carbonic anhydrase

Compound 1e, also known as ALP Carbonic anhydrase-IN-1, is a dual inhibitor targeting both carbonic anhydrase (CA) isozymes II, IX, and XII, as well as alkaline phosphatase (ALP). It exhibits inhibitory IC50 values of 0.44 µM for CA-II, 1.61 µM for CA-IX, 0.51 µM for CA-XII, and 0.107 µM for ALP [1].

Carbonic Anhydrase Inhibitor 15 (Compound 8), with an inhibitory constant (K_i) of 8.5 nM for hCA II, exhibits analgesic effects [1].

Carbonic Anhydrase Inhibitor 12 is a potent inhibitor of CA II, with additional inhibitory activity against CA I, exhibiting K_i values of 1.72 nM for CA II and 271 nM for CA I. Moreover, it demonstrates significant anticancer activity across various cancer cell lines [1].

Enpp Carbonic anhydrase-IN-1 (compound 1e) is a potent inhibitor of Enpp and carbonic anhydrase, exhibiting IC50s of 1.36, 1.35, 3.00, 0.88, and 1.02 µM for NPP1, NPP2, NPP3, CA-II, and CA-IX respectively. Enpp Carbonic anhydrase-IN-1 also demonstrates selective antiproliferative activity for cancer cells.

Carbonic anhydrase is a ubiquitous, zinc-containing metalloenzyme found in both prokaryotes and eukaryotes. It catalyzes the reversible conversion of carbon dioxide to bicarbonate and protons and can be used for research in cancer, glaucoma, obesity, and epilepsy [1] [2].

Enpp Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.07, 0.74, 0.33, 0.68, respectively.Enpp Carbonic anhydrase-IN-2 induced apoptosis.Enpp Carbonic anhydrase-IN-2 has antiproliferative activity against cancer cells and low cytotoxicity against normal cells.

Acetazolamide (Diamox) is a Carbonic Anhydrase Inhibitor. The mechanism of action of acetazolamide is as a Carbonic Anhydrase Inhibitor. The chemical classification of acetazolamide is Sulfonamides.

Acetazolamide sodium (OT-302 sodium) is a potent carbonic anhydrase (CA)IX inhibitor with diuretic, antigonococcal, and antihypertensive activity and may be used for indications such as epilepsy, glaucoma, edema, and altitude sickness.

Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.

Compound 4d, known as hCA XII-IN-6, is a potent inhibitor of human carbonic anhydrase XII (hCA XII) with a Ki value of 84.2 nM and exhibits anti-proliferative effects, making it useful in cancer research [1].

Compound 3e (hCAIX XII-IN-7) is a potent inhibitor of human carbonic anhydrase (hCA) isozymes IX and XII, displaying inhibitory constants (Kis) of 503.7 nM for hCA IX and 59 nM for hCA XII, while also showing activity against hCA I and II with Kis of 3.2 nM and 9.2 nM, respectively. It holds potential for research into hypoxic tumors [1].

hCAIX-IN-16 (Compound 12d), an inhibitor of hCA IX, exhibits inhibition constants (K i) of 190.0 nM for hCA IX and 187.9 nM for hCA XII. It can arrest the cell cycle in the G0-G1 and S phases and induce apoptosis in MDA-MB-468 breast cancer cells. Demonstrating broad-spectrum anticancer activity, hCAIX-IN-16 is a potential tool for cancer research [1].

Compound 4H is a potent carbonic anhydrase inhibitor with an IC50 value of 0.033 μM [1].

WES-1 (Compound 8g), a carbonic anhydrase IX inhibitor (Ki: 55.9 μM), exhibits broad-spectrum antiproliferative activity against various cancer cell lines, including leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI-H460), colon cancer (HCT 116 and HCT-15), and melanoma (LOX IMVI) [1].

PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.

TSPO Carbonic Anhydrase Modulator 1 (Compound 3) acts as a dual modulator of mitochondrial translocator protein and carbonic anhydrase, with a TSPOKi of 1.340 μM and a CAVII KA of 10.7 μM. It enhances neurosteroid production, increases BDNF gene expression, and demonstrates neuroprotective activity.

Chlorothiazide (Diuril) is a thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE.

Bendroflumethiazide (Naturetin) is a thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810)

hCAIX-IN-15, a potent inhibitor of human carbonic anhydrase IX (hCA IX), has an inhibition constant (Ki) of 38.8 nM and exhibits broad-spectrum anticancer activity suitable for cancer research [1].

hCAIX VII-IN-1 is a selective inhibitor of human carbonic anhydrase isoforms VII and IX, displaying inhibitory activity against hCA I, II, IV, VII, and IX with respective K_i values of 336.2 nM, 185.8 nM, 1055 nM, 35.6 nM, and 28.0 nM. This compound is applicable in cancer and neurological disease research [1].

hCAIX XII-IN-8 (compound 3g) is a potent inhibitor of the human carbonic anhydrases (CAs) IX and XII, with inhibition constants (K i) of 8.5 nM for CA IX and 6.7 nM for CA XII. It demonstrates significant inhibitory efficacy particularly against tumor-associated, membrane-bound isoforms hCA IX and XII, while exhibiting high selectivity over the cytosolic isoforms hCA I and II [1].

hCAXII-IN-7 (compound 6e) functions as an inhibitor of human carbonic anhydrase XII (hCA XII), possesses blood-brain barrier (BBB) permeability, and promotes apoptosis in 786-0, SF-539, and HS 578 T cell lines [1].

hCA VEGFR-2-IN-1 (compound 13a) is a potent dual inhibitor targeting both Carbonic Anhydrase (CA) IX XII and Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), exhibiting Ki values of 4.7 nM for hCA XII and 8.3 nM for hCA IX, alongside an IC50 of 26.3 nM for VEGFR-2, and demonstrating anticancer activity [1].

(Iso)-Samixogrel shows activity against Carbonic anhydrase and Cyclooxygenase 2.