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We Devoted Ourselves To The Development Of Biomedical Research Reagent.

PRODUCT

[Membrane Transporter/ Ion Channel]

(-)-Blebbistatin,856925-71-8,IC-0201092

Price : $108.00Price : ￥1080.00

(-)-Blebbistatin is a cell-permeable non-muscle myosin II ATPases inhibitor with an IC50 range of 2 μM [1,2]. Non-muscle myosin II (NM II), an actin-binding protein, plays a central role in regulation of cell migration, adhesion and differentiation [4]. Recent insight into the importance of NM II in these processes has been highlighted by genetic deletion and mutation methods that discovered NM II mutations affect the function of a wide range of proteins and cause monogenic diseases [5.6]. (-)-Blebbistatin is a small molecule inhibitor and preferentially binds to the myosin-ADP-Pi complex to slow down phosphate release [2]. The inhibitor completely eliminate contraction of activity of actin-activated Mg-ATPase and motility of myosins II for several species in vitro (IC50 = 0.5-5.0 μM) [8,9], but it has poor effects on smooth muscle myosin II (IC50 =80 μM) and myosins I,V, and X [3]. Furthermore, blebbistatin can potently inhibit mammalian arterial smooth muscle (IC50=5 μM) [9]. The property that blebbistatin blocks myosin II in an actin-detached state and prevents rigid actomyosin cross-linking is a great advantage in vivo applications [2,11]. In a constant-pressure gra......
[Membrane Transporter/ Ion Channel]

Brefeldin A,20350-15-6,IC-0201281

Price : $77.30Price : ￥773.00

Brefeldin A (BFA) is a fungal macrocyclic lactone and a potent, reversible inhibitor of intracellular vesicle formation and protein trafficking between the endoplasmic reticulum (ER) and the Golgi apparatus[1][2].Brefeldin A is an ATPase inhibitor with IC50 value of 0.2 µM[9].Brefeldin A and its analogs are promising inhibitors in drug development due to a number of key features such as apoptosis?inducing properties as well as antitumor, antifungal, and antiviral effects [3,6].Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity[4]. Perturbation of ER-Golgi trafficking by brefeldin A (BFA) treatment attenuated nucleotide-binding oligomerization domain-like receptor family, pyrin-domain-containing 3 (NLRP3) inflammasome activation in mouse bone marrow-derived macrophages (BMDMs) [5].ADP-ribosylation of BARS is mediated by formation of a conjugate between Brefeldin A and ADPR. BARS shows BAC binding when incubated with the medium from the brefeldin A-treated CD38+ HeLa cells[3].Brefeldin A induces anchorage-independent cell death in MDA-MB-231 breast cancer cells with an EC50 of 0.016 µg/mL, inhibits the formation of MDA-MB-231 c......
[Membrane Transporter/ Ion Channel]

MYK-461,1642288-47-8,IC-0201470

Price : $58.50Price : ￥585.00

MYK-461 is a small molecular chemical that reduces contractility by decreasing the adenosine triphosphatase activity of the cardiac myosin heavy chain. MYK-461 reduced ATPase activity in a dose-dependent manner with IC50 value of 0.3 mM after treatment of mouse cardiac myofibrils. MYK-461 (>10 mM) decreased the maximal ATPase rate by ~90%. MYK-461 is active against both the A and B isoforms of cardiac myosin. Treatment with MYK-461 decreased the rate of phosphate release in a dose-dependent manner without slowing adenosine diphosphate (ADP) release. MYK-461 decreases the myosin duty ratio and thus reduces the ensemble power, force and contractility produced by the sarcomere. Exposure to MYK-461 reduced maximal tension in a dose-dependent manner (~70% reduction at 1.0 mM) without altering the pCa50 or the tension at lower calcium concentrations. MYK-461 showed a dose-dependent reduction in fractional shortening (IC50=0.18 mM) without changing the calcium transient after treated with adult rat ventricular cardiomyocytes. MYK-461 plasma exposures decreased fractional shortening in WT and mutant mice. Although MYK-461 inhibits the ATPase activity of skeletal myosin with a l......
[Membrane Transporter/ Ion Channel]

Oligomycin A,579-13-5,IC-0201659

Price : $120.00Price : ￥1200.00

Oligomycin A is an inhibitor of ATP synthase, which inhibits the process taking place on mitochondria coupling membrane that depended on ATP and oxidative phosphorylation [1]. Oligomycin A produced a concentration-dependent block of Icrac with similar characteristics, but with lower potency than oligomycin B. Fits of averaged concentration-response data to a logistic function yielded IC50 values and slope factor coefficients (respectively) of 13.5 μM and 0.85 for oligomycin A, and 2.3 μM and 0.82 for oligomycin B. A two-way analysis of variance confirmed a significantly greater inhibition by oligomycin B over the concentration range tested [2]. Oligomycin A treated Wt(widetype) mice have decreased ATP levels in the liver. Concomitantly, these mice showed an enhanced apoptosis in hepatocytes as Tg mice after LPS/GalN administration [3]. Further activation of AMPK was detected in Wt mice after treatment with oligomycin A. Collectively, these data demonstrated that UCP2 expression in hepatocytes could alter mitochondrial parameters leading to activation of AMPK [3].
[Membrane Transporter/ Ion Channel]

Thapsigargin,67526-95-8,IC-0201848

Price : $150.00Price : ￥1500.00

Thapsigargin is an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase pump.[1] Thapsigargin can induce a potent host antiviral response that blocks influenza A virus replication at nano-molar non-cytotoxic levels.[2] In vitro efficacy test it shown that HEp2 cells primed with 0.5 µM Thapsigargin (as a non-cytotoxic inhibitor) before infection reduced progeny virus production by almost 10,000-fold. A549 cells primed with 0.3 µM Thapsigargin, in turn, was more inhibitory than the RDV-treated cells by 450-fold.[3] In vitro, treatment with 10 μM of Thapsigargin (a specific blocker SERCAs), can null EMF response by impairing the replenishment of the ER.[4] In vitro test it indicated that treatment with 0.001 μM - 1 μM of thapsigargin may arrest cell proliferations in MH7A human rheumatoid arthritis synovial cells in a time- and dose-dependent manner.[5] Treatment with 1 μM of thapsigargin mediated sensitization to TRAIL in ESCC cell lines through the activation of AMPK from the aspects of protein function and existence.[7] In vivo efficacy study it demonstrated that treatment with 0.5ug/g/body weight of Thapsigargin was safe and did not elicit any adverse effect......
[Membrane Transporter/ Ion Channel]

Tariquidar,206873-63-4,IC-0230387

Price : $33.90Price : ￥339.00

Tariquidar is a potent inhibitor of P-glycoprotein (Pgp), a 170-kDa transmembrane protein acting as a drug efflux pump to actively transport structurally unrelated compounds out of cells, that noncompetitively inhibits the basal the activity of ATPase associated with Pgp. Tariquidar contains a tertiary amine, dimethoxyphenyl group and amide group in its chemical structure, which contribute to its inhibition against Pgp. Results of in vitro assays of three different models have shown that Tariquidar inhibits Pgp with 50% inhibition concentration IC50 values ranging from 15 to 223 nM. However, the inhibition by tariquidar is Pgp-specific and attenuated in tumor cell lines, where multidrug resistance is mediated by multidrug resistance-associated protein.

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