目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T61488 | |||
Dynole 2 24 是一种基于吲哚的dynamin GTPase 抑制剂 (对 dynamin I 的IC50=0.56 μM)。Dynole 2 24 无毒,在体外和细胞内显示出增强的抗动力蛋白I 和II 的效力 (IC (CME)=1.9 μM)。Dynole 2 24 对 dynamin I 的选择性为4.4倍。Dynole 2 24在网格蛋白介导的内吞作用的细胞抑制剂中具有活性。CME: Clathrin mediated endocytosis | |||
TP1947 | |||
Dynamin-related protein 1 (Drp1) inhibitor, inhibits Drp1 GTPase activity. Displays no effect on dynamin 1 or other mitochondrial dynamics-related proteins. Inhibits mitochondrial fission, dysfunction and reactive oxygen species (ROS) production in vitro. | |||
T83891 | |||
Sulfonadyn-47是一种dynamin抑制剂,能在无细胞测定中抑制dynamin的GTP酶活性(IC50 = 3.5 µM)。在U2OS细胞中,Sulfonadyn-47抑制clathrin介导的内吞作用(IC50 = 27.3 µM),同时在分离的大鼠脑突触体中抑制由去极化刺激的FM4-64摄取,后者是突触小泡内吞(SVE)的标志(IC50 = 12.3 µM)。在体内,Sulfonadyn-47(30和60 mg/kg)在6 Hz角膜电引发小鼠癫痫模型中具有抗惊厥活性。 | |||
T72894 | |||
Clathrin-IN-2 是网格蛋白介导的内吞作用(CME)的有效抑制剂,IC50值为 2.3 μM。 Clathrin-IN-2 还对dyn I GTPase 具有抑制作用,IC50值为 7.7 μM。 | |||
T68788 | |||
Ellipticine quinone, also known as NSC-383230, is a Drp1 inhibitor. rpitor1 and Drpitor1a inhibited the GTPase activity of Drp1 without inhibiting the GTPase of dynamin 1. Ellipticine quinone showed greater potency than the current std. Drp1 GTPase inhibitor, mdivi-1, (IC50 for mitochondrial fragmentation are (0.06, and 10 μM, resp.). Ellipticine quinone suppressed lung cancer tumor growth in a mouse xenograft model. Ellipticine quinone also inhibited mitochondrial ROS prodn., prevented mitochondrial fission, and improved right ventricular diastolic dysfunction during IR injury. | |||
T73456 | |||
DRP1i27是一种有效抑制人源Drp1(动力蛋白相关蛋白1)的化合物。它通过与Drp1的GTPase位点结合,并与Gln34及Asp218形成氢键来发挥作用。DRP1i27主要针对Drp1介导的线粒体裂变细胞系模型,能有效防止模拟缺血再灌注引起的损伤。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
TMPH-01254 | DNM1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Microtubule-associated force-producing protein involved in producing microtubule bundles and able to bind and hydrolyze GTP. Most probably involved in vesicular trafficking processes. Involved in receptor-mediated endocytosis.
|
|||||
TMPH-01255 | DNM1L Protein, Human, Recombinant (His & Myc) | Human | E. coli | ||
Functions in mitochondrial and peroxisomal division. Mediates membrane fission through oligomerization into membrane-associated tubular structures that wrap around the scission site to constrict and sever the mitochondrial membrane through a GTP hydrolysis-dependent mechanism. The specific recruitment at scission sites is mediated by membrane receptors like MFF, MIEF1 and MIEF2 for mitochondrial membranes. While the recruitment by the membrane receptors is GTP-dependent, the following hydrolysis of GTP induces the dissociation from the receptors and allows DNM1L filaments to curl into closed rings that are probably sufficient to sever a double membrane. Acts downstream of PINK1 to promote mitochondrial fission in a PRKN-dependent manner. Plays an important role in mitochondrial fission during mitosis. Through its function in mitochondrial division, ensures the survival of at least some types of postmitotic neurons, including Purkinje cells, by suppressing oxidative damage. Required for normal brain development, including that of cerebellum. Facilitates developmentally regulated apoptosis during neural tube formation. Required for a normal rate of cytochrome c release and caspase activation during apoptosis; this requirement may depend upon the cell type and the physiological apoptotic cues. Required for formation of endocytic vesicles. Proposed to regulate synaptic vesicle membrane dynamics through association with BCL2L1 isoform Bcl-X(L) which stimulates its GTPase activity in synaptic vesicles; the function may require its recruitment by MFF to clathrin-containing vesicles. Required for programmed necrosis execution. Rhythmic control of its activity following phosphorylation at Ser-637 is essential for the circadian control of mitochondrial ATP production.; Inhibits peroxisomal division when overexpressed.; Inhibits peroxisomal division when overexpressed.
|
|||||
TMPY-03439 | UBASH3A Protein, Human, Recombinant (aa 354-623, His) | Human | E. coli | ||
UBASH3A is a member of the T-cell ubiquitin ligand (TULA) family. This family consists of two members. Both of them can negatively regulate T-cell signaling. UBASH3A can facilitate growth factor withdrawal-induced apoptosis in T cells, which may occur via its interaction with AIF, an apoptosis-inducing factor. Alternative splicing of UBASH3A gene results in multiple transcript variants. It interferes with CBL-mediated down-regulation and degradation of receptor-type tyrosine kinases. UBASH3A promotes accumulation of activated target receptors, such as T-cell receptors, EGFR and PDGFRB, on the cell surface. UBASH3A also exhibits negligigle protein tyrosine phosphatase activity at neutral pH. It may act as a dominant-negative regulator of UBASH3B-dependent dephosphorylation. It may also inhibit dynamin-dependent endocytic pathways by functionally sequestering dynamin via its SH3 domain.
|
|||||
TMPH-03149 | Porcine circovirus 2 (PCV2) Capsid Protein (E. coli, His) | PCV2 | E. coli | ||
Self-assembles to form the virion icosahedral capsid with a T=1 symmetry. This very small capsid (17 - 22 nm in diameter) allows the virus to be very stable in the environment and resistant to some disinfectants, including detergents. Essential for the initial attachment to heparan sulfate moieties and chondroitin sulfate B of the host cell surface proteoglycans. After attachment, the virus is internalized in a clathrin-, caveolae- and dynamin-independent, actin and Rho-GTPase-mediated pathway and traffics to the nucleus. The capsid protein binds and transports the viral genome and Rep across the nuclear envelope.
|
|||||
TMPH-01802 | NME4 Protein, Human, Recombinant (GST) | Human | E. coli | ||
Major role in the synthesis of nucleoside triphosphates other than ATP. The ATP gamma phosphate is transferred to the NDP beta phosphate via a ping-pong mechanism, using a phosphorylated active-site intermediate. Through the catalyzed exchange of gamma-phosphate between di- and triphosphonucleosides participates in regulation of intracellular nucleotide homeostasis. Binds to anionic phospholipids, predominantly to cardiolipin; the binding inhibits its phosphotransfer activity. Acts as mitochondria-specific NDK; its association with cardiolipin-containing mitochondrial inner membrane is coupled to respiration suggesting that ADP locally regenerated in the mitochondrion innermembrane space by its activity is directly taken up via ANT ADP/ATP translocase into the matrix space to stimulate respiratory ATP regeneration. Proposed to increase GTP-loading on dynamin-related GTPase OPA1 in mitochondria. In vitro can induce liposome cross-linking suggesting that it can cross-link inner and outer membranes to form contact sites, and promotes intermembrane migration of anionic phosphoplipids. Promotes the redistribution of cardiolipin between the mitochondrial inner membrane and outer membrane which is implicated in pro-apoptotic signaling.
|