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Carbonicanhydraseinhibitor 1 (compound 7c) is a carbonicanhydrase IIinhibitor. Carbonicanhydraseinhibitor 3 reduces the intraocular pressure in glaucomatous rabbits .
Carbonicanhydraseinhibitor 3 (compound 11g) is a carbonicanhydrase IIinhibitor. Carbonicanhydraseinhibitor 3 reduces the intraocular pressure in glaucomatous rabbits .
Carbonicanhydraseinhibitor 12 is a potent CA IIinhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonicanhydraseinhibitor 12 has potent anticancer activity against different cancer cell lines .
Carbonicanhydraseinhibitor 4 is carbonicanhydrase photoprobe/inhibitor. Carbonicanhydraseinhibitor 4 is against human carbonicanhydrases (hCA I-XIV) with Ki values of 640-1166 nM .
Carbonicanhydraseinhibitor 15 (Compound 8) is a carbonicanhydraseinhibitor (Ki: 8.5 nM for hCA II). Carbonicanhydraseinhibitor 15 has analgesic effect .
Carbonicanhydraseinhibitor 11 (compound VI) is a potent, selective carbonicanhydraseinhibitor. Carbonicanhydraseinhibitor 11 shows Ki values of 40, 39, 200 and 900 nM against CA II, IX, and XII, respectively .
Carbonicanhydraseinhibitor 21 (Compound 5h) is a selective carbonicanhydrase (hCA IX)inhibitor, with a Ki of 15.1 nM, and is highly selective against other investigated isoform. Carbonicanhydraseinhibitor 21 can be used for anticancer research .
Carbonicanhydraseinhibitor 14 (Compound 8b) is a carbonicanhydrase (CA)inhibitor with Ki values of 1203, 99.7, 9.4 and 27.7 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonicanhydraseinhibitor 14 can also inhibitCDK2 with an IC50 of 20.3 μM. Carbonicanhydraseinhibitor 14 shows antitumor activity .
Carbonicanhydraseinhibitor 10 is a potent hCA IXinhibitor with a Ki value of 6.2 nM. Carbonicanhydraseinhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonicanhydraseinhibitor 10 can be used for cancer research .
Carbonicanhydraseinhibitor 9 is a potent carbonicanhydrase (CA)inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity .
Carbonicanhydraseinhibitor 18 (Compound 9) is a human carbonicanhydrase (hCA) isoform inhibitor, with Kis of 604.8, 333.6, 1.9 and 6.7 nM for hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonicanhydraseinhibitor 18 can be used for the research of cancer .
Carbonicanhydraseinhibitor 16 (compound 1) is a dengue protease inhibitor with inhibitory activity against carbonicanhydrasehCA I and hCA II (Ki: 28.5 nM, 2.2 nM) .
Carbonicanhydraseinhibitor 5 is a potent and selective human carbonicanhydrase (hCA)inhibitor with IC50s of 42.9, 47,6 and 6.7 nM for hCA II, hCA IX and hCA XII, respectively .
Carbonicanhydraseinhibitor 19 (compound 26a) inhibits the Glaucoma related isoforms hCA II and hCA XII with Kis of 9.4 nM and 6.7 nM, respectively. Carbonicanhydraseinhibitor 19 reveals an intraocular pressure (IOP) lowering effect .
Carbonicanhydraseinhibitor 8 (compound R-13), a benzyl-derivative, is a potent human carbonicanhydrase (hCA)inhibitor with Ki values of 60.7 nM, 320.7 nM, 2298 nM for hCA I, hCA II, hCA IV, respectively .
Carbonicanhydraseinhibitor 7 (compound 5b) is a potent inhibitor of human carbonicanhydrase (hCA), with Kis of 6.5 nM, 7.1 nM, 72.1 nM, and 255.8 nM for hCA IX, hCA II, hCA XII and hCA I, respectively .
Carbonicanhydraseinhibitor 6 (compound 9b) is a potent inhibitor of human carbonicanhydrase (hCA), with Kis of 9.7 nM, 35.2 nM, 88.5 nM, and 91.8 nM for hCA IX, hCA II, hCA XII and hCA I, respectively .
Carbonicanhydraseinhibitor 13 (compound 7) is a potent carbonicanhydrase (CA)inhibitor, which features 3-methylthiazolo[3,2-a]benzimidazole moiety (as a tail) connected to the zinc anchoring benzenesulfonamide moiety via ureido linker .
Antibacterial agent 167 (compound 13) is an inhibitor of pathogenic bacterial carbonicanhydrases. Antibacterial agent 167 inhibits the growth of N. gonorrhea strains at concentrations ranging from 16 to 64 µg/mL .
Dichlorphenamide (Diclofenamide) disodium is an orally active, specific, carbonicanhydraseinhibitor. Dichlorphenamide can reduce intraocular pressure by inhibiting the secretion of water from the eye. Dichlorphenamide can be used for glaucoma research .
FC14-584B, a dithiocarbamate, is a β-CarbonicAnhydraseinhibitor. FC14-584B inhibits the growth of trophozoites. FC14-584B can be used for the research of tuberculosis .
hCAII-IN-6 (Compound S-13) is a potent human carbonicanhydrase II (hCA II)inhibitor with a Ki of 4.4 nM. hCAII-IN-6 also inhibits other hCAs isoforms I, IV and IX, with Ki values of 9.2 nM, 480.2 nM and 14.7 nM, respectively. hCAII-IN-6 can be used for glaucoma research .
CDK2-IN-12 (compound 10b) is a potent CDK2inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibitshCA (carbonicanhydrase) 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 .
Disulfamide, an orally active diuretic, is a carbonicanhydraseinhibitor with the IC50 value of 0.07 μM. Disulfamide leads to diuresis by inhibitingcarbonicanhydrase and preventing the reabsorption of sodium and bicarbonate in the proximal tubule .
Carbonicanhydrase/AChE-IN-1 (compound 16) is a carbonicanhydrase and AChEinhibitor with Kis of 24.42 nM, 19.95 nM, and 5.07 nM for hCA I, hCA II, and AChE, respectively .
Enpp/Carbonicanhydrase-IN-1 (compound 1e) is a potent Enpp and carbonicanhydraseinhibitor with IC50s of 1.36, 1.35, 3.00, 0.88, 1.02 μM for NPP1, NPP2, NPP3, CA-II, CA-IX respectively. Enpp/Carbonicanhydrase-IN-1 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonicanhydrase-IN-1 induces Apoptosis .
Enpp/Carbonicanhydrase-IN-2 (compound 1i) is a potent Enpp and carbonicanhydraseinhibitor with IC50s of 1.13, 1.07, 0.74, 0.33, 0.68 for NPP1, NPP2, NPP3, CA-IX, CA-XII respectively. Enpp/Carbonicanhydrase-IN-2 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonicanhydrase-IN-2 induces Apoptosis .
Carbonicanhydrase/AChE-IN-2 (compound 19) is a selective acetylcholinesterase (AChE) and carbonicanhydrase (CA) inhibitor, with Ei of 5.07 nM, 24.42 nM and 19.95 nM for AChE, hCAI and hCAII, respectively .
ALP/Carbonicanhydrase-IN-1 (Compound 1e) is a dual carbonicanhydrase (CA) and alkaline phosphatase (ALP)inhibitor. ALP/Carbonicanhydrase-IN-1 shows IC50 values of 0.44 µM, 1.61 µM, 0.51 µM, and 0.107 µM for CA-II, CA-IX, CA-XII, and ALP, respectively .
Methazolamide (L584601) is a sulfonamide derivative used as a carbonicanhydraseinhibitor with a Ki of 14 nM for human carbonicanhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders .
CAII-IN-1 (compound 3n), a thiosemicarbazide derivative, is a potent, selective carbonicanhydrase-II (CA-II)inhibitor with an IC50 value of 10.3 µM for bovine CA-II. CAII-IN-1 can be used in research of carbonicanhydrase related biological disorders .
CAII-IN-2 (compound 3g), a thiosemicarbazide derivative, is a potent, selective carbonicanhydrase-II (CA-II)inhibitor with an IC50 value of 12.1 µM for bovine CA-II. CAII-IN-2 can be used in research of carbonicanhydrase related biological disorders .
Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonicanhydraseinhibitor with a Ki of 14 nM for human carbonicanhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders[1][2].
Quinethazone is an orally active diuretic agent and is also a weak inhibitor of carbonicanhydrase. Quinethazone can be used for hypertension research .
Acetazolamide is a carbonicanhydrase (CA) IXinhibitor with an IC50 of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities .
Acetazolamide sodium is a carbonicanhydrase (CA) IXinhibitor with an IC50 of 30 nM for hCA IX. Acetazolamide sodium has diuretic, antihypertensive and anti-gonococcal activities .
O-Desmethyl Brinzolamide hydrochloride (compound 6a), an active metabolite of Brinzolamide, is a carbonicanhydrase (CA)inhibitor with a Kd of 0.136 nM for CA II and an IC50 of 165 nM for CA IV .
Dichlorphenamide (Diclofenamide) is an orally active, specific, carbonicanhydraseinhibitor. Dichlorphenamide can reduce intraocular pressure by inhibiting the secretion of water from the eye. Dichlorphenamide can be used for glaucoma research .
Halazone is an atypical antimicrobial sulfonamide derivative and a carbonicanhydrase IIinhibitor with a Kd value of 1.45 µM. Halazone protects sodium channels from inactivation. Halazone is widely used for disinfection of drinking water .
hCAI/II-IN-7 (compound 1F) is a potent carbonicanhydrase (CA)inhibitor with Ki values of 23 nM, 44 nM and 20.57 µM for hCA-I, hCA-II and bovine CA, respectively .
Furagin (Furazidine) is an analogue of Nitrofurantoin (HY-A0090) and has antibacterial activity. Furagin also inhibits human carbonicanhydrases (Kis: 260 and 57 nM for hCA IX and XII, respectively) .
Dorzolamide (L671152) hydrochloride is a potent carbonicanhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
Dorzolamide (L671152) is a potent carbonicanhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
ulfanilamide (Sulphanilamide) is a potent and orally active sulfonamide antibiotic and can be a major intermediate of sulfamethoxazole biodegradation. Sulfanilamide also is a carbonicanhydraseinhibitor. Sulfanilamide shows inhibition on virus of lymphogranuloma venereum .
hCAI/II-IN-2 (compound 2b) is a potent dual hCA I/II inhibitor with Ki values of 40.97, 15.15 and 61.88 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-2 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity .
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 .
hCAII-IN-7 (Compound R-13) is a potent human carbonicanhydrase(hCA)inhibitor with Kis of 60.7, 320.7, 2298, and 35.2 nM for hCA I, II, IV and IX, respectively .
hCAII-IN-1 (compound 7f) is a potent and selective inhibitor of carbonicanhydrase (CA II/IX) with Kis of 1.2 and 113.6 nM, respectively. hCAII-IN-1 has the potential for the research of cancer diseases .
hCAII-IN-3 (compound 7e) is a potent and selective inhibitor of carbonicanhydrase (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 .
hCAIX/XII-IN-9 (compound 8) is a potent carbonicanhydrase (CA)inhibitor with Ki values of 1658 nM, 184.8 nM, 8.9 nM, 64.8 nM for hCA I, hCA II, hCA IX, and hCA XII, respectively .
Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor of carbonicanhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), and has anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 67 has IC50s of 10.4 μM and 50 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 67 binding to different isoforms of carbonicanhydrase are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII) .
Anti-inflammatory agent 68 (compound 7b) is a dual inhibitor of carbonicanhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), with anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 68 has IC50s of 12.6 μM and 60 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 68 binding to different isoforms of carbonicanhydrase are 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII) .
Acetazolamide- 13C2,d3 is the 13C- and deuterium labeled Acetazolamide. Acetazolamide is a carbonicanhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX[1]. Diuretic effects[4].
hCAI/II-IN-1 (Compound 3h) is a human carbonicanhydrase I and II (hCA I/II) inhibitor with IC50 values of 0.047 µM and 0.024 µM against hCA I and hCA II, respectively .
hCAIX-IN-18 (compound 30) is an inhibitor of carbonicanhydrase (CA), with Kis of 3.5 nM, 9.4 nM, 43.0 nM and 8.2 nM for hCAI, hCAII, hCAIX, hCAXII, respectively. hCAIX-IN-18 can be used for cancer research .
Acetazolamide (Standard) is the analytical standard of Acetazolamide. This product is intended for research and analytical applications. Acetazolamide is a carbonicanhydrase (CA) IXinhibitor with an IC50 of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities .
Brinzolamide (AL-4862) hydrochloride is a selective carbonicanhydrase IIinhibitor with an IC50 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 .
Dichlorphenamide (Standard) is the analytical standard of Dichlorphenamide. This product is intended for research and analytical applications. Dichlorphenamide (Diclofenamide) is an orally active, specific, carbonicanhydraseinhibitor. Dichlorphenamide can reduce intraocular pressure by inhibiting the secretion of water from the eye. Dichlorphenamide can be used for glaucoma research .
hCAII-IN-2 (Compound 11f) is a cytosolic human carbonicanhydrase (hCA)inhibitor with Ki values of 261.4, 3.8, 19.6 and 45.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively .
hCA I-IN-1 (Compound 6q) is a human carbonicanhydrase I (hCA I)inhibitor with Ki values of 38.3, 716.4, 940.1 and 192.8 nM against hCA I, hCA II, hCAIX and hCAXII, respectively .
hCA I-IN-2 (Compound 6d) is a selective human carbonicanhydrase 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 .
Brinzolamide (AL-4862) is a selective carbonicanhydrase IIinhibitor with anIC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide can be used in glaucoma disease research .
Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonicanhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
U-104 (SLC-0111) is a potent carbonicanhydrase (CA)inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model .
Benzthiazide is a long-acting diuretic and a hypertension agent. Benzthiazide is an inhibitor of carbonicanhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells .
hCAXII-IN-2 (compound 5i) is a potent human carbonicanhydrase XII (hCA XII) and hCA IXinhibitor with Ki values of 84.2 nM and 268.5 nM, respectively. hCAXII-IN-2 shows less active against hCA I and hCA II .
hCAIX/XII-IN-10 (compound DK-8) is a carbonicanhydraseinhibitor. hCAIX/XII-IN-10 has potent inhibitory activity against tumor-associated membrane-bound isoforms hCA IX and XII, with Ki values of 32.5 nM and 29.2 nM .
Benzolamide (CL11366) is a potent carbonicanhydrase (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 inhibitsCAS3, with a Ki of 54 nM. Benzolamide can be used for the research of glaucoma and seizures .
hCAII-IN-9 is a potent carbonicanhydrase inhibitor with IC50s of 1.18 μM (hCA II), 0.17 μM (hCA IX), and 2.99 μM (hCA XII), respectively. hCAII-IN-9 has no blood-brain barrier permeability .
Dorzolamide-d5 is the deuterium labeled Dorzolamide. Dorzolamide (L671152) is a potent carbonicanhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity[1][2].
hCAII-IN-3 (Compound 16) is a human carbonicanhydrase (hCA) inhibitor with Ki values of 403.8, 5.1, 10.2 and 5.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-2 shows anticancer activity .
Dorzolamide (hydrochloride) (Standard) is the analytical standard of Dorzolamide (hydrochloride). This product is intended for research and analytical applications. Dorzolamide (L671152) hydrochloride is a potent carbonicanhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
Fluorometholone acetate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester. Fluorometholone acetate potently inhibitscarbonicanhydrase (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 .
hCA IX-IN-1 (Compound 6f) is a human carbonicanhydrase (hCA) inhibitor with Ki 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 .
hCAIX/XII-IN-6 is an orally active carbonicanhydrase (CA)inhibitor. hCAIX/XII-IN-6 inhibits human CA isoforms hCA I, II, IV, IX, and XII with Ki values of 6697 nM, 2950 nM, 4093 nM, 4.1 nM and 7.7 nM, respectively. hCAIX/XII-IN-6 can be used for the research of rheumatoid arthritis (RA) .
Brinzolamide-d5 (hydrochloride) is the deuterium labeled Brinzolamide hydrochloride[1]. Brinzolamide (AL-4862) hydrochloride is a selective carbonicanhydrase II inhibitor with an IC50 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[2][3].
Brinzolamide (Standard) is the analytical standard of Brinzolamide. This product is intended for research and analytical applications. Brinzolamide (AL-4862) is a selective carbonicanhydrase IIinhibitor with anIC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide can be used in glaucoma disease research .
CA/MAO-B-IN-1 (Compound 78) is a dual inhibitor for human brain carbonicanhydrases (CA) and Monoamine Oxidase-B (MAO-B), with IC50s of 8.8 and 7.0 nM, respectively. CA/MAO-B-IN-1 reveals a human oral absorption of 71.9% through in silico prediction .
CL 5343 (5-Amino-1,3,4-thiadiazole-2-sulfonamide) is an inhibitor of human carbonicanhydrase B (HCA-B). CL 5343 can serve as a CA9 ligand to achieve the targeted delivery of maytansinoid to the cell membrane of SKRC52 renal cancer cells .
Zonisamide-d4 is the deuterium labeled Zonisamide. Zonisamide (AD 810) is an inhibitor of zinc enzyme carbonicanhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity. Zonisamide can be used for the rsearch for epilepsy, seizures and Parkinson's disease[1][2].
hCA XII/II/IX-IN-1 (Compound 3) is a potent human carbonicanhydrase (hCA)inhibitor with IC50 values of 2.6, 0.004, 0.005 and 0.001 μM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA XII/II/IX-IN-1 shows anticancer activity .
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonicanhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibitsCA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .
Punicalin is a species that can be isolated from the leaves of Punica granatum. Punicalin is an active molecule against hepatitis b virus (HBV). Punicalin can induce pyroptosis. Punicalin is a Carbonicanhydraseinhibitor. Punicalin blocks the binding of S-glycoprotein and ACE2 receptors. Pnuicalin has anti-inflammatory, antioxidant and antiviral activity .
hCAIX-IN-11 (Compound 5d) is a selective carbonicanhydrase IX and XIIinhibitor with Ki s of 32.7 and 623.5 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
hCAIX-IN-10 (Compound 6i) is a selective carbonicanhydrase IX and XIIinhibitor with Ki s of 61.5 and 586.8 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
hCAIX/XII-IN-5 (Coumarin 9a) a carbonicanhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis .
Indisulam (E 7070) is a carbonicanhydraseinhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
DPP IV/hCA II-IN-1 is a potent and selective dipeptidyl peptidase IV (DPP IV) and carbonicanhydrase (CA)inhibitor with an IC50 value of 0.049 μM for DPP IV and with Ki 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 .
hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual CarbonicAnhydrase(CA) IX/XII with Ki values of 4.7 nM and 8.3 nM for hCA XII and hCA IX, respectively. hCA/VEGFR-2-IN-1 (compound 13a) is a potent VEGFR-2inhibitor with IC50 values 26.3 nM. hCA/VEGFR-2-IN-1 has anticancer activity .
hCAIX/XII-IN-8 (compound 3g) is a potent human (carbonicanhydrase) CA IX and XIIinhibitor, with Ki values of 8.5 and 6.7 nM, respectively. hCAIX/XII-IN-8 shows particularly strong inhibitory activity against the tumor-associated membrane-bound isoforms, hCA IX and XII, while maintaining a high selectivity ratio over cytosolic off-target isoforms hCA I and II .
Zonisamide (AD 810) is an orally active carbonicanhydraseinhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy .
Zonisamide (AD 810) sodium is an orally active carbonicanhydraseinhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide sodium exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide sodium also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide sodium can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy .
WES-1 (Compound 8g) is an inhibitor of carbonicanhydrase 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 .
hCAI/II-IN-6 is an orally active human carbonicanhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and >50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy .
4-(Chloromethyl)-7-hydroxycoumarin (compound 4) is a hydroxycoumarin derivative with potent antioxidant effect and high hydroxyl radical-scavenging property. 4-(Chloromethyl)-7-hydroxycoumarin contains a methyl group and a chlorine group in the heterocyclic ring. A series of coumarins incorporating hydroxy-, chloro- and/or chloromethyl-moieties has been investigated as potent inhibitors of the zinc enzyme carbonicanhydrase, expecially tumor-associated isoforms CA IX and XII .
hCAI/II-IN-5 (compound MZ8) is a potent hCA I and hCA II (human carbonicanhydrase isoenzymes I and II) inhibitor, with IC50 values of 37.88 and 45.23 nM, respectively. hCAI/II-IN-5 also shows inhibition profile against α-Glycosidase and AChE, with IC50 values of 48.98 and 420.14 nM, respectively. hCAI/II-IN-5 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy .
α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonicanhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy .
hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonicanhydrase XII (hCA XII)inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research .
Punicalin is a species that can be isolated from the leaves of Punica granatum. Punicalin is an active molecule against hepatitis b virus (HBV). Punicalin can induce pyroptosis. Punicalin is a Carbonicanhydraseinhibitor. Punicalin blocks the binding of S-glycoprotein and ACE2 receptors. Pnuicalin has anti-inflammatory, antioxidant and antiviral activity .
ICA Protein, a potent inhibitor of carbonic anhydrase 2 (CA2), intricately regulates enzymatic activity within a finely tuned network. Functionally, ICA, a non-iron-binding monomer, exhibits specificity in inhibiting CA2. Its transferrin-like domain 2 engages in molecular interactions, underscoring ICA's regulatory role. This positions ICA as a key player, adding nuance to the precise mechanisms governing carbonic anhydrase activity. ICA Protein, Mouse (HEK293, His) is the recombinant mouse-derived ICA protein, expressed by HEK293 , with C-His labeled tag. The total length of ICA Protein, Mouse (HEK293, His) is 681 a.a., with molecular weight of ~76.2-80 kDa.
Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonicanhydraseinhibitor with a Ki of 14 nM for human carbonicanhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders[1][2].
Acetazolamide- 13C2,d3 is the 13C- and deuterium labeled Acetazolamide. Acetazolamide is a carbonicanhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX[1]. Diuretic effects[4].
Dorzolamide-d5 is the deuterium labeled Dorzolamide. Dorzolamide (L671152) is a potent carbonicanhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity[1][2].
Brinzolamide-d5 (hydrochloride) is the deuterium labeled Brinzolamide hydrochloride[1]. Brinzolamide (AL-4862) hydrochloride is a selective carbonicanhydrase II inhibitor with an IC50 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[2][3].
Zonisamide-d4 is the deuterium labeled Zonisamide. Zonisamide (AD 810) is an inhibitor of zinc enzyme carbonicanhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity. Zonisamide can be used for the rsearch for epilepsy, seizures and Parkinson's disease[1][2].
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