hcai

hCAIX-IN-5 was a selective hCAIX inhibitor, inhibiting hCAI, hCAII, hCAIV, and hCAIX with Ki values of >10000, >10000, 130.7, and 829.1 nM, respectively.

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

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.

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.

hCAI/II-IN-11 (compound 2c) is a carbonic anhydrase inhibitor with IC50 values of 12.56 μM and 13.02 μM for hCAI and hCA II, respectively. In addition, hCAI/II-IN-11 exhibits antioxidant and antibacterial properties.

hCAI/II-IN-8 (Compound 8) is a hydrazone derivative originating from 4-hydroxybenzaldehyde. It primarily inhibits human carbonic anhydrase isoenzymes I (hCA I) and II (hCA II) with IC50 values of 21.35 ± 0.39 nM for hCA I and 7.12 ± 0.12 nM for hCA II. It also exhibits inhibitory effects on AChE and BChE, with IC50 values of 46.27 ± 0.75 nM and 43.38 ± 0.83 nM, respectively.

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].

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.

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].

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.

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.

hCAI/II-IN-7 (compound 1F) is an effective carbonic anhydrase (CA) inhibitor with Ki values of 23 nM, 44 nM, and 21 μM for hCA-I, hCA-II, and bCA respectively.

hCAI/II/IV-IN-28(WAY-638358) is a potent carbonic anhydrase inhibitor with potential anticonvulsant activity.

hCAII/XII/XIV-IN-1 is an effective inhibitor of the human carbonic anhydrases hCAII, hCAXII and hCAXIV, with Ki values of 78.5 nM, 9.1 nM, 605 nM, 7.7 nM, and 3.7 nM for hCAI, hCAII, hCAIX, hCAXII, and hCAXIV, respectively.

hCAII-IN-8 is a highly selective inhibitor of carbonic anhydrase (CA) with an IC50 value of 0.18 μM for hCA II.

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.

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.

hCAIX-IN-7 (compound 6c) is a potent and selective inhibitor of the tumor-associated isoform hCAIX, with inhibition constants (KIs) of >10000 nM for hCAI and hCAII, 43.0 nM for hCAIV, and 410.6 nM for hCAIX [1].

hCAIX/XII-IN-2 (compound 6a) is a potent and selective inhibitor of hCAIX and hCAXII, with Ki values of >10000 nM for hCAI and hCAII, and 30.0 nM and 3.6 nM for hCAIX and hCAXII respectively [1].

hCAIX/XII-IN-3 (compound 6q) is a potent, selective inhibitor of hCAIX and hCAXII, with K i values of >10000 nM for hCAI and hCAII, and 66.2 nM and 4.4 nM for hCAIX and hCAXII, respectively.

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).

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/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.