hca ii

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.

BChE/hCA II-IN-1 (Compound 20) is a dual inhibitor of butyrylcholinesterase (BChE) and human carbonic anhydrase II (hCA II), with IC50 values of 76.50 μM for BChE and 10.69 μM for hCA II. It is applicable in research on neurodegenerative diseases like Alzheimer's and conditions such as glaucoma.

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.

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

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.

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.

hCA-I/hCA-II-IN-1 (Compound P4) is a potent dual inhibitor of human carbonic anhydrase I (hCA-I) and human carbonic anhydrase II (hCA-II), with Ki values of 0.22 μM and 0.33 μM respectively. hCA-I/hCA-II-IN-1 is useful for research into diseases related to CA enzymes, including glaucoma, hypertension, and ulcers.

hCA-I/hCA-II-IN-2 (compound 5 k) is a potent inhibitor of human carbonic anhydrase I (hCA-I) and II (hCA-II), with IC50 values of 89.25 nM and 54.50 nM, respectively, for hCA I and hCA II.

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].

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-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].

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).

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.

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].

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].

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].

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].

hCAII/IX-IN-1 (compound 4o) is a potent inhibitor of hCAII and hCAIX, with Ki values of 7.4 nM and 7.0 nM, respectively. It plays a significant role in cancer research.

hCAII/XII-IN-1 (compound 4l) is a potent inhibitor of hCAXII and hCAII, with Ki values of 8.4 nM and 9.4 nM, respectively. It plays a significant role in cancer research.

hCAII Degrader 11 is a potent human carbonic anhydrase II (hCAII) degrader.

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.

hCAII-IN-1 (compound 7f) is a selective, potent inhibitor of carbonic anhydrase (CA II/IX) with Ki values of 1.2 nM and 113.6 nM, respectively, demonstrating investigational potential for cancer.