HCAIX-IN-2 (compound 9d) is a selective carbonic anhydrase inhibitor with the Ki values of 24.6 nM and 45.3 nM for hCA IX and hCA XII, respectively[1].
hCAIX-IN-8 (compound 7i) is a potent and selective hCAIX inhibitor with IC50s of 1.99, 0.024, 1.10 µM for CAII, CAIX, CAVA respectively. hCAIX-IN-8 shows anti-proliferation activity with low toxicity. hCAIX-IN-8 decreases the epithelial to mesenchymal transitions and induces apoptosis. hCAIX-IN-8 inhibits cell migration and colonization potential[1].
Sulthiame-d4 is the deuterium labeled Sultiame. Sultiame is a carbonic anhydrase inhibitor, widely used as an antiepileptic agent[1][2].
L-693612 hydrochloride (Compd 1) is an orally active and topical carbonic anhydrase inhibitor[1].
Carbonic anhydrase inhibitor 6 (compound 9b) is a potent inhibitor of human carbonic anhydrase (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[1].
Clofenamide (Aquedux) is a carbonic anhydrase (CA) inhibitor. Clofenamide exhibits diuretic activity[1].
hCAI/II-IN-6 is a human carbonic anhydrase(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[1].
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA 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[1].
Phenylsulfamide (Compound 10) is a human carbonic anhydrase-II (hCA-II) inhibitor with a Kd of 45.50 μM and a Ki of 79.60 μM[1].
hCAIX-IN-18 (compound 30) is an inhibitor of carbonic anhydrase (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[1].
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 carbonic anhydrase 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[1].
U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.IC50 value: 45.1 nM/4.5 nM(Ki, CA IX/CA XII) [1]Target: Carbonic anhydrase inhibitorin vitro: U-104 (50 μM) blocks the mesenchymal phenotype in the cancer stem cells population in hypoxia condition of 4T1 cells. U-104 (<50 μM) significantly reduces migration in a dose-dependent manner in metastatic MDA-MB-231 LM2-4Luc+ cells , with cells growing as compact colonies similar to parental MDA-MB-231 cells [2]. in vivo: U-104 (38 mg/kg) inhibits primary tumor growth in the mice implanted orthotopically with MDA-MB-231 LM2-4Luc+ cells. U-104 (19 mg/kg) inhibits metastases formation in the 4T1 experimental metastasis mice model [1]. U-104 (38 mg/kg) significantly delay primary tumor growth and reduces cancer stem cell population in NOD/SCID mice orthotopically implanted with MDA-MB-231 LM2-4Luc+ cells. U-104 (5 mg/mL, oral gavage) shows a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells [2].
hCAI/II-IN-5 (compound MZ8) is a potent hCA I and hCA II (human carbonic anhydrase 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[1].
VM4-037 can be used for the synthesis of VM4-037(18F). VM4-037(18F) is a fluorinated PET imaging agent for carbonic anhydrase IX[1].
hCAXII-IN-4 (compound 5j) is a potent and selective CA XII inhibitor with an Ki value of 6.4 nM for human CA XII[1].
hCAXII-IN-3 (Compound 6o) is a selective human carbonic anhydrase XII (hCAXII) inhibitor with a Ki of 10.0 nM[1].
hCAIX-IN-10 (Compound 6i) is a selective carbonic anhydrase IX and XII inhibitor 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[1].
hCAIX/XII-IN-2 (compound 6a) is a potent and selective hCAIX and hCAXIIinhibitor with Ki values of >10000, >10000, 30.0, 3.6 nM for hCAI, hCAII, hCAIX and hCAXII, respectively[1].
hCA I-IN-1 (Compound 6q) is a human carbonic anhydrase 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[1].
Dorzolamide-d5 (L671152-d5) is the deuterium labeled Dorzolamide. Dorzolamide (L671152) is a potent carbonic anhydrase 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].
Dichlorphenamide disodium is an orally active, specific, carbonic anhydrase inhibitor. Dichlorphenamide can reduce intraocular pressure by inhibiting the secretion of water from the eye. Dichlorphenamide can be used for glaucoma research[1].
(E)-Dehydrodiconiferyl alcohol behaves as good hCA IX and hCA XII dual inhibitors[1]. And (E)-Dehydrodiconiferyl alcohol suppresses the NF-κB nuclear translocation in connective tissue of healing area[2].
Methazolamide is a carbonic anhydrase inhibitor used to treat glaucoma.Target: Carbonic AnhydraseMethazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively [1]. Methazolamide is of strength equal to acetazolamide, another carbonic anhydrase inhibitor used to treat irregular breathing disorders. However, methazolamide differs from acetazolamide in that it fails to activate Ca2+-dependent potassium channels in skeletal muscles. Methazolamide does not impair respiratory work performance in anesthetized rabbits [2]. Oral administration of methazolamide decreases IOPs and AHFRs in clinically normal dogs, with effectiveness diminishing in the evening [3].
These compounds show selective inhibition on tumor related subtypes HCA IX and XII, and are also considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
DPP IV/hCA II-IN-1 is a potent and selective dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (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[1].
hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 µM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) [1].
Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase[1][2][3].
hCAII-IN-2 (Compound 11f) is a cytosolic human carbonic anhydrase (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[1].
Brinzolamide(AL 4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.Target: carbonic anhydrase IIBrinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1-2 hours. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. Brinzolamide dosages of 30 mg/kg, produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. Brinzolamide of 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice [1]. Brinzolamide (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily [2].
hCAIX-IN-14 (compound 5a) is a potent inhibitor of human CA IX with a Ki value of 134.8 nM[1].