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- Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
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osteoclastic bone resorption inhibitor
Zoledronic acid is a bisphosphonate which used to multiple myeloma and prostate cancer treament. -
Cdc42 GTPase inhibitor
CASIN is a novel and potent Cdc42 inhibitor.- Yongru Xu, .et al. , Int J Mol Sci, 2017, Mar; 18(3): 586 PMID: 28282856
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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. -
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). -
K-Ras(G12C) inhibitor
K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). -
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). -
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. -
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. -
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. -
KRAS G12C covalent inhibitor
AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity. -
KRAS G12C covalent inhibitor
AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity. -
pan GTPase inhibitor
CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
