease models related to cancer and other disorders.
  21. ICMT Inhibitor

    ICMT-IN-33 is a potent inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT) with an IC50 value of 0.46 μM. This compound effectively disrupts the post-translational modification of proteins by inhibiting ICMT activity. It is invaluable for research applications focused on elucidating the role of ICMT in cellular signaling and protein function, as well as potential therapeutic interventions targeting ICMT-related pathways.
  22. ICMT Inhibitor

    Farnesylcysteine (FC) is a competitive inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT). It has been shown to induce an abscisic acid (ABA) hypersensitive phenotype in Arabidopsis thaliana, highlighting its role in plant stress responses. This reagent is valuable for research applications focused on signaling pathways and mechanisms involving ICMT inhibition and ABA-related processes.
  23. ICMT Inhibitor

    ICMT-IN-55 is a selective inhibitor of isoprenylcysteine carboxymethyltransferase (ICMT) with an IC50 of 90 nM. This compound plays a crucial role in inhibiting ICMT activity, leading to the disruption of protein processing involved in various cellular signaling pathways. ICMT-IN-55 is utilized in research focused on understanding the biological significance of protein lipidation and its implications in cancer and other diseases.
  24. ICMT Inhibitor

    Spermatinamine is a natural inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT). This novel alkaloid, characterized by its bromotyrosyl-spermine-bromotyrosyl sequence, exhibits significant biological activity affecting protein prenylation. It is derived from the Australian sponge Pseudoceratina and is useful in research applications investigating the roles of ICMT and protein modification pathways in cellular processes.
  25. ICMT Inhibitor

    CAY10677 is a potent inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT), a critical enzyme involved in post-translational modifications of proteins. This compound has demonstrated significant ability to inhibit cancer cell proliferation, making it a valuable tool for cancer research. Additionally, CAY10677 exhibits favorable PAMPA permeability, enhancing its applicability in cellular assays.
  26. ICMT Inhibitor

    UCM-13207 is a selective inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT) with potential applications in aging research. This compound has been shown to mitigate progeria-like characteristics and enhance the survival rate in LmnaG609G/G609G mice, serving as an effective tool in studying cellular aging processes and related disorders. Researchers can utilize UCM-13207 to explore therapeutic strategies for age-related diseases.
  27. ICMT Inhibitor

    J1-1 is an inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), with an IC50 of 1.0 μM. This compound demonstrates notable anticancer activity, making it a valuable tool for research into cancer biology. J1-1 can be utilized in studies focusing on protein modification and its implications in oncogenic signaling pathways.
  28. LTD4/PAF Antagonist

    CP-96021 hydrochloride is a potent and orally active antagonist of the leukotriene D4 (LTD4) and platelet activating factor (PAF) receptors, exhibiting Ki values of 34 nM and 37 nM, respectively. This compound demonstrates significant biological activity by blocking LTD4 and PAF signaling pathways, which are implicated in various inflammatory conditions. CP-96021 hydrochloride serves as a valuable tool for research into respiratory diseases, allergies, and other disorders mediated by these signaling molecules.
  29. S1PR Agonist

    Sphingosine-1-phosphate (S1P) functions as an agonist of S1P1-5 receptors and acts as a ligand for GPR3, GPR6, and GPR12. It serves as an intracellular second messenger, promoting calcium mobilization and influencing various cellular processes. As a key lipid mediator derived from sphingomyelin and other membrane phospholipids, Sphingosine-1-phosphate plays a crucial role in stimulating DNA synthesis, cell proliferation, and migration, making it valuable for studies in cell signaling and cell biology research.
  30. S1P1,5 Agonist

    (S)-PF-462991 is a selective agonist of the S1P1 and S1P5 receptors. It exhibits key biological activity by modulating sphingosine 1-phosphate signaling pathways, which are crucial for immune cell trafficking and vascular integrity. This compound is primarily utilized in research to investigate its effects on inflammation, neuroprotection, and cardiovascular health.
  31. LPA2 Agonist

    Decyl phosphate is a selective agonist of the LPA2 receptor, exhibiting an EC50 value of 1.8 μM. Additionally, it acts as an antagonist for the LPA1 and LPA3 receptors. This compound is valuable for research applications focused on blood disorders and the modulation of lysophosphatidic acid signaling pathways.
  32. LPA Receptors Activator

    1-Oleoyl lysophosphatidic acid is a potent activator of lysophosphatidic acid (LPA) receptors, exhibiting strong biological activity due to its high affinity for these receptors. This compound is frequently utilized in research to investigate LPA receptor signaling pathways and related cellular responses. Additionally, 1-Oleoyl lysophosphatidic acid has been shown to enhance SRE-driven β-galactosidase activity, making it a valuable tool in studies of gene expression and cellular signaling.
  33. LPA1 Antagonist

    BMS-986278 is a potent, orally active antagonist of the lysophosphatidic acid receptor 1 (LPA1), exhibiting inhibition constants (Kbs) of 6.9 nM for human LPA1 and 4.0 nM for mouse LPA1. This compound is particularly useful for investigating pulmonary fibrotic disorders and exploring therapeutic strategies targeting LPA1 signaling pathways. Its selective activity makes it a valuable tool for elucidating the role of LPA1 in fibrotic disease mechanisms.
  34. S1P1 Receptor Antagonist

    Etrasimod is a potent and selective antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor, demonstrating an IC50 value of 1.88 nM in CHO cells. This orally bioavailable compound is primarily utilized in research focused on autoimmune diseases and cardiovascular conditions, where modulation of S1P signaling plays a crucial role in cell trafficking and inflammation. Its specificity makes it a valuable tool for exploring the therapeutic potential of S1P1 receptor inhibition.
  35. S1PR2 Agonist

    CYM-5520 is a selective allosteric agonist of the sphingosine 1-phosphate receptor 2 (S1PR2), exhibiting an EC50 of 480 nM. It specifically activates S1PR2 without influencing S1PR1, S1PR3, S1PR4, and S1PR5. CYM-5520’s unique mechanism allows for co-binding with sphingosine 1-phosphate (S1P) at the S1PR2 site. This compound is valuable for research applications related to osteoporosis and the modulation of related signaling pathways.
  36. S1P1 Agonist

    SAR247799 is a selective S1P1 agonist that acts through G-protein-biased signaling. It exhibits oral bioactivity with EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells and human umbilical vein endothelial cells (HUVECs). This compound is valuable for research into endothelial protection mechanisms, particularly in the context of type 2 diabetes and metabolic syndrome.
  37. S1P Receptor Agonist

    Fingolimod phosphate is an orally active sphingosine 1-phosphate (S1P) receptor agonist. This compound is known to enhance the neuroprotective activities of microglia, making it a valuable tool in the study of neuroinflammation. Fingolimod phosphate is primarily used in research related to multiple sclerosis and other neurological disorders.
  38. S1P3 Antagonist

    CAY10444 is an antagonist of the sphingosine-1-phosphate receptor 3 (S1P3). This compound effectively inhibits S1P-induced calcium ion (Ca2+) increases by 37% in HeLa cells that express S1P3 receptors. It serves as a valuable tool for research into S1P3-related signaling pathways and their implications in various physiological and pathological processes.
  39. S1PR4 Antagonist

    CYM50358 is a potent and selective antagonist of the sphingosine-1-phosphate receptor 4 (S1PR4), exhibiting an IC50 of 25 nM. This compound serves as a valuable tool for investigating the role of S1PR4 in various biological processes, including its implications in influenza infection research. Its selective inhibition of S1PR4 allows for detailed mechanistic studies and potential therapeutic applications in related inflammatory diseases.
  40. S1P2 Antagonist

    GLPG2938 is a potent and selective antagonist of the sphingosine-1-phosphate receptor 2 (S1P2). This compound demonstrates significant efficacy in inhibiting S1P2-mediated signaling pathways, making it a valuable tool for investigating mechanisms underlying idiopathic pulmonary fibrosis. Researchers can utilize GLPG2938 to explore its therapeutic potential and role in fibrotic disease models.
  41. LPA1 Antagonist

    H2L 5765834 is a potent antagonist of lysophosphatidic acid receptors LPA1, LPA3, and LPA5, exhibiting IC50 values of 94 nM, 752 nM, and 463 nM, respectively. This compound is valuable for studies investigating the role of LPA receptors in various biological processes, including cell proliferation, migration, and survival. Its ability to selectively inhibit these receptors makes it a useful tool for research in cancer biology, fibrosis, and neurobiology.
  42. S1PR1 Modulator

    Amiselimod hydrochloride is a selective sphingosine 1-phosphate receptor-1 (S1P1) modulator that is converted in vivo to its active metabolite, amiselimod phosphate. It is orally active and designed to minimize bradycardia effects commonly seen with other S1P receptor modulators. Key biological activities include the inhibition of chronic colitis through the reduction of Th1 and Th17 cell infiltration into the colon, as well as the suppression of autoreactive T cell infiltration in lupus nephritis. Amiselimod hydrochloride is of considerable interest for research in autoimmune diseases.
  43. S1P2 Agonist

    CYM-5478 is a potent and highly selective sphingosine-1-phosphate receptor 2 (S1P2) agonist, demonstrating an EC50 of 119 nM in TGFα shedding assays. This compound exhibits significant protective effects on neural-derived cell lines against Cisplatin-induced toxicity. Its applications include investigating the role of S1P2 in neural cell protection and exploring potential therapeutic strategies for mitigating chemotherapy-induced neurotoxicity.
  44. S1P Receptor Modulator

    Ozanimod hydrochloride, an S1P receptor modulator, selectively binds to sphingosine 1-phosphate receptor subtypes 1 (S1P1) and 5 (S1P5) with high affinity, exhibiting EC50 values of 1.03 nM and 8.6 nM, respectively. This compound demonstrates immunomodulatory effects, making it relevant for investigating mechanisms of action in relapsing multiple sclerosis (MS). Ozanimod hydrochloride serves as a valuable tool for research focused on S1P receptor signaling pathways and their implications in autoimmune disorders.
  45. LPA1 Agonist

    ONO-0740556 is a potent agonist of the Gi-coupled human lysophosphatidic acid receptor 1 (LPA1), exhibiting an EC50 value of 0.26 nM. This compound plays a significant role in modulating cellular signaling pathways associated with LPA1 activation. ONO-0740556 is valuable for research applications focused on investigating LPA1-related physiological and pathological processes, including cell proliferation, migration, and inflammatory responses.
  46. S1P Lyase Inhibitor

    2-Acetyl-4-tetrahydroxybutyl imidazole is a potent inhibitor of sphingosine-1-phosphate (S1P) lyase, demonstrating significant biological activity in vivo. This compound is useful for investigating the role of S1P metabolism in various physiological and pathological processes. Research applications include studying cell signaling pathways and exploring therapeutic targets in diseases related to S1P dysregulation.
  47. LPA5/GPR92 Antagonist

    TC LPA5 4 is a selective antagonist of LPA5 (GPR92) with a non-lipid structure. It effectively inhibits LPA-induced aggregation of isolated human platelets, demonstrating an IC50 value of 800 nM. Additionally, TC LPA5 4 shows potent inhibition of cell proliferation and migration in thyroid cancer cells, making it a valuable tool for research in cancer biology and cell signaling pathways associated with LPA5.
  48. LPA1 Antagonist

    ONO-9780307 is a potent antagonist of the LPA1 (lysophosphatidic acid receptor 1) with an IC50 value of 2.7 nM. This compound effectively inhibits LPA1-mediated signaling pathways, making it a valuable tool for studying the role of lysophosphatidic acid in various biological processes. It is suitable for research applications involving cellular signaling, inflammation, and cancer biology.
  49. S1PR1 Agonist

    RP101988 is a potent and selective agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 of 0.19 nM for S1PR1. Additionally, it demonstrates moderate activity at S1PR5 with an EC50 of 32.8 nM. This compound is valuable for research into immune modulation and inflammation pathways, making it a useful tool for studying S1PR1-related physiological processes and potential therapeutic applications.
  50. LPA1 NAM

    TAK-615 is a negative allosteric modulator (NAM) of the lysophosphatidic acid receptor 1 (LPA1). It exhibits high-affinity binding with a Kd of 1.7 nM, along with a lower affinity of 14.5 nM. This compound is primarily used in research focused on pulmonary fibrosis, enabling investigations into the role of LPA1 in fibrotic pathways and potential therapeutic interventions.

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