atpase-in-2

ATPase-IN-2 is an effective bacterial F1F0-ATPase inhibitor. It interferes with energy metabolism by blocking ATP synthesis, used for developing novel antibiotics against drug-resistant pathogens.

CB-6644 is a small molecule inhibitor of the ATPase activity of the RUVBL1/2 complex. It specifically interacts with RUVBL1/2 in cancer cells and blocks the ATPase activity of RUVBL1/2 with a half-maximal inhibitory concentration (IC50) of 15 nM[1].

Lansoprazole (A-65006) is a 2, 2, 2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

Paxilline is an indole alkaloid mycotoxin from *Penicillium paxilli*, acting as a potent BK channel inhibitor via an almost exclusively closed-channel block mechanism. Paxilline possesses significant anticonvulsant activity.

JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.

Brr2-IN-2 (Compound 30) is an inhibitor of Brr2, exhibiting an IC50 of 42 nM against Brr2 ATPase.

TIP48/49-IN-1 (Compound B) is an orally active, specific RUVBL1/2 ATPase inhibitor, with an IC50 of 59 nM for purified RUVBL1/2. It disrupts the DNA replication process, causing S phase arrest, induces apoptosis, inhibits tumor growth, and enhances the radiosensitivity of non-small cell lung cancer cells (NSCLC).

ATPase-IN-6 is an inhibitor of H+/K+-ATPase (ATPase) and a derivative of imidazopyridine. It exhibits significant antiviral activity against various viruses, such as HIV-1 and SARS-CoV-2. ATPase-IN-6 is applicable in antiviral infection research.

CHIKV nsP2 protease-IN-2 (Compound 2o) is an allosteric inhibitor of the non-structural protein 2 helicase (nsP2hel), with IC50 values of 0.5 μM for nsP2 ATPase and 0.9 μM for RNA helicase. It exhibits broad-spectrum antiviral activity against alphaviruses, effectively targeting Chikungunya virus (CHIKV), Mayaro virus (MAYV), and Venezuelan equine encephalitis virus (VEEV), with an EC50 of 0.12 μM against CHIKV-nLuc. This compound is useful for research on alphavirus infections.

Myosin-IN-2 (Example 16) is an inhibitor of Myosin ATPase, exhibiting an IC50 value of 1.06 μM. It is applicable in research related to cardiac diseases, including hypertrophic cardiomyopathy (HCM).

Aha1/Hsp90-IN-2 is a selective inhibitor of the Hsp90/Aha1 interaction, with an IC50 of 1.46 μM. By specifically blocking the binding of Hsp90 to Aha1, Aha1/Hsp90-IN-2 inhibits the activation of Hsp90 ATPase activity mediated by Aha1, thereby reducing tau protein aggregation. This compound can be used for researching neurodegenerative diseases such as Alzheimer's disease.

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)16-HETE is the racemic version of a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation. The biological activity of 16-HETE is stereospecific. 16(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney, however 16(S)-HETE does not affect perfusion pressure. At a concentration of 2 μM the (S)-enantiomer of 16-HETE inhibits proximal tubule ATPase activity by as much as 60%, whereas the (R)-isomer has negligible effects on ATPase activity.

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)17-HETE is the racemic version of a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney. At a concentration of 2 μM the (S)-enantiomer of 17-HETE inhibits proximal tubule ATPase activity by as much as 70%, whereas the (R)-isomer is inactive.

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. 16(S)-HETE inhibits proximal tubule ATPase activity by as much as 60% at a concentration of 2 µM.[1]

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. 16(S)-HETE inhibits proximal tubule ATPase activity by as much as 60% at a concentration of 2 μM.

17(S)-HETE is an arachidonic acid metabolite generated via the CYP450 pathway. 17(S)-HETE acts as an allosteric activator of CYP450 1B1 and an ATPase inhibitor, capable of inducing cardiac hypertrophy.

para-amino-Blebbistatin is a more water-soluble form of (S)-4'-nitro-blebbistatin , which is a more stable and less phototoxic form of (-)-blebbistatin .1,2,3 (-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases that rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM).2,3,4 Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications.5,6 The addition of a 4'-amino group increases its water solubility, decreases the inherent fluorescence, stabilizes the molecule to circumvent its degradation by prolonged blue light exposure, and decreases its phototoxicity while retaining the in vitro and in vivo activity of blebbistatin.7 para-amino-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer. |1. Várkuti, B.H., Képiró, M., Horváth, I.á., et al. A highly soluble, non-phototoxic, non-fluorescent blebbistatin derivative. Sci. Rep. 6:26141, (2016).|2. Straight, A.F., Cheung, A., Limouze, J., et al. Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science 299(5613), 1743-1747 (2003).|3. Kovács, M., Tóth, J., Hetényi, C., et al. Mechanism of blebbistatin inhibition of myosin II. J. Biol. Chem. 279(34), 35557-35563 (2004).|4. Limouze, J., Straight, A.F., Mitchison, T., et al. Specificity of blebbistatin, an inhibitor of myosin II. J. Muscle Res. Cell Motil. 25(4-5), 337-341 (2004).|5. Kolega, J. Phototoxicity and photoinactivation of blebbistatin in UV and visible light. Biochem. Biophys. Res. Commun. 320(3), 1020-1025 (2004).|6. Sakamoto, T., Limouze, J., Combs, C.A., et al. Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. Biochemistry 44(2), 584-588 (2005).|7. Verhasselt, S., Roman, B.I., Bracke, M.E., et al. Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs. Eur. J. Med. Chem. 136, 85-103 (2017).

KUS121 is a valosin-containing protein modulator that inhibits VCP ATPase activity with an IC50 of 330 nM, suppresses tunicamycin-induced ATP depletion, cell death, and CHOP upregulation in HeLa cells, protects primary cortical neurons from oxygen-glucose deprivation injury in vitro, reduces infarct volume and improves motor performance in mouse models of focal cerebral ischemia, and preserves retinal structure and visual function in rd10 retinitis pigmentosa models, supporting its investigation in neuroprotection and ischemic disease research.

Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg/ml) and induces efflux of potassium ions from B. subtilis without affecting Na+/K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg/ml. It inhibits the growth of B. halodurans (MIC = 10 ng/ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromycin (3.4 nM) reverses bleomycin-induced cell cycle arrest at the G2 phase in Jurkat cells. It inhibits replication of the HIV-1 strains LAV-1 and RF and the HIV-2 strain LAV-2 in MT-4 cells (IC50s = 0.008, 0.11, and 0.007 μM, respectively). It also inhibits replication of a clinical isolate of HIV-1, strain KK-1, in MT-4 cells and peripheral blood mononuclear cells (PBMCs; IC50s = 0.14 and <0.1 μM, respectively).

5-hydroxy Omeprazole is one of the major metabolites of the proton pump inhibitor omeprazole in the body; it is formed by hydroxylation catalyzed by the CYP2C19 and CYP3A4 enzymes in the liver. 5-hydroxy Omeprazole can be used in pharmacokinetic studies.

Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 17-HETE is a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney. 17(R)-HETE is an inactive isomer of 17-HETE, whereas the (S) enantiomer can inhibit proximal tubule ATPase activity at a concentration of 2 μM.

β-Cyfluthrin is a type II synthetic pyrethroid compound commonly utilized as an active ingredient in agricultural insecticide products. It exerts its insecticidal properties by acting as a neurotoxicant, primarily impacting the calcium concentration within nervous tissue. This effect is achieved through the inhibition of Ca 2+ ATPase, a crucial component involved in calcium transport.

1. Oleandrin (Folinerin), the principal cardiac glycoside component of PBI-524, can quantitatively account for regulation of BDNF at both the protein and transcriptional levels. 2. Oleandrin are known to inhibit the Na, K-ATPase pump, resulting in a consequent increase in calcium influx in heart muscle. 3. Oleandrin has stronger anti-proliferative activity in undifferentiated CaCO-2 cells (IC50, 8.25 nM) , causes an autophagic cell death and altered ERK phosphorylation in undifferentiated.

1. Periplocin (Periplocoside) has anti-cancer effects on lung cancer cells, induces apoptosis and inhibits growth of cancer cells by the beta-catenin/Tcf signaling pathway. 2. Periplocin is used for treatment of rheumatoid arthritis, reinforcement of bones and tendons, palpitations or shortness of breath and lower extremity edema in traditional medicine.