Ras

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  1. Rac family GTPase inhibitor

    EHT 1864 is an antiproliferative chemical shown to inhibit Rac family GTPases.
  2. Cdc42 GTPase inhibitor

    CASIN is a novel and potent Cdc42 inhibitor.
  3. PPMTase inhibitor

    Salirasib is an inhibitor of prenylated protein methyltransferase (PPMTase) with Ki value of 2.6 uM.
  4. Cdc42 GTPase inhibitor

    ZCL-278 is a selective inhibitor of Cdc42. Targets the binding site of the Cdc42 guanine nucleotide exchange factor, intersectin (ITSN). Inhibits Cdc42-mediated cellular effects, including microspike formation in 3T3 fibroblasts and neuronal branching in primary neonatal cortical neurons. Also suppresses cell motility and migration in PC3 cells, without cytotoxic effects.
  5. PDE-KRAS inhibitor

    Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling.
  6. Rac GTPase inhibitor

    NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 uM).
  7. K-Ras(G12C) inhibitor

    K-Ras(G12C) inhibitor 6 is an irreversible inhibitor of oncogenic K-Ras(G12C), subverting the native nucleotide preference to favour GDP over GTP.
  8. K-Ras(G12C) inhibitor

    K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).
  9. K-Ras inhibitor

    6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).
  10. K-Ras(G12C) inhibitor

    K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
  11. Rho inhibitor

    CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription.
  12. mutant K-ras G12C inhibitor

    ARS-1323 is a novel inhibitor of mutant K-ras G12C.
  13. mutant K-ras G12C inhibitor

    ARS-1630 is a novel inhibitor of mutant K-ras G12C.
  14. Ras inhibitor

    Antineoplaston A 10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.
  15. pan-RAS inhibitor

    Ras-IN-3144 is a pan-RAS inhibitor which inhibits RAS signaling pathways in cancer cells and prevents the growth of RAS mutant mouse cancer xenografts.
  16. KRAS-G12C inhibitor

    MRTX1257 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, MRTX1257 inhibited KRAS dependent ERKphosphorylation in the H358cell assay with an IC50= 900 pM.
  17. SOS1 inhibitor

    BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction with IC50 of 21 nM.
  18. ATP-competitive STK19 inhibitor

    ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor. ZT-12-037-01 effectively blocks oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vitro and in vivo.
  19. KRAS G12C inhibitor

    KRAS G12C inhibitor 17 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 82, has an IC50 of 5 nM.
  20. KRAS G12C inhibitor

    KRAS G12C inhibitor 16 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 39, has an IC50 of 97 nM.
  21. KRAS G12C inhibitor

    KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 nM.
  22. Cnk1 inhibitor

    PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain, which inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling.
  23. Rab7 activator

    ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM).
  24. Ras-Net inhibitor

    XRP44X is a Ras-Net (Elk-3) pathway inhibitor (IC50 = 10-20 nM). Indirectly inhibits Net phosphorylation upstream of Erk1/2 activation.
  25. K-Ras inhibitor

    6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  26. KSR/Ras inhibitor

    APS-2-79 HCl, small molecule that stabilizes the KSR (Kinase suppressor of Ras) inactive state and antagonizes oncogenic Ras signalling (IC50 value 120 nM against ATP-biotin probe-labelling of KSR2).
  27. KSR/Ras inhibitor

    APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.
  28. KRAS G12C inhibitor

    Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity.

  29. GGTase I inhibitor

    GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.
  30. Ral GTPase inhibitor

    RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
  31. Dual inhibitor of Rac and Cdc42

    MBQ-167 is a potent and dual inhibitor of Rac and Cdc42 with IC50s of 103 nM and 78 nM respectively, in metastatic breast cancer cells.
  32. KRAS-G12C inhibitor

    ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRAS-G12C) and could achieve rapid and sustained in vivo target occupancy to induce tumor regression.
  33. MRCK inhibitor

    BDP9066 is a potent and selective MRCK inhibitor, reducing substrate phosphorylation.
  34. SRE activation inhibitor

    CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM.
  35. Rac1 inhibitor

    1A-116 is a specific Rac1 inhibitor, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo.

  36. ROCK and MRCK inhibitor

    BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
  37. K-Ras inhibitor

    K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.(the detailed information refer to the reference).
  38. K-ras G12C inhibitor

    K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
  39. covalent K-Ras G12C inhibitor

    K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
  40. K-ras G12C inhibitor

    K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
  41. exchange protein inhibitor

    (R)-CE3F4 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC50 of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC50, 44 μM).
  42. RhoA subfamily Rho GTPases inhibitor

    Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis.
  43. Epac inhibitor

    EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC50 of 4 ?M in Swiss 3T3 cells.
  44. Epac1 antagonist

    CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
  45. Wnt/beta-catenin modulator

    KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
  46. GGTase I inhibitor

    GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
  47. KRAS G12C covalent inhibitor

    AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
  48. KRas G12C inhibitor

    KRAS G12C inhibitor 5 is a KRas G12C inhibitor extracted from patent WO2017201161A1, Compound example 147.
  49. KRAS G12C covalent inhibitor

    AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
  50. KRAS G12C inhibitor

    KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30.

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