1. シグナル伝達
  2. Metabolic Enzyme/Protease
  3. Carbonic Anhydrase

Carbonic Anhydrase

Carbonate dehydratase

Carbonic anhydrase (CA) is a zinc-containing enzyme that catalyzes the reversible hydration of carbon dioxide: CO2 + H2O ⇋ HCO3- + H+. Eight genetically distinct carbonic anhydrase enzyme families (α-, β-, γ- δ-, ζ-, η-, θ- and ι- CAs) were described to date. Carbonic anhydrases are involved in numerous physiological and pathological processes. Many of them are important therapeutic targets with the potential to be inhibited to treat a range of disorders including oedema, glaucoma, obesity, cancer, epilepsy, and osteoporosis.

The carbonic anhydrase reaction is involved in many physiological and pathological processes, including respiration and transport of CO2 and bicarbonate between metabolizing tissues and lungs; pH and CO2 homeostasis; electrolyte secretion in various tissues and organs; biosynthetic reactions (such as gluconeogenesis, lipogenesis, and ureagenesis); bone resorption; calcification; and tumorigenicity. α-CAs are Zn2+ metalloproteins expressed in animals, vertebrates, prokaryotes, fungi, algae, protozoa, and plants. Sixteen mammalian α-CA isoforms are known to be involved in many diseases such as glaucoma, edema, epilepsy, obesity, hypoxic tumors, neuropathic pain, arthritis, neurodegeneration, etc.

製品番号 製品名 製品効果 純度 構造式
  • HY-161322
    hCAXII-IN-9 Inhibitor
    hCAXII-IN-9 (Compound 3I) is a selective inhibitor of hCAXII with Ki values of 28 nM, 7192.6 nM, 188.6 nM, and >100000 nM for hCAXII, hCAI, hCAII, and hCAIX, respectively. hCAXII-IN-9 can be utilized in antitumor research.
    hCAXII-IN-9
  • HY-120321
    DSR-71167 Inhibitor
    DSR-71167 is an orally active mineralocorticoid receptor (MR) antagonist with an IC50 of 0.26 μM. DSR-71167 exhibits weak carbonic anhydrase (CA) inhibitory activity with an IC50 of 19 μM. DSR-71167 can dose-dependently increase urinary sodium excretion in rat models and has a very low risk of hyperkalemia in potassium-loading rat models. DSR-71167 lowers systolic blood pressure in hypertensive rat models. DSR-71167 can be used for research on hypertension and heart failure.
    DSR-71167
  • HY-178922
    CAI/II-IN-13 Inhibitor
    CAI/II-IN-13 (Compound 5f) is a CAI/II inhibitor, with IC50 values of 309.16 nM for hCA I and 267.27 nM for hCA II. CAI/II-IN-13 exhibits potent and selective antiproliferative activity against A549 lung cancer cells (IC50 = 0.58 μM). CAI/II-IN-13 can be used for the study of lung cancer.
    CAI/II-IN-13
  • HY-147986
    hCA I-IN-2 Inhibitor
    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.
    hCA I-IN-2
  • HY-178017
    BChE/hCA II-IN-1 Inhibitor
    BChE/hCA II-IN-1 (Compound 20) is a dual-functional inhibitor of Butyrylcholinesterase (BChE) and human carbonic anhydrase II (hCA II) with IC50s of 76.50 and 10.69  μM for BChE and hCA II, respectively. BChE/hCA II-IN-1 can be used for neurodegenerative diseases like Alzheimer's and glaucoma research.
    BChE/hCA II-IN-1
  • HY-B0122A
    Topiramate lithium Inhibitor
    Topiramate (McN 4853) lithium is a broad-spectrum antiepileptic agent. Topiramate lithium 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.
    Topiramate lithium
  • HY-155522
    WES-1 Inhibitor
    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.
    WES-1
  • HY-150695
    hCAIX/XII-IN-5 Inhibitor
    hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (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.
    hCAIX/XII-IN-5
  • HY-168124
    Carbonic anhydrase inhibitor 26 Inhibitor
    Carbonic anhydrase inhibitor 26 (compund 6T) is a carbonic anhydrase II inhibitor with IC50 of 9.10 ± 0.26 μM.
    Carbonic anhydrase inhibitor 26
  • HY-178030
    CAXII-IN-3 Inhibitor
    CAXII-IN-3 is an effective carbonic anhydrase (CA XII) inhibitor with a Ki of 53 nM. CAXII-IN-3 exhibits selective inhibition against multiple human CA subtypes with Kis of 5.3 μM, 75 nM, 1.9 μM, > 10 μM against CA I, CA II, CA IV and CA IX. CAXII-IN-3 mainly inhibits CA II and XII, and reduces aqueous humor production. CAXII-IN-3 exhibits β3-AR agonistic activity, can dilate retinal blood vessels, and improve optic nerve perfusion. CAXII-IN-3 can be used in the research of ocular disorders such as glaucoma.
    CAXII-IN-3
  • HY-155271
    hCAXII-IN-7 Inhibitor
    hCAXII-IN-7 (compound 6e) is a hCA XII inhibitor. hCAXII-IN-7 has BBB permeability. hCAXII-IN-7 induces 786-0, SF-539 and HS 578 T cells apoptotic.
    hCAXII-IN-7
  • HY-161174
    Carbonic anhydrase inhibitor 17 Inhibitor
    Carbonic anhydrase inhibitor 17 (compound 7c) ,pyridazine-tethered sulfonamide, is a carbonic anhydrase II inhibitor with IC50 of 0.63 nM.
    Carbonic anhydrase inhibitor 17
  • HY-150573
    CDK2-IN-12 Inhibitor
    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.
    CDK2-IN-12
  • HY-175239
    CAII/CAXII-IN-1 Inhibitor
    CAII/CAXII-IN-1 (compound 8d) is a CAII/CAXII inhibitor with IC50 values of 0.38 µM and 0.61 µM for CAII and CAXII, respectively.
    CAII/CAXII-IN-1
  • HY-155760
    hCA/VEGFR-2-IN-3 Inhibitor
    hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells.
    hCA/VEGFR-2-IN-3
  • HY-161522
    α-Glucosidase-IN-63 Inhibitor
    α-Glucosidase-IN-63 (Compound 4d) is an inhibitor of α-Glucosidase (IC50=0.44 μM). α-Glucosidase-IN-63 inhibits hCA II with an activity of Ki= 7.0 nM. α-Glucosidase-IN-63 is orally effective..
    α-Glucosidase-IN-63
  • HY-120677
    AHR-15010 Inhibitor
    AHR-15010 is an oral active carbonic anhydrase inhibitor with the IC50 of 0.13 μM. AHR-15010 shows anti-arthritic activity and can be used for study of arthritis .
    AHR-15010
  • HY-156013
    CA inhibitor 2 Inhibitor
    CA inhibitor 2 (Compound 4H) is a carbonic anhydrase inhibitor (IC50: 0.033 μM).
    CA inhibitor 2
  • HY-147828
    hCAIX-IN-11 Inhibitor
    hCAIX-IN-11 (Compound 5d) is a selective carbonic anhydrase IX and XII inhibitor 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-11
  • HY-151472
    hCAIX/XII-IN-6 Inhibitor
    hCAIX/XII-IN-6 is an orally active carbonic anhydrase (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).
    hCAIX/XII-IN-6
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