hca-i

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.

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).

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].

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.

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.

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).

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).

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].

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).

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.

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].

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.

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.

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].

Compound 1, known as Carbonic anhydrase inhibitor 16, acts as a dengue protease inhibitor and also inhibits carbonic anhydrase hCA I and hCA II, with inhibitory constants (K i) of 28.5 nM and 2.2 nM, respectively [1].

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

hCAIX-IN-21 (compound 16c) is an effective inhibitor of hCAIX, exhibiting KI values of 5.2 nM, 3.5 nM, 12.6 nM, and 13600 nM against hCAIX, hCA II, hCA XII, and hCA I, respectively. Moreover, it inhibits the enzymatic activity of tissue protease B.

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].

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].

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].

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.

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).

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.

hCAIX-IN-11 (Compound 5d) is a selective inhibitor of carbonic anhydrase IX and XII, exhibiting K_i values of 32.7 nM for hCA IX and 623.5 nM for hCA XII.

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].

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.

hCAI II-IN-7 (compound 1F) serves as a potent inhibitor of carbonic anhydrase (CA), exhibiting K i values of 23 nM and 44 nM for hCA-I and hCA-II, respectively, and a K i value of 20.57 µM for bovine CA [1].

hCAIX-IN-18 (compound 30), a potent inhibitor of the carbonic anhydrase enzyme family (CA), exhibits K i values of 3.5 nM for hCAI, 9.4 nM for hCAII, 43.0 nM for hCAIX, and 8.2 nM for hCAXII. This compound is applicable in cancer research [1].

hCAIX VII-IN-1 is a selective inhibitor of human carbonic anhydrase isoforms VII and IX, displaying inhibitory activity against hCA I, II, IV, VII, and IX with respective K_i values of 336.2 nM, 185.8 nM, 1055 nM, 35.6 nM, and 28.0 nM. This compound is applicable in cancer and neurological disease research [1].

hCAII-IN-6 (Compound S-13), a potent inhibitor of human carbonic anhydrase II (hCA II) with a K i of 4.4 nM, also exhibits inhibitory activity against other hCA isoforms, namely I, IV, and IX, with K i values of 9.2 nM, 480.2 nM, and 14.7 nM, respectively. It is utilized in glaucoma research [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].

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].

hCAIX XII-IN-8 (compound 3g) is a potent inhibitor of the human carbonic anhydrases (CAs) IX and XII, with inhibition constants (K i) of 8.5 nM for CA IX and 6.7 nM for CA XII. It demonstrates significant inhibitory efficacy particularly against tumor-associated, membrane-bound isoforms hCA IX and XII, while exhibiting high selectivity over the cytosolic isoforms hCA I and II [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-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].

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].

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].

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].

hCAIX-IN-19 is a sulfonamide inhibitor with an inhibition constant (KI) of 6.2 nM for hCAIX, exhibiting significant selectivity towards hCAIX over hCAI (hCA I/hCAIX = 117).

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.

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.

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.

hCA IX-IN-2 is a highly potent and selective inhibitor of hCA IX, with an inhibition constant (K I) of 32.1 nM, demonstrating significant anti-proliferative activity.