hca-ii

hCA XII II IX-IN-1 is a potent inhibitor of human carbonic anhydrase (hCA), acting on hCA I (IC50: 2.6 μM), hCA II (IC50: 0.004 μM), hCA IX (IC50: 0.005 μM), and hCA XII (IC50: 0.001 μM). hCA XII II IX-IN-1 exhibited anticancer effects.

AChE hCA I II-IN-1 (Compound 6) is a potent AChE Hca inhibitor with IC50 values of 22.21, 60.79, and 66.64 nM for AChE, Hca Ⅰ, and Hca Ⅱ. AChE hCA I II-IN-1 can be used in glaucoma, Alzheimer's disease, and diabetes research[1].

DPP IV hCA II-IN-1 is a potent, selective inhibitor of dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA), exhibiting an IC50 of 0.049 μM for DPP IV and K_i values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively [1].

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.

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.

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.

Carbonic anhydrase inhibitor 6 is a potent human carbonic anhydrase (hCA) inhibitor that inhibits hCA IX, hCA II, hCA XII, and hCA I. It is used in the study of diseases caused by abnormalities in carbonic anhydrase.

Benzolamide (CL 11366) inhibits carbonic anhydrase effectively and low-threshold calcium currents in hippocampal pyramidal neurons.

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.

AChE-IN-20 is a potent inhibitor of AChE (IC50: 397.32 nM, Ki: 335.76 nM). AChE-IN-20 inhibits hCA-I (IC50: 84.14 nM, Ki: 97,86 nM), hCA-II (IC50: 69.24 nM, Ki: 76.23 nM) and α GLY (IC50: 52.08 nM, Ki: 57.93 nM).

hCAII-IN-2 is a cytoplasmic human carbonic anhydrase (hCA) inhibitor that acts on hCA I (Ki: 261.4 nM), hCA II (Ki: 3.8 nM), hCA IX (Ki: 19.6 nM) and hCA XII (Ki: 45.2 nM).

Compound 6f, also known as hCA IX-IN-1, is a human carbonic anhydrase (hCA) inhibitor that exhibits varying inhibitory effectiveness across different hCA isoforms, with K i values of 331.4 nM for hCA I, 28.4 nM for hCA II, 9.4 nM for hCA IX, and 17.8 nM for hCA XII. It is notable for its anticancer activity [1].

hCAII-IN-3 (Compound 16) is an inhibitor of human carbonic anhydrase (hCA) with high affinity for hCA I, hCA II, hCA IX, and hCA XII, exhibiting Ki values of 403.8 nM, 5.1 nM, 10.2 nM, and 5.2 nM, respectively. Notably, hCA IX-IN-2 demonstrates anticancer activity [1].

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

Human carbonic anhydrase II-IN-1 (Compound S-13) is a potent human carbonic anhydrase II (hCA II) inhibitor. Human carbonic anhydrase II-IN-1 shows Kis of 4.4 nM, 9.2 nM, 480.2 nM and 14.7 nM for hCA II, I, IV and IX, respectively. Human carbonic anhydrase II-IN-1 can be used for glaucoma research.

Compound 8g (hCA/VEGFR-2-IN-2) is an indolinonylbenzenesulfonamide identified as a potential dual inhibitor targeting cancer-associated isozymes hCA IX/XII and the angiogenic receptor VEGFR-2. It demonstrates VEGFR-2 inhibition with an IC50 of 204 nM and high affinity for hCAs, exhibiting Kis of 3.6 nM for hCA IX, 16.1 nM for hCA II, 16.7 nM for hCA XII, and 75.3 nM for hCA I. Furthermore, compound 8g exhibits antiproliferative effects on breast cancer cells overexpressing VEGFR-2 [1].

hA2A/hCA XII modulator 1 is a potent antagonist of the hA2A adenosine receptor (hA2AAR), a triazolopyrazine that acts on hA2AAR (Ki: 6.4 nM), hA1AR (Ki: 4.819 μM), and hA3AR (Ki>30 μM). hA2A/hCA XII modulator 1 Also a potent inhibitor of human carbonic anhydrase XII (hCA XII), capable of acting on hCA XII (Ki: 6.2 nM), hCA II (Ki: 46 nM), hCA IX (Ki: 466 nM) and hCA I (Ki: 8.351 μM). hA2A/hCA XII modulator 1 exhibits potential for cancer research.

Fluorometholone Acetate (Oxylone acetate) is a synthetic corticosteroid, used in the treatment of steroid responsive inflammatory conditions of the eye.

hCAI II-IN-3 (compound 5b) is a highly effective dual inhibitor of hCA I II enzymes, exhibiting Ki values of 51.25, 13.15, and 42.18 nM for hCA I, hCA II, and hCA Ⅸ, respectively. It demonstrates anti-hypoxic properties against acute mountain sickness (AMS) and exhibits low cellular activity [1].

Carbonic anhydrase inhibitor 9 is a potent inhibitor of carbonic anhydrase (CA), targeting hCA II (Ki: 56.4 nM) and IX (Ki: 56.9 nM), and exhibits antiproliferative effects.

Human carbonic anhydrase II-IN-24 (Compound R-13) is a potent human carbonic anhydrase (hCA) inhibitor. Human carbonic anhydrase II-IN-24 shows K i s of 60.7, 320.7, 2298, and 35.2 nM for hCA I, II, IV and IX, respectively.

hCA I-IN-1 is a human carbonic anhydrase I (hCA I) inhibitor that acts on hCA I (Ki: 38.3 nM), hCA II (Ki: 716.4 nM), hCAIX (Ki: 940.1 nM) and hCAXII (Ki: 192.8 nM).

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].

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].

Carbonic anhydrase inhibitor 8 (compound R-13) is a potent human carbonic anhydrase (hCA) with K i values of 60.7 nM, 320.7 nM, and 2298 nM for hCA I, hCA II, and hCA IV, respectively.

CDK2-IN-12 (compound 10b) is a potent inhibitor of CDK2 (IC50: 11.6 μM) and exhibits inhibition of hCA subtypes I, II, IX, and XII with KI values of 3534, 638.4, 44.3, and 48.8 nM, respectively. Additionally, CDK2-IN-12 shows anti-cancer effects.

hCAI II-IN-6 is a selective and orally active inhibitor of human carbonic anhydrase (CA). hCAI II-IN-6 inhibited hCA I, hCA II, hCA VII, and hCA XII with Ki values of 220, 4.9, 6.5, and ＞50,000 nM. hCAI II-IN-6 showed anticonvulsant activity in vivo. hCAI II-IN-6 can be used to study epilepsy. hCAI II-IN-6 showed anticonvulsant activity in vivo. hCAI II-IN-6 can be used to study epilepsy.

hCAIX XII-IN-5 (Coumarin 9a) is an inhibitor of carbonic anhydrase (CA) with excellent selectivity for hCA IX XII, displaying Kis of 93.3 nM and 85.7 nM over hCA I and hCA II, respectively. It exhibits anti-proliferative activities in cancer cells, delaying the cell cycle and inducing apoptosis [1].

hCAXII-IN-2 (compound 5i) is a potent inhibitor of human carbonic anhydrase XII (hCA XII) with a Ki of 84.2 nM and hCA IX with a Ki of 268.5 nM, exhibiting low activity against hCA I and hCA II.

β-Glucuronidase hCAII-IN-2 (Compound 12e) effectively inhibits β-glucuronidase and human Carbonic Anhydrase II (hCA II) with IC50 values of 440.1 μM and 4.91 μM, respectively [1].

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

hCA VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide with potential as a dual inhibitor of cancer-associated hCA IX XII and VEGFR-2. It inhibits VEGFR-2 with an IC50 of 358 nM and exhibits high affinity for hCAs, with Ki values of 4.2 nM for hCA IX, 22.9 nM for hCA II, 25.1 nM for hCA I, and 28.0 nM for hCA XII. Furthermore, it demonstrates specific antiproliferative activity against breast cancer cells that overexpress VEGFR-2 [1].

β-Glucuronidase/hCAII-IN-2 is a potent inhibitor of β-glucuronidase and hCA II, and their IC50 values were 670.7 μM and 21.77 μM, respectively.

hCAI/II-IN-5 is a potent inhibitor of hCA I and hCA II (human carbonic anhydrase isozymes I and II), with IC50 values of 37.88 and 45.23 nM, respectively. hCAI/II-IN-5 also inhibits α-Glycosidase (IC50: 48.98 nM) and AChE (IC50: 420.14 nM). nM). hCAI/II-IN-5 can be used in the study of diabetes, heart failure, Alzheimer's disease, ulcers, epilepsy and many other diseases.

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].

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].

hCA I-IN-2 (Compound 6d) is a selective inhibitor of human carbonic anhydrase I (hCA I) with inhibition constants (Ki) as follows: 18.8 nM for hCA I, 375.1 nM for hCA II, 1721 nM for hCAIX, and 283.9 nM for hCAXII.

hCAIX/XII-IN-6, an orally active carbonic anhydrase (CA) inhibitor, targets human CA isoforms hCA I, II, IV, IX, and XII with inhibition constants (K i) of 6697 nM, 2950 nM, 4093 nM, 4.1 nM, and 7.7 nM, respectively. This compound is utilized in rheumatoid arthritis (RA) research.

Compound R-13, also known as hCAII-IN-7, is a powerful inhibitor of human carbonic anhydrase (hCA), exhibiting inhibition constants (Ki) of 60.7 nM for hCA I, 320.7 nM for hCA II, 2298 nM for hCA IV, and 35.2 nM for hCA IX, respectively [1].

Phenylsulfamide (Compound 10), acting as an inhibitor of human carbonic anhydrase-II (hCA-II), exhibits a dissociation constant (Kd) of 45.50 μM and an inhibition constant (Ki) of 79.60 μM [1].

Carbonic anhydrase inhibitor 7 is a potent inhibitor of human carbonic anhydrase (hCA), acting on hCA IX (Ki: 6.5 nM), hCA II (Ki: 7.1 nM), hCA XII (Ki: 72.1 nM) and hCA I (Ki: 255.8 nM).

hCA Wnt β-catenin-IN-1 (Compd 15) is an inhibitor selectively targeting hCA isoforms II, IX, and XII, with K i values of 33.6, 24.1, and 6.8 nM, respectively. It also attenuates P-gp activity, disrupts the Wnt β-catenin signaling pathway, and compromises the viability of cancer cells, specifically against the NCI ADR-RES DOX-resistant cell line [1].

α-Glycosidase-IN-1 (compound MZ7) is a potent inhibitor of α-GLY (α-glycosidase) with an IC50 of 44.72 nM and a Ki of 44.74 nM. It also inhibits human carbonic anhydrase isozymes I (hCA I) and II (hCA II) with IC50 values of 104.87 nM and 100.04 nM, respectively, and acetylcholine esterase (AChE) with an IC50 value of 654.87 nM. α-Glycosidase-IN-1 is applicable in the study of diabetes, Alzheimer's disease, ulcers, heart failure, epilepsy, and various other diseases.

hCAII-IN-5 (compound 12h) is a potent and selective inhibitor of human carbonic anhydrase II (hCA II) with an inhibition constant (IC50) of 4.55 µM [1].

hCA IX-IN-1 (Compound 6f) is a human carbonic anhydrase ( hCA ) inhibitor with K i values of 331.4, 28.4, 9.4 and 17.8 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-1 shows anticancer activity [1].

hCAI II-IN-1 (Compound 3h) is a human carbonic anhydrase I and II (hCA I II) inhibitor, with an IC50 value of 0.047 μM for hCA I and 0.024 μM for hCA II.

Carbonic anhydrase inhibitor 14 (Compound 8b) is a potent CA inhibitor, exhibiting K i values of 1203, 99.7, 9.4, and 27.7 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. Additionally, it effectively inhibits CDK2 with an IC 50 of 20.3 μM and demonstrates significant antitumor activity [1].

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (40 mg/kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

Zonisamide sodium is a 1,2 benzisoxazole derivative. It is the first agent of this chemical class to be developed as an antiepileptic drug.