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Cat. No. | Product Name | ||
---|---|---|---|
L1110 | 微管靶向化合物库 | 142 compounds | |
142 种靶向微管的分子集合,用于高通量筛选和高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8684 |
Sotorasib
AMG-510 |
Ras | GPCR/G Protein; MAPK |
Sotorasib (AMG-510) 是一种 KRAS G12C 共价抑制剂,具有口服活性和选择性。Sotorasib 与 KRAS G12C 非活性构象的 GDP 状态结合,抑制 KRAS 及其下游信号的传导。Sotorasib 对 KRAS G12C 突变肿瘤具有抑制活性。 | |||
T8369 |
Adagrasib
MRTX849 |
Ras | GPCR/G Protein; MAPK |
Adagrasib (MRTX849) 是一种 KRAS G12C 共价抑制剂,具有口服活性和选择性。Adagrasib 与 KRAS G12C 非活性构象的 GDP 状态结合,抑制 KRAS 及其下游信号的传导。Adagrasib 对 KRAS G12C 突变肿瘤具有抑制活性。 | |||
T13983 |
0990CL
|
cAMP; Others | GPCR/G Protein; Others |
0990CL 是一种有效的异三聚体Gαi subunit 特异性抑制剂,可与纯化的Go±在gdp 结合状态下相互作用,能够阻断α2AR 介导的cAMP 调控。 在细胞模型中低浓度0990CL 能够部分恢复cAMP 水平,高浓度的0990CL (10 μM)下,开始对细胞活力产生负面影响。 | |||
T7414 |
ARS-853
|
Apoptosis; Raf; Ras | Apoptosis; GPCR/G Protein; MAPK |
ARS-853 是一种选择性共价KRAS G12C 抑制剂,IC50为 2.5 μM。它通过与 GDP 结合的癌蛋白结合并阻止激活来抑制突变 KRAS 驱动的信号传导。 | |||
T38411 |
KRA-533
|
Others | Others |
KRA-533, a potent KRAS agonist, directly targets the GTP/GDP binding pocket within the KRAS protein, inhibiting GTP cleavage. This inhibition leads to the buildup of constitutively active GTP-bound KRAS, which subsequently activates both apoptotic and autophagic cell death pathways specifically in cancer cells. | |||
T63201 |
SOS1 activator 1
|
Others | Others |
SOS1 activator 1 是一种 SOS1 介导的核苷酸交换的激活剂(Kd: 44 nM)。SOS1 是一种鸟嘌呤核苷酸交换因子,能与 Ras 蛋白结合,催化 GDP 与 RAS 上的 GTP 交换,使原来与 Ras 结合的 GDP 交换成 GTP。 | |||
T37422 |
Ras Inhibitory Peptide
|
Others | Others |
Son of sevenless homolog 1 (Sos1) is a guanine nucleotide exchange factor (GEF) that directs the exchange of Ras-GDP to Ras-GTP by binding to SH3 domains of the growth factor receptor-bound protein 2 (Grb2), leading to the activation of ERK. Ras inhibitory peptide is a synthetic peptide that contains the sequence PVPPR, which corresponds to a region within human Sos1 that interacts with an SH3 domain of Grb2. It specifically blocks the interaction of the GEF with Grb2, preventing an interaction ... |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01209 |
DENND1A Protein, Human, Recombinant (His & SUMO)
KIAA1608,Connecdenn 1,DENN domain-containing protein 1A,DENN... |
Human | E. coli |
Guanine nucleotide exchange factor (GEF) regulating clathrin-mediated endocytosis through RAB35 activation. Promotes the exchange of GDP to GTP, converting inactive GDP-bound RAB35 into its active GTP-bound form. Regulates clathrin-mediated endocytosis of synaptic vesicles and mediates exit from early endosomes. Binds phosphatidylinositol-phosphates (PtdInsPs), with some preference for PtdIns(3)P. DENND1A Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6... | |||
TMPH-02334 |
RAB12 Protein, Human, Recombinant (His & Myc)
Ras-related protein Rab-12,RAB12 |
Human | E. coli |
The small GTPases Rab are key regulators of intracellular membrane trafficking, from the formation of transport vesicles to their fusion with membranes. Rabs cycle between an inactive GDP-bound form and an active GTP-bound form that is able to recruit to membranes different set of downstream effectors directly responsible for vesicle formation, movement, tethering and fusion. That Rab may play a role in protein transport from recycling endosomes to lysosomes regulating, for instance, the degrada... | |||
TMPH-01285 |
EEF1D Protein, Human, Recombinant (His)
Elongation factor 1-delta,EF1D,EF-1-delta,EEF1D,Antigen NY-C... |
Human | E. coli |
EF-1-beta and EF-1-delta stimulate the exchange of GDP bound to EF-1-alpha to GTP, regenerating EF-1-alpha for another round of transfer of aminoacyl-tRNAs to the ribosome.; Regulates induction of heat-shock-responsive genes through association with heat shock transcription factors and direct DNA-binding at heat shock promoter elements (HSE). | |||
TMPY-02805 |
GNGT1 Protein, Human, Recombinant (His)
guanine nucleotide binding protein (G protein), γ transducin... |
Human | E. coli |
GNGT1 is a subunit of transducin. Heterotrimeric G proteins consist of alpha, beta, and gamma subunits. They are membrane-bound GTPases that are linked to 7-TM receptors. They function as signal transducers for the 7-transmembrane-helix G protein-coupled receptors. They are involved as a modulator or transducer in various transmembrane signaling systems. G proteins are bound to GDP in the 'off' state. GNGT1 is the gamma subunit of transducin. Ligand-receptor binding results in detachment of the ... | |||
TMPH-03445 |
GSP1 Protein, S. cerevisiae, Recombinant (His)
GSP1,Genetic suppressor of PRP20-1,GTP-binding nuclear prote... |
Saccharomyces cerevisiae | P. pastoris (Yeast) |
GTP-binding protein involved in nucleocytoplasmic transport. Required for the import of protein into the nucleus and also for RNA export. Essential for cell viability. By analogy with Ras, Ran may be activated when GTP is exchanged for bound GDP by RCC1 and inactivated when GTP is hydrolyzed by Ran upon activation by RanGAP1. GSP1 Protein, S. cerevisiae, Recombinant (His) is expressed in yeast with N-6xHis tag. The predicted molecular weight is 26.7 kDa and the accession number is P32835. | |||
TMPH-01207 |
DOCK8 Protein, Human, Recombinant (His)
DOCK8,Dedicator of cytokinesis protein 8 |
Human | P. pastoris (Yeast) |
Guanine nucleotide exchange factor (GEF) which specifically activates small GTPase CDC42 by exchanging bound GDP for free GTP. During immune responses, required for interstitial dendritic cell (DC) migration by locally activating CDC42 at the leading edge membrane of DC. Required for CD4(+) T-cell migration in response to chemokine stimulation by promoting CDC42 activation at T cell leading edge membrane. Is involved in NK cell cytotoxicity by controlling polarization of microtubule-organizing c... | |||
TMPH-02622 |
DOCK8 Protein, Mouse, Recombinant (E. coli, His)
DOCK8,Dedicator of cytokinesis protein 8 |
Mouse | E. coli |
Guanine nucleotide exchange factor (GEF) which specifically activates small GTPase CDC42 by exchanging bound GDP for free GTP. During immune responses, required for interstitial dendritic cell (DC) migration by locally activating CDC42 at the leading edge membrane of DC. Required for CD4(+) T-cell migration in response to chemokine stimulation by promoting CDC42 activation at T cell leading edge membrane. Is involved in NK cell cytotoxicity controlling polarization of microtubule-organizing cent... | |||
TMPJ-01126 |
RheB Protein, Human, Recombinant (GST)
RHEB,Ras Homolog Enriched in Brain,GTP-Binding Protein Rheb,... |
Human | E. coli |
GTP-Binding Protein Rheb (RHEB) is a member of the small GTPase superfamily and encodes a lipid-anchored, cell membrane protein with five repeats of the RAS-related GTP-binding region. Highest levels of RHEB can be found in the skeletal and cardiac muscle, and it is vital in the regulation of growth and cell cycle progression due to its role in the Insulin/TOR/S6K signaling pathway. RHEB stimulates the phosphorylation of S6K1 and EIF4EBP1 through activation of mTORC1 signaling, and it activates... | |||
TMPH-02623 |
DOCK8 Protein, Mouse, Recombinant (His)
Dedicator of cytokinesis protein 8,DOCK8 |
Mouse | P. pastoris (Yeast) |
Guanine nucleotide exchange factor (GEF) which specifically activates small GTPase CDC42 by exchanging bound GDP for free GTP. During immune responses, required for interstitial dendritic cell (DC) migration by locally activating CDC42 at the leading edge membrane of DC. Required for CD4(+) T-cell migration in response to chemokine stimulation by promoting CDC42 activation at T cell leading edge membrane. Is involved in NK cell cytotoxicity controlling polarization of microtubule-organizing cent... | |||
TMPY-02802 |
GNG13 Protein, Human, Recombinant (His)
G(gamma)13,h2-35,G(γ)13,guanine nucleotide binding protein (... |
Human | E. coli |
GNG13 is a subunit of heterotrimeric G proteins which consist of alpha, beta, and gamma subunits. Heterotrimeric G proteins are membrane-bound GTPases that are linked to 7-TM receptors. They function as signal transducers for the 7-transmembrane-helix G protein-coupled receptors. They are involved as a modulator or transducer in various transmembrane signaling systems. Each G protein is composed of an alpha-, beta- and gamma-subunit and is bound to GDP in the 'off' state. Ligand-receptor binding... | |||
TMPH-02020 |
RGS17 Protein, Human, Recombinant (GST)
Regulator of G-protein signaling 17,RGS17 |
Human | E. coli |
Regulates G protein-coupled receptor signaling cascades, including signaling via muscarinic acetylcholine receptor CHRM2 and dopamine receptor DRD2. Inhibits signal transduction by increasing the GTPase activity of G protein alpha subunits, thereby driving them into their inactive GDP-bound form. Binds selectively to GNAZ and GNAI2 subunits, accelerates their GTPase activity and regulates their signaling activities. Negatively regulates mu-opioid receptor-mediated activation of the G-proteins. R... | |||
TMPY-03430 |
RheB Protein, Human, Recombinant (His)
Ras homolog enriched in brain,RHEB2 |
Human | Baculovirus Insect Cells |
RHEB is a recently discovered member of the Ras superfamily that may be involved in neural plasticity. This function is novel and not typically associated with the Ras proteins. RHEB gene is a member of the small GTPase superfamily and encodes a lipid-anchored, cell membrane protein with five repeats of the RAS-related GTP-binding region. RHEB is vital in regulation of growth and cell cycle progression due to its role in the insulin / TOR / S6K signaling pathway. The protein has GTPase activity ... | |||
TMPH-02873 |
RAB10 Protein, Mouse, Recombinant (His & SUMO)
Ras-related protein Rab-10,Rab10 |
Mouse | E. coli |
The small GTPases Rab are key regulators of intracellular membrane trafficking, from the formation of transport vesicles to their fusion with membranes. Rabs cycle between an inactive GDP-bound form and an active GTP-bound form that is able to recruit to membranes different set of downstream effectors directly responsible for vesicle formation, movement, tethering and fusion. That Rab is mainly involved in the biosynthetic transport of proteins from the Golgi to the plasma membrane. Regulates, f... | |||
TMPH-01524 |
KPNA1 Protein, Human, Recombinant (His)
Nucleoprotein interactor 1,SRP1-beta,Karyopherin subunit alp... |
Human | E. coli |
Functions in nuclear protein import as an adapter protein for nuclear receptor KPNB1. Binds specifically and directly to substrates containing either a simple or bipartite NLS motif. Docking of the importin/substrate complex to the nuclear pore complex (NPC) is mediated by KPNB1 through binding to nucleoporin FxFG repeats and the complex is subsequently translocated through the pore by an energy requiring, Ran-dependent mechanism. At the nucleoplasmic side of the NPC, Ran binds to importin-beta ... | |||
TMPY-01187 |
Rac1 Protein, Human, Recombinant (GST)
Rac-1,p21-Rac1,MIG5,ras-related C3 botulinum toxin substrate... |
Human | Baculovirus Insect Cells |
RAC1 is a GTPase that belongs to the RAS superfamily of small GTP-binding proteins. Members of this superfamily appear to regulate a diverse array of cellular events, including the control of cell growth, cytoskeletal reorganization, and the activation of protein kinases. Two transcript variants encoding different isoforms have been found for RAC1 gene. RAC1 is a plasma membrane-associated small GTPase which cycles between active GTP-bound and inactive GDP-bound states. In its active state, bind... |