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)
PAK(13)
PARP(67)
PLK(26)
Potassium Channel(146)
RAD51(1)
Rho(16)
ROCK(42)
Telomerase(12)
Topoisomerase(88)
Wee1(7)
Rho
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AZA1
产品货号 : M35559
cas no: 1071098-42-4
AZA1 是 Rac1 和 Cdc42 的有效抑制剂。AZA1 诱导前列腺癌细胞凋亡并抑制增殖,迁移和侵袭。 -
Z62954982
产品货号 : M34915
cas no: 1090893-12-1
Z62954982 (ZINC08010136) 是一种强效的、选择性的、细胞渗透性强的 Rac1 (IC50=12 μM) 抑制剂,比 NSC23766 (HY-15723A) (IC50=50 μM) 有效性强 4 倍。Z62954982 干扰 Rac1/Tiam1 复合物,降低活性 Rac1 (GTP 结合的 Rac1) 的细胞质水平,而不影响其他 Rho GTPases (如,Cdc42 或 RhoA) 的活性。 -
CCG-257081
产品货号 : M34540
cas no: 1922098-90-5
MRTF/SRF-IN-1 (example 41) 是心肌素相关转录因子和血清反应因子 (MRTF/SRF) 的抑制剂。MRTF/SRF-IN-1 可用于预防癌症和纤维化的研究。 -
ITX3
产品货号 : M33387
cas no: 347323-96-0
ITX3 是特异的、无毒的 TrioN (N-terminal GEF domain of the multidomain Trio protein) 抑制剂,IC50 值为 76 μM。ITX3 可用于活性分子的研究。 -
Digeranyl bisphosphonate
产品货号 : M33063
cas no: 878143-03-4
Digeranyl bisphosphonate (DGBP) 是一种有效的香叶基焦磷酸香叶酯 (GGPP) 合酶抑制剂,抑制 Rac1 的香叶基焦磷酸化。