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Carbonic anhydrase (CA) inhibitors block zinc enzymes that interconvert carbon dioxide and bicarbonate. The enzyme was purified from red blood cells in 1933 and shown to speed up the hydration of carbon dioxide. Humans express many CA isoforms, which regulate pH, ion transport, fluid secretion and respiration. CA IX, cloned in 1994 as a tumor-associated protein, is induced by hypoxia in many solid tumors. Most inhibitors are sulfonamides that bind the active-site zinc, from the parent benzenesulfonamide to dorzolamide, brinzolamide and diclofenamide. DTP348 is a CA IX inhibitor that is also described as a radiosensitizer. Indisulam, another sulfonamide, is also studied as a molecular glue that degrades RNA-binding motif protein 39 (RBM39).
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.
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CAIX/CAXII-IN-1 is a potent inhibitor of carbonic anhydrase IX (CAIX) and carbonic anhydrase XII (CAXII), demonstrating Ki values of 29.1 nM and 8.8 nM, respectively. This compound exhibits significant cytotoxicity against various cancer cell lines, including HepG-2, HCT-116, and MCF-7, with IC50 values of 1.78 μM, 1.94 μM, and 3.07 μM. Its selective action and efficacy make it a valuable tool for studying tumor biology and evaluating potential therapeutic strategies targeting CAIX/CAXII in cancer research.
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Synonyms: AL-4862 hydrochloride
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.
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Synonyms: Diclofenamide disodium
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.
hCAIX-IN-24 is a potent inhibitor of human carbonic anhydrase IX (hCA IX) with a KI value of 32.1 nM. This compound exhibits significant anti-proliferative activity, making it valuable for research in cancer biology, particularly in studying tumor growth and metastasis where hCA IX is often overexpressed. hCAIX-IN-24 serves as a critical tool for investigating the therapeutic potential of targeting hCA IX in cancer treatment strategies.
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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 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.
FC11409B is a ureido-sulfamate inhibitor of carbonic anhydrase IX (CAIX). This compound effectively suppresses the proliferation and migration of breast cancer cell lines under both hypoxic (0.5% O2) and normoxic (21% O2) conditions. Additionally, FC11409B inhibits the invasion of 3D spheroids derived from various breast cancer subtypes. Its potential applications make it a valuable tool for research focused on breast and ovarian cancers.
AChE/hCA I-IN-1 is a selective inhibitor of acetylcholinesterase (AChE) and human carbonic anhydrases (hCA I and hCA II). It demonstrates potent inhibition with IC50 values of 302 nM for AChE, 265 nM for hCA I, and 283 nM for hCA II. This compound is valuable for research applications exploring neurodegenerative disorders and the regulation of physiological pH balance.
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hCAI/II-IN-2 is a potent dual inhibitor of human carbonic anhydrases I and II, demonstrating Ki values of 40.97 nM, 15.15 nM, and 61.88 nM for hCA I, hCA II, and hCA IX, respectively. This compound exhibits anti-hypoxic activity, making it relevant for research in acute mountain sickness (AMS) and related conditions. Its effective inhibition of these carbonic anhydrases highlights its potential applications in understanding and treating hypoxia-related disorders.
AChE/hCA I/II-IN-1 is a potent inhibitor of acetylcholinesterase (AChE) and human carbonic anhydrases I and II (hCA I/II), demonstrating IC50 values of 22.21 nM for AChE, and 60.79 nM and 66.64 nM for hCA I and II, respectively. This compound is valuable for research applications related to glaucoma, Alzheimer’s disease, and diabetes, providing insights into the modulation of these critical enzymatic targets.
hCAI/II-IN-3 is a potent dual inhibitor of human carbonic anhydrases I and II, exhibiting Ki values of 51.25 nM for hCA I and 13.15 nM for hCA II, along with an affinity for hCA IX at 42.18 nM. This compound demonstrates significant anti-hypoxic activity, making it relevant for investigations into acute mountain sickness (AMS) and related hypoxic conditions. Its unique properties may facilitate research into therapeutic approaches for managing hypoxia-induced pathologies.
hCAIX-IN-14 is a potent inhibitor of human carbonic anhydrase IX (CA IX), exhibiting a Ki value of 134.8 nM. This compound is primarily used in cancer research, particularly in studies investigating tumor microenvironment regulation and therapeutic strategies targeting hypoxic tumors. Its ability to inhibit CA IX makes it a valuable tool for exploring the role of this enzyme in cancer progression and for developing novel anti-cancer therapies.
hCAIX-IN-7 is a selective inhibitor of human carbonic anhydrase IX (hCAIX), exhibiting remarkable potency with inhibition constants (KIs) of >10000 nM for hCAI and hCAII, 43.0 nM for hCAIV, and 410.6 nM for hCAIX. This compound is crucial for research applications focusing on tumor biology and hypoxia, as hCAIX is highly expressed in various cancer types. hCAIX-IN-7 serves as a valuable tool for investigating therapeutic strategies targeting hCAIX in cancer research.
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.
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hCAIX/XII-IN-4 is a selective inhibitor of the carbonic anhydrases IX (CAIX) and XII (CAXII), exhibiting Ki values of 4.5 nM and 23.6 nM for CAXII and CAIX respectively. This compound demonstrates significant inhibition of carbonic anhydrase activity, making it valuable for research into tumor biology and potential cancer therapies. Its high specificity may also enhance studies focused on the physiological roles of these enzymes in various pathophysiological conditions.
hCAI/II-IN-5 is a potent inhibitor of human carbonic anhydrase isoenzymes I and II, exhibiting IC50 values of 37.88 nM and 45.23 nM, respectively. Additionally, it demonstrates inhibitory activity against α-Glycosidase and acetylcholinesterase (AChE) with IC50 values of 48.98 nM and 420.14 nM. This compound is valuable for research applications in various diseases, including diabetes, Alzheimer's disease, heart failure, ulcers, and epilepsy.
hCAII-IN-5 is a potent and selective inhibitor of human carbonic anhydrase II (hCA II), exhibiting an IC50 value of 4.55 μM. This compound demonstrates significant biological activity in modulating hCA II activity, making it a valuable tool for research focused on enzymatic regulation and metabolic pathways. Its specificity for hCA II highlights its potential applications in studies related to cancer, glaucoma, and other disorders where carbonic anhydrase plays a critical role.
hCAIX-IN-5 is a selective inhibitor of human carbonic anhydrase IX (hCAIX) with a Ki value of 829.1 nM, demonstrating high potency against this target while showing minimal activity against hCAI and hCAII. This compound is valuable in research focused on cancer biology, particularly in studies investigating tumor microenvironments and hypoxia, where hCAIX is often upregulated. Its specificity makes hCAIX-IN-5 an important tool for elucidating the role of carbonic anhydrases in various cellular processes and therapeutic interventions.
hCAII-IN-6 is a potent inhibitor of human carbonic anhydrase II (hCA II), exhibiting a Ki of 4.4 nM. This compound also demonstrates inhibitory activity against additional hCA isoforms, including hCA I, hCA IV, and hCA IX, with Ki values of 9.2 nM, 480.2 nM, and 14.7 nM, respectively. hCAII-IN-6 is valuable for research into glaucoma, contributing to studies focused on intraocular pressure regulation and therapeutic interventions.
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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.
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.
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hCA I-IN-4 is an inhibitor of carbonic anhydrase (CA) and cholinesterase (ChE), demonstrating potent inhibitory activity against hCA I, hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) with Ki values of 29.94 nM, 17.72 nM, 21.21 nM, and 7.65 nM, respectively. This compound also exhibits cytotoxic effects in BT-549 cancer cells, with an IC50 value of 16.59 μM. hCA I-IN-4 is valuable for research involving enzyme regulation and cancer therapeutics.
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hCAXII-IN-3 is a selective inhibitor of human carbonic anhydrase XII (hCAXII), exhibiting a Ki value of 10.0 nM. This compound is valuable for research investigating the role of hCAXII in various physiological and pathological processes. It can be utilized in studies related to cancer biology, metabolic diseases, and other conditions where carbonic anhydrase activity is implicated.
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.
