Carbonic Anhydrase

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].

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

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].

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.

Sultiame is an inhibitor of carbonic anhydrase. Sultiame can be used in antiepileptic research.

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.

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.

Mafenide hydrochloride (4-Aminomethylbenzenesulfonamide hydrochloride) is a sulfonamide that inhibits the enzyme carbonic anhydrase and is used as topical anti-infective, especially in burn therapy.

Methocarbamol (AHR 85) is a centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm.

Orthanilamide (Orthanilamide) is a molecule containing the sulfonamide functional group attached to an aniline.

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.

Histone acetyltransferase p300 Inhibitor 4c is a 2-aminothiazole derivative. Histone acetyltransferase p300 Inhibitor 4c inhibited hCA I, hCA II, AChE and BChE with Ki values of 0.008 ± 0.001, 0.124 ± 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 µM. 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 μM.

Methyl 2,4-dihydroxybenzoate is a natural product.

2,3-dihydro-1H-indene-5-sulfonamide is Carbonic anhydrase 12 (human) inhibitor.

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

Benzthiazide (Lemazide) is used in the therapy of edema and hypertension. Like other thiazides, benzthiazide accelerates water loss from the body (diuretics). They inhibit Na+ Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

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)

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.

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

Dimethylfraxetin (6,7,8-Trimethoxycoumarin) is a Carbonic anhydrase inhibitor(Ki:0.0097 μM)

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].

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].