Cart
sales@molnova.com
Rho
The Rho GTPase family forms part of the Ras superfamily and consists, in humans, of 20 members, which can be classified into eight subgroups. Rho GTPases are best known for their roles in regulating cytoskeletal rearrangements, cell motility, cell polarity, axon guidance, vesicle trafficking and the cell cycle. Alterations in Rho GTPase signalling contribute to malignant transformation, neurological abnormalities and immunological diseases. Most Rho GTPases cycle between an active GTP bound conformation and an inactive GDP-bound conformation. This cycling is regulated by three types of protein, Guanine nucleotide exchange factors (GEFs) catalyse the exchange of GDP for GTP, thereby activating the GTPase4, whereas GTPase-activating proteins (GAPs) increase the intrinsic GTP hydrolysis rate of the GTPase, thereby inactivating it. Guanine nucleotide dissociation inhibitors (GDIs) sequester the GDP-bound form of some GTPases in the cytosol and prevent them from localizing to membranes or being activated by GEFs. Rho GTPases are rapidly activated by various cell-surface receptors, including integrins, cadherins, cytokine receptors, Tyr kinase receptors and G protein-coupled receptors.
References
1.Hodge RG, et al. Nat Rev Mol Cell Biol. 2016;17(8):496–510.
References
1.Hodge RG, et al. Nat Rev Mol Cell Biol. 2016;17(8):496–510.
Cell Cycle/DNA Damage
ABC(12)
AChR(104)
Antifolate(12)
ATM/ATR(26)
Aurora Kinase(51)
CLK(15)
c-Myc(22)
DHFR(16)
DNA Alkylator(34)
DNA gyrase(11)
DNA Repair Protein(21)
DNA/RNA Synthesis(187)
DNA-PK(15)
GPR(97)
HDAC(152)
Hec1/Nek2(9)
Integrin(77)
LIM Kinase (LIMK)(7)
Mps1/TTK(2)
Nucleoside Antimetabolite/Analog(48)
Other Targets(4)
PARP(67)
PLK(26)
Potassium Channel(146)
RAD51(1)
Rho(16)
ROCK(42)
Telomerase(12)
Topoisomerase(88)
Wee1(7)
Rho
-
AZA1
catalog no : M35559
cas no: 1071098-42-4
AZA1 (Rac1/Cdc42-IN-1) is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induced apoptosis of prostate cancer cells and inhibited cell proliferation, migration and invasion.
-
Z62954982
catalog no : M34915
cas no: 1090893-12-1
Z62954982 (ZINC08010136) is a selective inhibitor of Rac1, which stunts the growth and branching of neurons.
-
CCG-257081
catalog no : M34540
cas no: 1922098-90-5
CCG-257081 (MRTF/SRF-IN-1) is an inhibitor of cardiac myosin-related transcription factor and serum response factor (MRTF/SRF) that acts by inhibiting the Rho/MRTF/SRF pathway.CCG-257081 has shown efficacy in preventing bleomycin-induced fibrosis in several mouse models.
-
ITX3
catalog no : M33387
cas no: 347323-96-0
ITX3 is a specific, non-toxic, active and selective TrioN RhoGEF inhibitor with IC50 of 76 μM. ITX3 has anticancer effects, inhibits trion mediated GTP exchange on RhoG and Rac1, inhibits NGF-mediated neurite growth in PC12 cells and REF52 fibroblast structure formation induced by trion.
-
Digeranyl bisphosphonate
catalog no : M33063
cas no: 878143-03-4
Digeranyl bisphosphonate (DGBP) is a potent geranylgeranyl pyrophosphate (GGPP) synthase inhibitor that impedes the geranyl pyrophosphorylation of Rac1 and induces autophagy without causing apoptosis.