Catalog No.
Product Name
Application
Product Information
Citations
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PDE5A Inhibitor
PF-03049423 is a potent and highly selective inhibitor of phosphodiesterase-5A (PDE5A), demonstrating an IC50 of approximately 0.2 nM for both rat and human platelet enzymes. This compound is primarily used in research related to acute ischemic stroke, providing valuable insights into the therapeutic potential of PDE5A modulation in cerebrovascular conditions. Its specificity and potency make it a critical tool for exploring the role of phosphodiesterase inhibition in neuroprotection and recovery following ischemic events. -
PDE4/PDE5 Inhibitor
PDE4/5-IN-1 is a selective inhibitor targeting phosphodiesterase 4 and 5 (PDE4/5). This compound effectively inhibits the activity of PDE5, PDE4B2, and PDE4D2, leading to relaxation of isolated rat prostate tissue and enhanced nitric oxide-induced relaxation. Additionally, PDE4/5-IN-1 reduces alpha-1 adrenoceptor-mediated contractile responses and inhibits the proliferation of human hyperplastic prostate cells. It is a valuable tool for research into benign prostatic hyperplasia. -
PDE1 Inhibitor
PDE1-IN-4 is a selective inhibitor of phosphodiesterase-1 (PDE1), demonstrating IC50 values of 10 nM, 145 nM, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. This compound effectively inhibits the TGF-β1-induced differentiation of human lung fibroblasts into myofibroblasts, showcasing its potential in anti-fibrosis research. By modulating the levels of cAMP and cGMP, PDE1-IN-4 serves as a valuable tool for investigating therapeutic strategies in idiopathic pulmonary fibrosis (IPF). -
PDE4 Inhibitor
PDE4-IN-19 is a selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating IC50 values of less than 10 nM for PDE4B1 and between 10-100 nM for PDE4D3. This compound plays a significant role in modulating intracellular levels of cyclic AMP, making it valuable for research on inflammatory diseases and neurological conditions. PDE4-IN-19 is useful in studying the effects of PDE4 inhibition on cellular signaling pathways and may aid in the development of therapeutics targeting these pathways. -
PDE7 Inhibitor
P7-2104 is a potent inhibitor of phosphodiesterase 7 (PDE7), demonstrating an IC50 of 31 nM. This compound is valuable for studies aimed at modulating cyclic nucleotide signaling pathways, particularly in neurological research. Additionally, P7-2104 can be labeled with carbon-11 for use in positron emission tomography (PET) neuroimaging applications, aiding in the exploration of PDE7's role in various neurological disorders. -
PDE3/PDE4 Inhibitor
Ensifentrine tosylate is a potent dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4), exhibiting IC50 values of 0.4 nM and 1479 nM, respectively. By inhibiting these enzymes, Ensifentrine tosylate enhances levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lung cells, leading to bronchodilation and suppression of inflammatory cell activation and migration. This compound is instrumental in research pertaining to chronic obstructive pulmonary disease (COPD). -
PDE3/PDE4 Inhibitor
Pumafentrine is a potent orally active dual inhibitor of phosphodiesterase type 3 (PDE3) and phosphodiesterase type 4 (PDE4). It has demonstrated the ability to ameliorate clinical symptoms and reduce colonic TNFα production in murine models of Dextran sulphate sodium (DSS)-induced colitis. Pumafentrine is relevant for research in inflammation and gastrointestinal disorders, providing insights into therapeutic strategies targeting these pathways. -
PDE1 Inhibitor
PF-04827736 is a selective phosphodiesterase 1 (PDE1) inhibitor, exhibiting IC50 values of 9.1 nM, 38 nM, and 42 nM for PDE1B, PDE1C, and PDE1A, respectively. This compound demonstrates a high degree of selectivity for human PDE1 compared to other members of the PDE superfamily (PDE2-PDE11). PF-04827736 is primarily utilized in research related to cardiovascular disease, providing valuable insights into the role of PDE1 in cardiovascular pathology and potential therapeutic interventions. -
Phosphodiesterase (PDE)
Hoquizil hydrochloride functions primarily as a phosphodiesterase (PDE) inhibitor, presenting significant bronchodilator activity. It effectively relaxes smooth muscle tissue, making it a valuable tool in the study of airway conditions and potential therapeutic applications for respiratory diseases. Its oral bioactivity enhances its relevance in pharmacological research and drug development. -
PDE5 Inhibitor
PDE5-IN-1 is a potent phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 5.6 nM and notable oral bioavailability. It interacts with the catalytic domain of PDE5 through hydrogen bonds with the Q817 residue and π-π stacking with the F820 residue. PDE5-IN-1 demonstrates significant anti-cardiac hypertrophy and vasodilatory effects, effectively lowering mean pulmonary arterial pressure and right ventricular hypertrophy index. This compound is valuable for research focused on pulmonary arterial hypertension. -
PDE-10A/A2AR Antagonist
PBF-999 is a dual antagonist of phosphodiesterase 10A (PDE-10A) and adenosine A2A receptors (A2AR). This compound exhibits significant modulation of intracellular signaling pathways, contributing to its potential in neuroscience research, particularly in studying disorders such as schizophrenia and Parkinson's disease. PBF-999 may facilitate insights into the therapeutic effects of PDE-10A and A2A receptor signaling in cognitive and motor function. -
PDE4 Inhibitor
Ronomilast is a potent phosphodiesterase-4 (PDE4) inhibitor, exhibiting an IC50 of 3 nM. This compound is primarily utilized in research focused on inflammation-related diseases. By inhibiting PDE4, Ronomilast increases intracellular cyclic AMP levels, thereby modulating inflammatory responses and offering insights into therapeutic strategies for various inflammatory conditions. -
CYP Isozymes Inhibitor
RPR203494 is a selective inhibitor of cytochrome P450 (CYP) isozymes, with significant activity against p38 mitogen-activated protein kinase, exhibiting an IC50 of 9 nM and an EC50 of 60 nM. This compound effectively inhibits hepatic CYP enzymes, making it a valuable tool in the study of drug metabolism and pharmacokinetics. RPR203494 holds potential for research applications related to rheumatoid arthritis and other inflammatory conditions, aiding in the exploration of therapeutic strategies targeting CYP-mediated pathways. -
NMT Inhibitor
MYX1715 is a potent inhibitor of N-Myristoyltransferase (NMT) with a KD value of 0.09 nM. This compound effectively inhibits the proliferation of LU0884 and LU2511 cell lines, demonstrating IC50 values of 44 nM and 9 nM, respectively. MYX1715 has shown significant antitumor activity against neuroblastoma and gastric cancer in murine models, and it may be exploited as an antibody-drug conjugate (ADC) toxin for targeted cancer therapies. -
Nampt Inhibitor
Nampt-IN-10 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), exhibiting nanomolar inhibitory activity in various cancer cell lines, including MDA-MB453, NCI-N87, and NCI-H526. This compound can be utilized as a payload in antibody-drug conjugates (ADCs), where it has been shown to enhance anti-tumor efficacy. It serves as a valuable tool for researchers investigating NAMPT's role in cancer metabolism and therapeutic resistance. -
Carbonic Anhydrase Inhibitor
5,6-Dihydro-2H-pyran-2-one is a prodrug that functions as a selective inhibitor of carbonic anhydrases. It exhibits inhibitory activity against the tumor-associated isoform hCA IX and the cytoplasmic form hCA I, with Ki values of 1.35 μM and 8.03 μM, respectively. This compound is valuable for investigating mechanisms of hypoxia-related cancer, providing insights into tumor biology and potential therapeutic targets. -
Carbonic Anhydrase Inhibitor
2-Aminobenzenesulfonamide is an inhibitor of carbonic anhydrase IX, an enzyme implicated in various physiological processes, including respiration and acid-base balance. This compound exhibits significant biological activity, making it a valuable tool in cancer research and the study of metabolic disorders. Its ability to modulate carbonic anhydrase activity positions it as a potential lead compound for therapeutic development in conditions where altered enzyme activity plays a crucial role. -
Carbonic Anhydrase Inhibitor
Lasamide is a potent inhibitor of human carbonic anhydrases, specifically targeting hCAXII and hCAIX with Ki values of 7.54 nM and 2.76 nM, respectively. This compound exhibits significant biological activity in regulating pH and bicarbonate levels, making it valuable in research areas related to cancer, glaucoma, and metabolic disorders. Its specificity for human carbonic anhydrase isoforms allows for precise investigation of the enzyme's role in physiological and pathological processes. -
Carbonic Anhydrase Inhibitor
4-Chloro-3-sulfamoylbenzoic acid is a potent inhibitor of human carbonic anhydrase, specifically targeting cytosolic isoforms hCA I and hCA II, as well as transmembrane isoforms hCA IV and hCA IX. Its inhibition of these enzymes is significant in the study of glaucoma-associated conditions and tumor hypoxia-induced responses. This compound is valuable for research applications focused on exploring the roles of carbonic anhydrases in various physiological and pathological processes. -
COX-2/Carbonic Anhydrase Inhibitor
Polmacoxib is a novel, orally active nonsteroidal anti-inflammatory drug (NSAID) that acts as a dual inhibitor of cyclooxygenase-2 (COX-2) and carbonic anhydrase, with an IC50 value of approximately 0.1 μg/ml for COX-2. It exhibits significant biological activity by inhibiting the growth of colorectal adenomas and tumors in mouse models, making it a promising tool for cancer research. Polmacoxib is valuable for studying the roles of COX-2 and carbonic anhydrase in cancer biology and inflammation. -
Carbonic Anhydrase Inhibitor
hCAI/II-IN-6 is a selective inhibitor of human carbonic anhydrase isoforms II and VII, exhibiting Ki values of 4.9 nM and 6.5 nM, respectively. This compound demonstrates pronounced anticonvulsant activity and provides protective effects against maximal electroshock (MES) seizures in vivo. hCAI/II-IN-6 serves as a valuable tool for research studies focusing on epilepsy and related neurophysiological conditions. -
Carbonic Anhydrase II Inhibitor
Carbonic Anhydrase Inhibitor 2 specifically targets carbonic anhydrase II, functioning as an effective inhibitor. This compound is primarily used in research applications related to the modulation of intraocular pressure and may offer insights into potential therapeutic strategies for glaucoma. Its ability to influence carbonic anhydrase activity highlights its significance in biochemical studies and pharmacological investigations. -
Carbonic Anhydrase Inhibitor
hCAIX-IN-18 is a potent inhibitor of carbonic anhydrase (CA), demonstrating inhibition constants (Kis) of 3.5 nM, 9.4 nM, 43.0 nM, and 8.2 nM for human carbonic anhydrases I, II, IX, and XII, respectively. This compound is particularly relevant for cancer research, where it may affect tumor growth and metabolism through the modulation of CA activity. Its specificity and efficacy make it a valuable tool for investigating the role of carbonic anhydrases in various pathological conditions. -
Carbonic Anhydrase II Inhibitor
Dorzolamide is a potent inhibitor of carbonic anhydrase II, exhibiting an IC50 of 0.18 nM for red blood cell CA-II and 600 nM for CA-I. This compound is known for its therapeutic applications in reducing intraocular pressure and has demonstrated potential anti-tumor activity. It is a valuable reagent for research in cancer biology and ocular studies. -
Carbonic Anhydrase Inhibitor
Carbonic anhydrase inhibitor 17 is a pyridazine-tethered sulfonamide that specifically targets carbonic anhydrase II with an impressive IC50 value of 0.63 nM. This compound demonstrates potent inhibitory activity, making it a valuable tool for studying the role of carbonic anhydrases in various physiological and pathological processes. Its application is significant in research areas such as enzyme regulation, metabolic disorders, and cancer biology. -
α-Glucosidase Inhibitor
α-Glucosidase-IN-63 is a potent inhibitor of α-Glucosidase, displaying an IC50 value of 0.44 μM. Additionally, it inhibits human carbonic anhydrase II (hCA II) with a Ki of 7.0 nM. This compound is of interest for research applications focusing on glucose metabolism and enzymatic regulation in metabolic disorders. Its oral effectiveness enhances its utility in in vivo studies. -
Carbonic Anhydrase Inhibitor
AHR-15010 is a potent carbonic anhydrase inhibitor with an IC50 value of 0.13 μM. This compound exhibits anti-arthritic activity, making it a valuable tool for research on arthritis and related inflammatory conditions. Its ability to inhibit carbonic anhydrase opens avenues for studying therapeutic strategies in managing arthritis. -
Carbonic Anhydrase Inhibitor
hCAIX-IN-11 is a selective inhibitor of carbonic anhydrase IX (hCA IX) and XII (hCA XII), demonstrating Ki values of 32.7 nM and 623.5 nM, respectively. hCA IX and hCA XII are transmembrane isoforms that serve as biomarkers for various tumors, making them critical targets for cancer research. In addition to its role in tumor biology, hCA XII is involved in regulating acid-base homeostasis in both normal and cancerous cells, supporting its relevance in studies of metabolic regulation and tumor microenvironments. -
Carbonic Anhydrase Inhibitor
L-693612 is a potent, orally active carbonic anhydrase inhibitor. It effectively modulates bicarbonate and pH levels, making it a valuable tool for research into metabolic and respiratory disorders. This compound supports investigations into the therapeutic potential of carbonic anhydrase inhibition in various biological contexts. -
Carbonic Anhydrase Inhibitor
hCAII-IN-9 is a potent inhibitor of carbonic anhydrases, specifically exhibiting IC50 values of 1.18 μM for hCA II, 0.17 μM for hCA IX, and 2.99 μM for hCA XII. This compound demonstrates significant potential for research applications related to the modulation of carbonic anhydrase activity in various physiological and pathological conditions. Notably, hCAII-IN-9 does not exhibit permeability across the blood-brain barrier, making it suitable for studies focused on peripheral rather than central effects. -
Carbonic Anhydrase II Inhibitor
Carbonic Anhydrase Inhibitor 3 is a potent inhibitor of Carbonic Anhydrase II. This compound effectively reduces intraocular pressure, making it a valuable tool in the study of glaucoma and related ocular conditions. Its role in modulating intraocular pressure offers insights into therapeutic strategies for managing glaucoma. -
Carbonic Anhydrase II Inhibitor
Brinzolamide hydrochloride is a selective inhibitor of carbonic anhydrase II with an IC50 of 3.2 nM. It effectively lowers intraocular pressure (IOP) by targeting ciliary carbonic anhydrase II, leading to a reduction in aqueous humor secretion. This compound is particularly valuable for research applications related to glaucoma and other ocular conditions. -
Carbonic anhydrase Inhibitor
Dichlorphenamide disodium is a specific inhibitor of carbonic anhydrase, which functions by reducing the secretion of aqueous humor in the eye. This compound is effective in lowering intraocular pressure and is primarily utilized in glaucoma research. Its role in studying carbonic anhydrase inhibition provides insights into therapeutic strategies for managing elevated intraocular pressure and related ocular conditions. -
Carbonic Anhydrase Inhibitors
L-650719 is a potent carbonic anhydrase inhibitor, exhibiting a Ki value of 10 nM for carbonic anhydrase II (CA II). This compound has demonstrated significant efficacy in reducing intraocular pressure in rabbit models, highlighting its potential for therapeutic application. L-650719 is suitable for research focused on glaucoma and related ocular conditions. -
Carbonic Anhydrase Inhibitor
Carbonic Anhydrase Inhibitor 11 is a selective inhibitor targeting carbonic anhydrases, particularly exhibiting Ki values of 40 nM for CA II, 39 nM for CA IX, and 200 nM for CA XII. This compound demonstrates potential biological activity in modulating pH regulation and ion transport. It is valuable for research applications related to cancer, glaucoma, and other conditions where carbonic anhydrase plays a critical role in pathology. -
Carbonic Anhydrase Inhibitor
Carbonic anhydrase inhibitor 10 is a highly selective inhibitor of human carbonic anhydrase IX (hCA IX), with a Ki value of 6.2 nM. This compound demonstrates significant anti-proliferative activity in the MCF-7 cancer cell line, exhibiting an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 is suitable for applications in cancer research, particularly in studies investigating the role of hCA IX in tumorigenesis and malignancy. -
Carbonic Anhydrase Inhibitor
Carbonic Anhydrase Inhibitor 13 is a potent inhibitor of carbonic anhydrase (CA), characterized by its 3-methylthiazolo[3,2-a]benzimidazole moiety linked to a zinc-coordinating benzenesulfonamide via a ureido linkage. This compound demonstrates significant inhibition of carbonic anhydrase activity, making it a valuable tool for investigating the role of CA in various physiological processes. Its applications extend to studies in cancer, glaucoma, and metabolic disorders, where modulation of CA activity may provide therapeutic insights. -
Carbonic Anhydrases Inhibitor
Antibacterial agent 167 is a potent inhibitor of pathogenic bacterial carbonic anhydrases. It demonstrates significant antibacterial activity against Neisseria gonorrhoeae strains, effectively inhibiting growth at concentrations between 16 and 64 µg/mL. This compound serves as a valuable tool for research into antibacterial mechanisms and the development of new therapeutic strategies against resistant bacterial infections. -
Carbonic Anhydrase Inhibitor
L-693612 hydrochloride is a potent inhibitor of carbonic anhydrase, demonstrating both oral and topical bioactivity. Its primary mechanism involves the inhibition of carbonic anhydrase enzymes, which play a critical role in regulating acid-base balance and fluid secretion. This compound is widely used in research applications targeting therapeutic areas such as glaucoma and edema, facilitating studies on the modulation of intraocular pressure and fluid management. -
Carbonic Anhydrase Inhibitor
HCAIX-IN-2 is a selective inhibitor of carbonic anhydrase, specifically targeting isoforms hCA IX and hCA XII with Ki values of 24.6 nM and 45.3 nM, respectively. This compound exhibits significant biological activity in modulating carbonic anhydrase activity, making it a valuable tool in cancer research and therapeutic development. Its inhibitory effects may provide insights into the role of carbonic anhydrases in tumor progression and offer potential avenues for treatment strategies. -
Carbonic Anhydrase Inhibitor
O-Desmethyl Brinzolamide hydrochloride is a potent carbonic anhydrase inhibitor, demonstrating a Kd of 0.136 nM for carbonic anhydrase II and an IC50 of 165 nM for carbonic anhydrase IV. This active metabolite of Brinzolamide is essential for research focused on the regulation of bicarbonate ions and pH homeostasis in various biological systems. It holds potential applications in studying conditions driven by abnormal carbonic anhydrase activity, including glaucoma and other metabolic disorders. -
Carbonic Anhydrase Inhibitor
Disulfamide is a potent carbonic anhydrase inhibitor with an IC50 value of 0.07 μM. By inhibiting carbonic anhydrase, Disulfamide disrupts the reabsorption of sodium and bicarbonate in the proximal tubule, leading to increased diuresis. This compound is valuable for research applications focusing on renal physiology and electrolyte balance. -
Carbonic Anhydrase Inhibitor
Clofenamide is a potent inhibitor of carbonic anhydrase (CA), an enzyme involved in maintaining acid-base balance and fluid homeostasis. This compound displays significant diuretic activity, making it valuable in research related to renal function and fluid regulation. Clofenamide is utilized in studies investigating the role of carbonic anhydrase in various physiological and pathological conditions. -
Carbonic Anhydrase Inhibitor
(Rac)-Sezolamide hydrochloride is a potent inhibitor of carbonic anhydrase, with a Ki value of 12.0 nM. This compound effectively lowers intraocular pressure (IOP), making it valuable for research into glaucoma and related ocular conditions. Its mechanism of action provides a useful tool for investigating the physiological and pharmacological pathways involved in eye health and disease. -
Human Carbonic Anhydrase Inhibitors
hCAI/II/XII-IN-1 is a potent inhibitor of human carbonic anhydrases I, II, and XII, exhibiting Ki values of 78.5 nM, 9.1 nM, 605 nM, 7.7 nM, and 3.7 nM for each isoform respectively. This compound demonstrates significant biological activity that can be leveraged in research applications targeting metabolic regulation, pH balance, and various diseases such as glaucoma and cancer. Its specificity and efficacy make it a valuable tool for investigating the role of carbonic anhydrases in physiological and pathological processes. -
Carbonic Anhydrase Inhibitor
Carbonic Anhydrase Inhibitor 12 is a selective inhibitor of carbonic anhydrase II (CA II), exhibiting a Ki value of 1.72 nM, and also demonstrating inhibitory activity against carbonic anhydrase I (CA I) with a Ki of 271 nM. This compound displays significant anticancer activity across various cancer cell lines, making it a valuable tool for cancer research and therapeutic development. Its ability to selectively target carbonic anhydrases influences pH regulation and may contribute to tumor growth modulation. -
Carbonic Anhydrase Inhibitor
Carbonic Anhydrase Inhibitor 9 is a selective inhibitor of carbonic anhydrases II and IX, exhibiting Ki values of 56.4 nM and 56.9 nM, respectively. This compound has demonstrated significant antiproliferative activity, making it a valuable tool for studying the role of carbonic anhydrases in cancer research and cellular metabolism. It serves as a potential therapeutic agent in conditions where modulation of carbonic anhydrase activity is desired. -
Carbonic Anhydrase Inhibitor
Carbonic Anhydrase Inhibitor 7 is a highly effective inhibitor of human carbonic anhydrase enzymes, with inhibition constants (Kis) of 6.5 nM for hCA IX, 7.1 nM for hCA II, 72.1 nM for hCA XII, and 255.8 nM for hCA I. This compound exhibits potent biological activity, making it a valuable tool for investigating the role of carbonic anhydrases in various physiological and pathological processes. It is particularly useful in cancer research and related fields where hCA IX is implicated. -
Carbonic Anhydrase Inhibitor
Sezolamide hydrochloride is a potent inhibitor of the enzyme carbonic anhydrase, primarily utilized in the context of ocular research. This compound effectively reduces intraocular pressure, making it valuable for studies related to glaucoma and other conditions affecting eye health. Sezolamide hydrochloride is instrumental in investigating the physiological mechanisms and therapeutic strategies for managing elevated ocular pressure. -
Carbonic Anhydrase 2 Inhibitor
GV2-20 is a potent inhibitor of Carbonic Anhydrase 2, demonstrating significant antiproliferative effects in chronic myeloid leukemia (CML) cells. This compound is valuable for research applications aimed at understanding the role of carbonic anhydrases in cancer biology and exploring potential therapeutic strategies for CML. Its selective inhibition may provide insights into cellular metabolism and proliferation mechanisms associated with cancer progression.
