hca 4

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.

hCA VEGFR-2-IN-4 (compound 15b), an indolinylbenzenesulfonamide, serves as a potential dual inhibitor targeting cancer-related human carbonic anhydrases hCA IX XII and vascular endothelial growth factor receptor 2 (VEGFR-2). It exhibits an IC50 value of 0.811 µM against VEGFR-2 and shows high affinity for hCAs, with inhibition constants (Ki) of 3.8 nM for hCA XII, 6.2 nM for hCA IX, 19.8 nM for hCA II, and 35.5 nM for hCA I. Additionally, the compound demonstrates antiproliferative effects on breast cancer cells overexpressing VEGFR-2 [1].

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.

hCAI II-IN-4 (compound 6d) is a potent inhibitor of both hCA I and hCA II enzymes, with Ki values of 16.95 nM and 15.22 nM, respectively. It also inhibits hCA IX with a Ki value of 27.04 nM, exhibits anti-hypoxia properties, and maintains low toxicity. This compound is suitable for investigating acute mountain sickness (AMS) in research studies [1].

Carbonic anhydrase inhibitor 4 is a photoprobe that inhibits the activity of carbonic anhydrase. It specifically targets human carbonic anhydrases, including hCA I-XIV, with K i values ranging from 640-1166 nM [1].

hCAII-IN-4 (Compound 12j) is a potent inhibitor of human carbonic anhydrase II (hCA II) with an IC50 of 7.78 μM, and also inhibits β-glucuronidase with an IC50 of 773.9 μM [1].

compound EMAC10101d, bearing a 2,4-dichorophenyl substituent in position 4 of the dihydrothiazole ring, was the most potent and selective toward hCA II with an inhibitory activity in the low nanomolar range.

4-Acetylphenylboronic acid acts as an effective inhibitor targeting carbonic anhydrase II (CAII), displaying inhibitory concentrations (IC50) of 246 μM for bovine CAII (bCA II) and 281.40 μM for human CAII (hCA II).

Zonisamide-d4 is a deuterated compound of Zonisamide. Zonisamide has a CAS number of 68291-97-4. Zonisamide, 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.