hca-i

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.

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].

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 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.

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.

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

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-13 functions as an inhibitor targeting specific human carbonic anhydrases (hCA) IX and XII, crucial in tumor-related processes. Demonstrating efficacy, this compound offers inhibitory K i values of 0.08 µM for IX and 0.06 µM for XII. Additionally, under hypoxic conditions, hCAIX XII-IN-13 enhances the effectiveness of Doxorubicin on MCF-7 cells by promoting G2 M phase cell cycle arrest and increasing apoptosis.

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.

AChE CA I-IN-1 (Compound 2g) acts as an inhibitor for both AChE and hCA I, with Ki values of 1.85 µM and 0.53 µM, respectively. It has shown potential applications in the research of Alzheimer's disease, glaucoma, and epilepsy.

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.

2,5-dimethyl Celecoxib is a derivative of celecoxib that does not inhibit COX-2 (IC50 = >100 μM).1 It does inhibit microsomal prostaglandin E synthase-1 (mPGES-1) in HeLa cells (IC50 = 15.6 μM) and reduces prostaglandin E2 production in HeLa, A549, and HCA-7 cells (IC50s = 0.64, 0.83, and 3.08 μM, respectively).2 It inhibits proliferation of drug-sensitive RPMI8226 and multidrug-resistant 8226 Dox40 multiple myeloma cells, as well as increases the rate of apoptosis when used at concentrations of 20 and 30 μM.3 2,5-dimethyl Celecoxib reduces the expression of survivin, cyclin A, cyclin B, MEK1, and MEK2 in 8226 Dox40 cells. The antiproliferative effect of 2,5-dimethyl celecoxib is independent of mPGES-1 inhibition.2References1. Zhu, J., Song, X., Lin, H.-P., et al. Using cyclooxygenase-2 inhibitors as molecular platforms to develop a new class of apoptosis-inducing agents. J. Natl. Cancer Inst. 94(23), 1745-1757 (2002).2. Wobst, I., Schiffmann, S., Birod, K., et al. Dimethylcelecoxib inhibits prostaglandin E2 production. Biochem. Pharmacol. 76(1), 62-69 (2008).3. Kardosh, A., Soriano, N., Liu, Y.-T., et al. Multitarget inhibition of drug-resistant multiple myeloma cell lines by dimethyl-celecoxib (DMC), a non-COX-2 inhibitory analog of celecoxib. Blood 106(13), 4330-4338 (2005). 2,5-dimethyl Celecoxib is a derivative of celecoxib that does not inhibit COX-2 (IC50 = >100 μM).1 It does inhibit microsomal prostaglandin E synthase-1 (mPGES-1) in HeLa cells (IC50 = 15.6 μM) and reduces prostaglandin E2 production in HeLa, A549, and HCA-7 cells (IC50s = 0.64, 0.83, and 3.08 μM, respectively).2 It inhibits proliferation of drug-sensitive RPMI8226 and multidrug-resistant 8226 Dox40 multiple myeloma cells, as well as increases the rate of apoptosis when used at concentrations of 20 and 30 μM.3 2,5-dimethyl Celecoxib reduces the expression of survivin, cyclin A, cyclin B, MEK1, and MEK2 in 8226 Dox40 cells. The antiproliferative effect of 2,5-dimethyl celecoxib is independent of mPGES-1 inhibition.2 References1. Zhu, J., Song, X., Lin, H.-P., et al. Using cyclooxygenase-2 inhibitors as molecular platforms to develop a new class of apoptosis-inducing agents. J. Natl. Cancer Inst. 94(23), 1745-1757 (2002).2. Wobst, I., Schiffmann, S., Birod, K., et al. Dimethylcelecoxib inhibits prostaglandin E2 production. Biochem. Pharmacol. 76(1), 62-69 (2008).3. Kardosh, A., Soriano, N., Liu, Y.-T., et al. Multitarget inhibition of drug-resistant multiple myeloma cell lines by dimethyl-celecoxib (DMC), a non-COX-2 inhibitory analog of celecoxib. Blood 106(13), 4330-4338 (2005).

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].

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].

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-2 (compound 2b) is a highly effective dual inhibitor of human carbonic anhydrase I and II (hCA I II), with Ki values of 40.97 nM for hCA I, 15.15 nM for hCA II, and 61.88 nM for hCA IX. With its anti-hypoxic properties, hCAI II-IN-2 demonstrates activity against acute mountain sickness (AMS) and exhibits low cellular activity [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].

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].

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 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].

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.

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.

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.