ca-ii

Dorzolamide hydrochloride (MK507 hydrochloride) is the hydrochloride salt form of dorzolamide, an inhibitor of carbonic anhydrase, a zinc-containing enzyme that catalyzes the rapid conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. Distributed throughout many cells and tissues, various carbonic anhydrases play important roles in mineral and metabolic homeostasis.

U-104 (NSC-213841) is an effective carbonic anhydrase (CA) inhibitor for CA IX( Ki=45.1 nM) and CA XII(Ki=4.5 nM).

Methazolamide (CL 8490) is a carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.

Brinzolamide (AL-4862) is a Carbonic Anhydrase Inhibitor. Its mechanism of action involves inhibiting the enzyme Carbonic Anhydrase.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Compound CDy9 is a highly selective inhibitor of carbonic anhydrase (CA) with an IC50 value of 0.18 μM for hCA II.

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.

hCAII-IN-9 is a potent carbonic anhydrase inhibitor with IC50 values of 1.18 μM for hCA II, 0.17 μM for hCA IX, and 2.99 μM for hCA XII. It is not blood-brain barrier permeable.

PNU-159682, a metabolite of anthracycline nemorubicin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity.

hBChE-IN-4 (compound 40) serves as an effective activator for hCA and an inhibitor for BChE. It demonstrates affinity for various hCA subtypes with affinity constants (KA) of 266 nM for hCA I, 76.9 nM for hCA II, 918 nM for hCA IV, 893 nM for hCA VB, and 98.0 nM for hCA VII. Inhibition concentrations (IC50) for eeAChE and eqBChE are recorded at 72.1 nM and 4.2 nM, respectively. hBChE-IN-4 is non-cytotoxic and has demonstrated potential cognitive enhancement effects. It holds potential for research in neurodegenerative and other neuropsychiatric disorders.

CAⅡ-IN-1 (compound 2i) is an inhibitor of the CA Ⅱ isozyme, exhibiting an IC50 of 0.44 µM. This compound is utilized in metabolic research.

hCA I-IN-4 (Compound 14) is an inhibitor of carbonic anhydrase and cholinesterase, effectively inhibiting hCA I, hCA II, AChE, and BChE with Ki values of 29.94 nM, 17.72 nM, 21.21 nM, and 7.65 nM, respectively. It also demonstrates cytotoxicity in BT-549 cells, with an IC50 of 16.59 μM.

AChE/hCA I-IN-1 (Compound L3) is an inhibitor of acetylcholinesterase (AChE) and carbonic anhydrase (CA), effectively inhibiting AChE, hCA I, and hCA II with IC50 values of 302 nM, 265 nM, and 283 nM, respectively.

hCAI/II-IN-10 (Compound 5d) is an inhibitor of human carbonic anhydrase I and II (hCA I and hCA II), with IC50 values of 4.32 nM and 3.89 nM, respectively.

BChE-IN-38 (compound 13) is a potent BChE inhibitor, with Ki values of 62.05, 28.78, 14.09, and 1.15 nM for hCAI, hCAII, AChE, and BChE, respectively. BChE-IN-38 also demonstrates cytotoxic activity.

hCAII/XII-IN-1 (compound 4l) is a potent inhibitor of hCAXII and hCAII, with Ki values of 8.4 nM and 9.4 nM, respectively. It plays a significant role in cancer research.

CAIX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. It exhibits anticancer activity by inhibiting the growth of MCF-7 breast cancer cells (IC50 of 22.33 μM) and mouse fibroblast cell line 3T3, where cell viability is reduced to below 40% at a concentration of 100 μM. This compound is applicable for research in the field of cancer treatment.

CAIX/CAXII-IN-4 (Compound 7h) is an inhibitor of carbonic anhydrase (CA) that binds to CAIX, CA XII, and CAII with Ki values of 1.324 μM, 0.435 μM, and 3.035 μM, respectively. This compound exhibits broad-spectrum anti-tumor activity and inhibits the proliferation of central nervous system tumor cells U251, with a GI50 of 0.361 μM.

hCAIX/XII-IN-9 (compound 8) is a potent inhibitor of carbonic anhydrase (CA), with Ki values of 1658 nM for hCA I, 184.8 nM for hCA II, 8.9 nM for hCA IX, and 64.8 nM for hCA XII.

Carbonic anhydrase/AChE-IN-1 (compound 16) is an inhibitor of carbonic anhydrase and AChE, with Ki values of 24.42 nM for hCA I, 19.95 nM for hCA II, and 5.07 nM for AChE.

hCAII-IN-10 (compound 11d) is an inhibitor of hCAII with IC50 values of 14 nM for hCAII and 29.2 μM for hCAI. It demonstrates inhibitory effects on HT-29 cells with an IC50 of 74 μM and is effective in reducing intraocular pressure in a rabbit model of glaucoma.

Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor targeting Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib. It exhibits anti-inflammatory and analgesic properties. The IC50 values for COX-1 and COX-2 are 10.4 μM and 50 nM, respectively. The Ki values for binding to various Carbonic Anhydrase isoforms are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII).

Anti-inflammatory agent 68 (compound 7b) is a dual inhibitor that targets Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib, exhibiting anti-inflammatory and analgesic properties. The IC50 values of Anti-inflammatory agent 68 for COX-1 and COX-2 are 12.6 μM and 60 nM, respectively. It binds to different Carbonic Anhydrase isoforms with Ki values of 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII).

hCAXII-IN-9 (Compound 3I) is a selective hCAXII inhibitor with Ki values of 28 nM for hCAXII, 7192.6 nM for hCAI, 188.6 nM for hCAII, and greater than 100000 nM for hCAIX. This compound may be utilized in anti-tumor research.