Ras

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  1. KRAS Inhibitor

    KRAS inhibitor-32 targets the KRAS protein, a critical component in many oncogenic signaling pathways. This compound exhibits selective inhibition of KRAS, making it a valuable tool for cancer research, particularly in the study of tumor growth and progression in KRAS-driven malignancies. Its application in preclinical studies can aid in understanding the therapeutic potential of KRAS inhibition in various cancer types.
  2. Anti-cancer Agent

    KRAS G12C inhibitor 41 is a selective inhibitor targeting the KRAS G12C mutant protein, a critical player in oncogenic signaling pathways. This compound demonstrates significant anti-cancer activity, making it a valuable tool for investigating KRAS G12C-mediated malignancies. Its application in research can facilitate the development of targeted therapies aimed at overcoming resistance mechanisms in cancer treatment.
  3. KRAS G12C Inhibitor

    KRAS G12C inhibitor 53 is a selective inhibitor targeting the G12C mutated form of the KRAS protein. This compound demonstrates potent anti-proliferative activity in KRAS G12C-driven cancer cell lines, making it a valuable tool in oncology research. It is applicable for studies focused on signaling pathways involved in tumorigenesis and the development of targeted therapies for KRAS G12C mutations.
  4. KRAS G12C Inhibitor

    KRAS G12C Inhibitor 33 selectively targets the KRAS G12C mutant, inhibiting its activity. This compound is essential for investigating the mechanisms of KRAS-driven cancers and contributes to the development of targeted therapies. It is a valuable tool for cancer research, particularly in studies focused on signaling pathways associated with KRAS mutations.
  5. KRAS Inhibitor

    ZINC57632462 (ACA-6) is a non-covalent allosteric inhibitor targeting KRAS. It effectively disrupts nucleotide exchange and impairs RAS-effector interaction, making it a valuable tool for investigating KRAS-related signaling pathways. This compound is particularly relevant for cancer research, enabling studies focused on tumorigenesis and therapeutic interventions.
  6. K-Ras Inhibitor

    (±)-Spiro-oxanthromicin A is a K-Ras inhibitor with an IC50 value of 26.7 μM. This polyketide compound is derived from soil-isolated Streptomyces sp. and has been shown to mislocalize oncogenic mutant K-Ras from the plasma membrane in intact MDCK cells. (±)-Spiro-oxanthromicin A serves as a valuable tool for cancer research, particularly in studies targeting K-Ras-related pathways.
  7. K-Ras Inhibitor

    KS-58 is a K-Ras (G12D) inhibitory peptide that selectively targets and binds to K-Ras. It effectively enters cells to disrupt intracellular interactions between Ras and effector proteins. This compound demonstrates significant antitumor activity by inhibiting the proliferation of tumor cells, making it a valuable tool for research on K-Ras-related cancers and therapeutic interventions.
  8. KRAS Inhibitor

    KRAS-IN-5 is a selective inhibitor targeting KRAS mutants, including KRASG12D and KRASG12V, with a GNE IC50 value of 1.3 nM against KRASG12D. This compound inhibits KRAS-mediated signaling pathways, effectively blocking tumor cell proliferation by reducing ERK phosphorylation. KRAS-IN-5 exhibits potential for research applications in KRAS mutation-related cancers, including pancreatic, colorectal, and lung cancer.
  9. KRAS G12C inhibitor

    KRAS G12C inhibitor 20 is a selective inhibitor targeting the KRAS G12C mutation. This compound exhibits significant anticancer activity by disrupting KRAS signaling pathways, thereby inhibiting cellular proliferation in KRAS-dependent tumors. It is applicable in research focused on cancer biology and targeted therapies for malignancies associated with the KRAS G12C mutation.
  10. KRAS G12V Inhibitor

    KRAS inhibitor-26 is a potent inhibitor targeting the KRAS G12V mutation, exhibiting an IC50 of ≤100 nM. This compound effectively disrupts oncogenic signaling pathways associated with KRAS, making it a valuable tool for cancer research. Its applications include studies on tumor growth, survival, and potential therapeutic interventions in KRAS-driven malignancies.
  11. Lbc-RhoA Interaction Inhibitor

    ZINC09659342 is an inhibitor of the Lbc-RhoA interaction, exhibiting an IC50 value of 3.6 μM. This compound serves as a valuable tool for studying RhoA-mediated cellular processes and signaling pathways. Its ability to disrupt Lbc-RhoA interactions makes it suitable for research applications in cancer biology and cellular mechanism studies.
  12. KRAS Inhibitor

    KRAS Inhibitor-25 is a pyridopyrimidine compound that selectively inhibits KRAS with an IC50 of less than 100 nM for KRas G12V, KRas wild type (WT), and KRas G12R variants. This inhibitor is valuable for research applications focused on understanding KRAS-driven oncogenic signaling pathways and developing targeted cancer therapies. Its potency makes it suitable for studies investigating the biological effects of KRAS mutations and their role in tumorigenesis.
  13. KRAS-LZTR1 Interaction Modulator

    LZTR1-KRAS modulator 1 is designed to modulate the interaction between KRAS and LZTR1, thereby enhancing the recruitment of the LZTR1-KRAS complex. This compound is crucial for studies investigating the regulation of KRAS signaling pathways and their implications in cellular processes. Its application can further elucidate the role of LZTR1 in cancer biology and potential therapeutic interventions targeting KRAS-driven tumors.
  14. Epac Agonist

    8-pHPT-2'-O-Me-cAMP is a cAMP analog that acts as an Epac agonist, specifically enhancing the activity of the exchange protein activated by cyclic AMP (Epac). This compound is utilized in cardiac research to explore signaling mechanisms and cellular responses associated with cardiac function and pathophysiology. Its ability to modulate Epac pathways makes it a valuable tool for investigating the roles of cAMP in cardiac health and disease.
  15. GGTase-I Inhibitor

    GGTI-297 is an inhibitor of geranylgeranyl transferase I (GGTase-1), exhibiting IC50 values of 56 nM for GGTase-1 and 203 nM for farnesyl transferase (FTase). This compound specifically inhibits the geranylgeranylation of the protein Rap1A, effectively disrupting its processing while leaving the farnesylated protein H-Ras unaffected. GGTI-297 is valuable for research applications focused on protein prenylation and its implications in cellular signaling pathways.
  16. KRAS G12C Inhibitor

    KRAS G12C Inhibitor 62 is designed to selectively inhibit the KRAS G12C mutant protein. This compound demonstrates potential in the study of KRAS G12C-mediated cancers, offering valuable insights into therapeutic strategies targeting this challenging oncogenic driver. Its application may facilitate research into tumor growth inhibition and the underlying mechanisms of KRAS-related malignancies.
  17. RasGRP3 Ligand

    RasGRP3 ligand 1 is a specific ligand for RasGRP3 with a binding affinity characterized by a Ki of 1.75 nM. This compound effectively induces Ras activation, making it a valuable tool for investigating downstream signaling pathways in cancer research. Its targeted mechanism allows for detailed studies of RasGRP3's role in cellular processes associated with tumorigenesis.
  18. Z52/Z56 intermediate

    Z52/Z56 intermediate is a crucial building block in the synthesis of RAS inhibitors. This compound plays an important role in facilitating research on the modulation of RAS signaling pathways, which are critical in cancer biology. Its use in the development of RAS-targeted therapeutics makes it valuable for studies focused on oncogenic signaling and drug discovery efforts in oncology.
  19. L-731735 Prodrug

    L 731734 is a prodrug of L-731735, designed to inhibit Ras processing in v-ras-transformed cells. This compound plays a critical role in the study of cell signaling and oncogenic processes associated with Ras. Its application in research provides valuable insights into targeted cancer therapies and the manipulation of Ras signaling pathways.
  20. Farnesyltransferase Inhibitor

    L-739749 is a potent farnesyltransferase inhibitor that selectively inhibits the prenylation of Ras proteins. This compound has demonstrated significant efficacy in blocking the hypersensitivity of juvenile myelomonocytic leukaemia (JMML) cells to granulocyte-macrophage colony-stimulating factor (GM-CSF). In vitro studies show that L-739749 effectively reduces the growth of primary human JMML cells, making it a valuable tool for research into targeted therapies for this disease.
  21. K-Ras Localization Modulator

    (+)-Oxanthromicin is a K-Ras localization modulator that disrupts the localization of oncogenic mutant K-Ras from the plasma membrane in intact Madin-Darby canine kidney (MDCK) cells. This compound demonstrates significant antitumor efficacy, making it valuable for research into cancer biology and potential therapeutic strategies targeting K-Ras-mediated signaling pathways. Its ability to alter K-Ras localization positions it as a promising candidate in the development of targeted cancer therapies.
  22. RhoA Inhibitor

    Dykellic acid is a potent inhibitor of RhoA, a small GTPase involved in regulating cell migration and cytoskeletal dynamics. This compound demonstrates significant inhibitory effects on the migration and motility of B16 melanoma cells, as well as on the tube formation capacity of human umbilical vein endothelial cells (HUVECs). Dykellic acid holds promise for applications in cancer research, particularly related to metastatic processes and tumor microenvironment interactions.
  23. K-Ras Ligand

    SML-10-70-1 is a K-Ras ligand that covalently modifies the K-Ras G12C mutant protein, providing a targeted approach in cancer research. This compound effectively inhibits the phosphorylation of ERK and Akt, key signaling pathways involved in cell proliferation. In vitro studies demonstrate that SML-10-70-1 significantly reduces the proliferation of cancer cell lines H23, H358, and A549, with IC50 values ranging from 26.6 to 47.6 μM, indicating its potential utility in therapeutic applications against K-Ras-driven malignancies.
  24. Ligand for Target Protein for PROTAC

    pan-KRAS ligand 1 is a potent ligand designed for Target Protein applications within PROTAC technology. It facilitates the development of PROTAC pan-KRAS degrader 4, enabling targeted degradation of KRAS mutants. This compound is instrumental for researchers investigating KRAS-related oncogenic pathways and therapeutic strategies against cancer.
  25. EPAC Activator

    Sp-8-Br-2'-O-Me-cAMPS is a cAMP analog that serves as a potent activator of the exchange protein directly activated by cyclic AMP (EPAC). This compound is valuable for studying the role of EPAC in various biological pathways, particularly those related to metabolism. Its ability to modulate EPAC activity makes it an important tool for investigating signaling mechanisms and their implications in metabolic processes.
  26. Azathioprine Metabolite

    6-T-GDP (6-Thioguanosine 5'-diphosphate) operates as a metabolite of azathioprine, targeted for its role in modulating inflammatory responses. By inhibiting Rac1 activity, 6-T-GDP reduces the transcription of inflammatory factors and decreases the expression of cell adhesion molecules. This action subsequently inhibits leukocyte migration and the onset of tissue inflammation, making it a valuable reagent for research into inflammatory diseases and mechanisms of immune regulation.
  27. cAMP Analogue

    2'-O-Me-cAMP is a cAMP analogue that selectively stimulates exchange proteins activated by cAMP (Epac). This compound serves as a valuable tool for studying cAMP-mediated signaling pathways and the role of Epac in various biological processes. Its low membrane permeability can provide insights into the mechanisms of cAMP action in cellular contexts.
  28. Ras Activation Inhibitor

    SCH-53870 is a Ras activation inhibitor that specifically binds to the Ras-GDP complex, thereby maintaining Ras in an inactive GDP-bound state and inhibiting its activation to the GTP-bound form. This compound modulates cell signaling pathways and subsequently affects cell proliferation by obstructing Ras activation. SCH-53870 is applicable in cancer research, providing a valuable tool for studying Ras-related oncogenic mechanisms.
  29. EPAC Antagonist

    NY-0173 is an antagonist of exchange proteins directly activated by cAMP (EPAC), demonstrating IC50 values of 3.5 μM for EPAC2 and 4.0 μM for EPAC1. This reagent serves as a valuable tool for investigating the biological roles and pathways mediated by EPAC. Researchers can utilize NY-0173 to explore its impact on cellular processes influenced by EPAC signaling.
  30. CDC42/RHOJ Inhibitor

    ARN25062 is a potent inhibitor targeting CDC42 and RHOJ, demonstrating significant antitumor activity. This novel trisubstituted pyrimidine derivative is suitable for research applications investigating the modulation of cell signaling pathways involved in cancer progression and metastasis. Its specific inhibition of CDC42 and RHOJ makes it a valuable tool for studying cellular processes related to tumorigenesis.
  31. Ra Activator

    Goralatide is a Ra activator that modulates the thermal sensitivity of hematopoietic progenitor cells. It enhances the disparity in thermal sensitivity between leukemia progenitor cells and normal hematopoietic progenitor cells, thereby increasing the efficacy of hyperthermia therapy. This compound is relevant for research in cancer treatment strategies, particularly those involving targeted thermal therapies.
  32. EPAC Activator

    Sp-8-pCPT-2'-O-Me-cAMPS is a selective activator of the exchange protein directly activated by cyclic AMP (EPAC). This compound enhances EPAC-mediated signaling pathways, playing a significant role in the regulation of various physiological processes. It is valuable for research into endocrine metabolism and related signaling mechanisms.
  33. pan-KRAS Inhibitor

    Eras-4001 is a pan-KRAS inhibitor that demonstrates significant antitumor activity by effectively inhibiting the proliferation of both wild-type and mutant KRAS cancer cells, including variants such as KRASG12D, KRASG12V, and KRASG12C. In preclinical studies, Eras-4001 has evidenced a robust ability to suppress tumor growth in xenograft mouse models, such as GP2D and Panc0403, making it a valuable tool for investigating KRAS-driven malignancies and potential therapeutic strategies in cancer research.
  34. KRAS Agonist

    KRA-533 is a potent KRAS agonist that selectively binds to the GTP/GDP binding pocket of the KRAS protein. This interaction inhibits GTP cleavage, leading to the accumulation of constitutively active GTP-bound KRAS. Consequently, KRA-533 induces both apoptotic and autophagic cell death pathways in cancer cells, making it a valuable tool for research into cancer biology and therapeutic strategies targeting KRAS signaling.
  35. Cdc42 Inhibitor

    CID44216842 is a selective inhibitor of the small GTPase Cdc42, acting primarily by disrupting its guanine nucleotide binding. It demonstrates potent inhibitory activity with EC50 values of 1.0 μM and 1.2 μM for wild-type Cdc42 and the Cdc42Q61L mutant, respectively, in GTP binding assays, and 0.3 μM and 0.5 μM in GDP binding assays. This compound is suitable for use as a molecular probe in studies related to Cdc42 signaling pathways and its role in cellular processes such as cytoskeletal dynamics and cell migration.
  36. KRAS G12D Inhibitor

    AZD0022 is a selective and orally active inhibitor of the KRAS G12D mutant protein. It effectively disrupts the KRAS signaling pathway, demonstrating suppression of tumor growth in the GP2D xenograft model. This compound is relevant for research in cancer therapeutics, particularly for investigating KRAS-driven malignancies.
  37. KRAS Inhibitor

    KRAS inhibitor-3 is a selective inhibitor of the KRAS protein, effectively targeting both wild-type and various oncogenic mutants, including KRAS G12C, G12D, and Q61H, with affinities ranging from 0.28 μM to 0.74 μM. This compound disrupts the interaction between KRAS and Raf, thereby influencing downstream signaling pathways critical for cell proliferation and survival. KRAS inhibitor-3 is a valuable tool for research applications focused on cancer biology and the development of targeted therapies for KRAS-driven malignancies.
  38. Cdc42/Rac1 Inhibitor

    l-Naproxen is an enantiomer of (S)-Naproxen, functioning as an inhibitor of Cdc42 and Rac1 with EC50 values of 96 μM and 212 μM, respectively. It exhibits anti-tumor activity in addition to its role as a nonsteroidal anti-inflammatory drug (NSAID). This compound is valuable for research applications involving cellular signaling pathways, inflammation, and cancer biology.
  39. KRasG12C Inhibitor

    CFL-137 is a potent inhibitor of KRasG12C, a pivotal mutation implicated in various cancers. This compound demonstrates significant antiproliferative activity, making it a valuable tool for studying oncogenic signaling pathways. CFL-137 holds promise for research applications focused on lung cancer and other KRas-driven malignancies.
  40. KRAS Inhibitor

    KRAS Inhibitor-10 is a selective inhibitor targeting RAS proteins, with a strong emphasis on KRAS variants. This orally active compound demonstrates significant anti-cancer activity, making it suitable for research applications in various malignancies, including pancreatic cancer, breast cancer, multiple myeloma, leukemia, and lung cancer. KRAS Inhibitor-10 is derived from a tetrahydroisoquinoline structure and is detailed in patent WO2021005165 A1.
  41. KRASG12D Mutant Inhibitor

    KRAS G12D-IN-29 is a selective inhibitor targeting the KRAS G12D mutant, known for its oral bioavailability. This compound effectively disrupts downstream signaling pathways associated with KRAS G12D, leading to a reduction in tumor cell proliferation. KRAS G12D-IN-29 shows potential for research applications focused on cancers driven by the KRAS G12D mutation, including pancreatic, lung, and colorectal cancers.
  42. KRAS Inhibitor

    KRAS Inhibitor-31 is a potent inhibitor targeting mutant forms of the KRAS protein, specifically KRAS G12D, G12C, and G12V, with KD (SPR) values of 0.019 nM, 0.019 nM, and 0.096 nM, respectively. This compound demonstrates significant biological activity in the inhibition of KRAS-driven signaling pathways, making it a valuable tool for research in cancer biology, particularly in the study of tumors harboring KRAS mutations.
  43. pan-KRAS Inhibitor

    pan-KRAS-IN-2 is a potent pan-KRAS inhibitor with IC50 values of ≤ 10 nM against both wild-type and prevalent mutant forms of KRAS, including G12D, G12C, G12V, G12S, G12A, and Q61H, while exhibiting an IC50 > 10 μM for KRAS G13D. This compound is valuable for investigating KRAS-mediated cancers, specifically in pancreatic and colorectal cancer models, aiding in the understanding of tumor biology and potential therapeutic interventions.
  44. EPAC1 Agonist

    I942 is a selective non-cyclic nucleotide (NCN) agonist of EPAC1. It effectively modulates proinflammatory cytokine signaling pathways associated with various cardiovascular diseases. This compound serves as a valuable tool in research focused on understanding EPAC1-related mechanisms and developing therapeutic strategies for inflammatory cardiovascular conditions.
  45. Isomer

    (R)-BI-2852 is the isomer of BI-2852, designed as an experimental control in KRAS research. It functions as a KRAS inhibitor targeting the switch I/II pocket with nanomolar affinity, displaying a ten-fold stronger binding to active KRASG12D compared to KRAS wild type. This compound effectively disrupts guanine nucleotide exchange factor, GTPase-activating protein, and effector interactions with KRAS, resulting in the inhibition of downstream signaling pathways and an antiproliferative effect in KRAS mutant cell lines.
  46. Rac1 Inhibitor

    Rac1-IN-3 is an inhibitor of the Rac1 protein, exhibiting an IC50 of 46.1 μM. This compound effectively disrupts Rac1 signaling pathways, which are implicated in various cellular functions such as cytoskeletal dynamics and cell migration. Rac1-IN-3 is valuable for research applications focused on cancer biology, neurodegenerative diseases, and cardiovascular disorders, providing insights into the role of Rac1 in disease progression and therapeutic targeting.
  47. pan-KRAS Inhibitor

    pan-KRAS-IN-18 is a pan-KRAS inhibitor targeting both KRAS wild-type and KRAS G12V, with IC50 values of 29 nM and 9 nM, respectively. This compound demonstrates significant antiproliferative activity in KRAS-mutant cell lines, making it a valuable tool for researchers studying KRAS-driven cancers. Its application is particularly relevant in the context of lung cancer research.
  48. KRAS G12C Inhibitor

    Divarasib adipate is a potent and selective inhibitor of KRAS G12C with an IC50 of <0.01 μM. By covalently binding to the switch II pocket of KRAS G12C, Divarasib irreversibly stabilizes the protein in its inactive GDP-bound state. This compound is primarily utilized in research applications focused on cancer biology, particularly in studies targeting KRAS-driven tumors.
  49. KRAS(G12D) Inhibitor

    MRTX-EX185 formic is a potent inhibitor of KRAS(G12D) with an IC50 of 90 nM. It effectively binds to both GDP-loaded and active GTP-bound states of KRAS, displaying broad-spectrum activity with additional IC50 values of 110, 290, 130, and 240 nM for KRAS WT, KRAS(G12C), KRAS(Q61H), and KRAS(G13D), respectively. MRTX-EX185 formic also shows affinity for GDP-loaded HRAS. This compound is valuable for investigating RAS-driven tumors, including pancreatic cancer, facilitating insights into therapeutic strategies targeting KRAS mutations.
  50. Pan-RAS Inhibitor

    Pan-RAS-IN-3 is a pan-RAS inhibitor that targets various isoforms of the RAS protein family, known for their role in promoting cellular proliferation and survival. This compound exhibits significant biological activity in inhibiting the signaling pathways associated with melanoma and acute myeloid leukemia. It is a valuable tool for researchers investigating RAS-driven cancers and studying the therapeutic potential of targeting these oncogenic signaling pathways.

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