CAXII-IN-1 (Compound 17) is a selective CA XII inhibitor with Ki values of 3.8 nM and 56.0 nM against hCA XII and hCA IX, respectively. CAXII-IN-1 shows antitumor activity[1].
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines[1].
Benzenesulphonamide (compound 1) is a potent carbonic anhydrase inhibitor. Benzenesulphonamide shows CA II inhibitory activity[1].
hCAXII-IN-5 (compound 6o) is a potent and selective hCAXII inhibitor with Ki values of >10000, >10000, 286.1, 1.0 nM for hCAI, hCAII, hCAIX and hCAXII, respectively[1].
hCA I-IN-2 (Compound 6d) is a selective human carbonic anhydrase I (hCA I) inhibitor with Ki values of 18.8, 375.1, 1721 and 283.9 nM against hCA I, hCA II, hCAIX and hCAXII, respectively[1].
CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity[1].
hCAII-IN-3 (compound 7e) is a potent and selective inhibitor of carbonic anhydrase (CA II/IX) with Kis of 124.2 and 30.5 nM, respectively. hCAII-IN-3 has the potential for the research of cancer diseases[1].
hCAIX/XII-IN-3 (compound 6q) is a potent and selective hCAIX and hCAXIIinhibitor with Ki values of >10000, >10000, 66.2, 4.4 nM for hCAI, hCAII, hCAIX and hCAXII, respectively[1].
Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX[1]. Diuretic effects[4].
Ethoxzolamide is a carbonic anhydrase inhibitor with Ki of 1 nM.
Acetazolamide sodium is the sodium salt of Acetazolamide. Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities[1][4][5][6].
Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with anIC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research[1][2].
Dorzolamide(L671152; MK507) is an anti-glaucoma agent, which is a carbonic anhydrase inhibitor.Target: carbonic anhydrase (CA)Dorzolamide is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent, and acts by decreasing the production of aqueous humour [1]. Glaucoma was induced in the right eye of adult Wistar rats by episcleral venous occlusion. One experimental group was administered dorzolamide 2%-timolol 0.5% combination eye drops, while the other experimental group was administered dorzolamide 2% eye drops. Control groups had surgery without drug administration. Drug application was initiated either 2 weeks before surgery (Group A), from the day of surgery (Group B), 2 weeks after surgery (Group C), or 4 weeks after surgery (Group D). RGCs were labeled by intratectal Fluorogold injections and counted from flat-mount preparations, and IOP was measured using Tonopen. Both dorzolamide-timolol combination and dorzolamide, when applied topically, significantly reduced IOP and improved RGC densities in experimental eyes when compared to control eyes. Earlier initiation, as well as longer duration of drug application, resulted in higher RGC densities [2].Clinical indications: Glaucoma; Ocular hypertensionFDA Approved Date: 1995Toxicity: Dizziness, headache, shortness of breath, slow heartbeat, severe asthma, cardiac arrest
Dimethylfraxetin is a Carbonic anhydrase inhibitor, with a Ki value of 0.0097 μM.
Fluorometholone acetate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester. Fluorometholone acetate potently inhibits carbonic anhydrase (CA) with IC50s of 2.18 μM and 17.5 μM for hCA-I and hCA-II, respectively. Fluorometholone acetate has anti-inflammatory effect and has the potential for external ocular inflammation research[1][2][3].
Acetazolamide D3 is deuterium labeled Acetazolamide, which is a potent carbonic anhydrase (CA) inhibitor.
Methyclothiazide is an orally active antihypertensive agent and a diuretic agent. Methyclothiazide leads to a reduction of the vascular response to the action of endogenous vasoconstricting stimuli, such as Norepinephrine (HY-13715). Methyclothiazide is against voltage-dependent Ca-channel (VDCC) activity in vitro[1][2][3].
Benzolamide (CL11366) is a potent carbonic anhydrase (CA) inhibitor, with Kis of 15 nM, 9 nM, 94 nM and 78 nM for hCA I, hCA II, EcoCAγ and VchCAγ, respectively. Benzolamide also inhibits CAS3, with a Ki of 54 nM. Benzolamide can be used for the research of glaucoma and seizures[1][2][3].
hCAIX-IN-7 (compound 6c) is a potent and selective hCAIX inhibitor with KIs of >10000, >10000, 43.0, 410.6 nM for hCAI, hCAII, hCAIV, hCAIX, respectively[1].
hCAIX-IN-5 (compound 6b) is a potent and selective hCAIX inhibitor with KIs of >10000, >10000, 130.7, 829.1 nM for hCAI, hCAII, hCAIV, hCAIX, respectively[1].
HCAIX-IN-1 (compound 21e) is a potent and selective HCAIX inhibitor with KIs of 694.9, 126.6, 3.3, 9.8 nM for hCA I, hCA II, hCA IX, hCA XII, respectively[1].
hCAI/II-IN-3 (compound 5b) is a potent dual hCA I/II inhibitor with Ki values of 51.25, 13.15 and 42.18 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-3 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity[1].
Tioxolone, a metalloenzyme carbonic anhydrase I inhibitor, is an anti-acne preparation.Target: Carbonic Anhydrase Tioxolone is a metalloenzyme carbonic anhydrase I inhibitor with a Ki of 91 nM. Tioxolone lacks sulfonamide, sulfamate, or hydroxamate functional groups that are typically found in therapeutic carbonic anhydrase (CA) inhibitors, such as acetazolamide. Tioxolone is proposed to be a prodrug inhibitor that is cleaved via a CA II zinc-hydroxide mechanism known to catalyze the hydrolysis of esters. When tioxolone binds in the active site of CA II, it is cleaved and forms 4-mercaptobenzene-1,3-diol via the intermediate S-(2,4-thiophenyl) hydrogen thiocarbonate. The esterase cleavage product binds to the zinc active site via the thiol group and is therefore the active CA inhibitor, while the intermediate is located at the rim of the active-site cavity. From Wikipedia.