2. Signalwege
  3. Metabolic Enzyme/Protease
  4. Carbonic Anhydrase
  5. CA IX Isoform

CA IX

Carbonic anhydrase IX (CA IX, CA9) is a transmembrane, tumor-associated carbonic anhydrase isoform that catalyzes the reversible hydration of carbon dioxide to bicarbonate and protons, thereby contributing to cellular and extracellular pH regulation under hypoxic conditions[1][2]. CA IX is strongly induced by hypoxia through hypoxia-inducible factor (HIF)-dependent transcriptional regulation and functions as a key component of the adaptive response of tumor cells to oxygen deprivation[3][4]. Mechanistically, CA IX supports the bicarbonate import arm of pH-control machinery and participates directly in the establishment of an acidic tumor microenvironment while maintaining conditions compatible with cancer cell survival and proliferation[1][5][6]. Consequently, CA IX contributes to extracellular acidification, tumor progression, invasion, metastasis, and resistance to therapy in multiple solid tumors[5][7][8]. In disease models, CA IX expression is broadly associated with hypoxic regions of tumors and has been linked to poor prognosis, increased metastatic potential, and aggressive tumor phenotypes[7][8][9]. Compared with related carbonic anhydrase isoforms, CA IX possesses a unique extracellular proteoglycan domain that is absent from other family members and is considered a distinctive structural feature relevant to its biological functions in the tumor microenvironment[2]. Furthermore, CA IX is one of only a few carbonic anhydrase isoenzymes with strong tumor association and limited expression in most normal tissues, enhancing its value as a disease biomarker and experimental target[10][11]. For research applications, selective sulfonamide-based CA IX inhibitors suppress CA IX-mediated extracellular acidification and have been widely employed for functional studies, molecular imaging, and evaluation of therapeutic strategies targeting hypoxic tumors[6][12].

References:

Art. -Nr. Produktname Wirkung Reinheit
  • HY-P991887
    CA9hu-1
    CA9hu-1 is an internalization‑inducing antibody. CA9hu-1 triggers internalization of CA IX in cells. CA9hu-1 can be used for the research of cancer.
  • HY-151633
    hCAIX-IN-14
    		Inhibitor
    hCAIX-IN-14 (compound 5a) is a potent inhibitor of human CA IX with a Ki value of 134.8 nM.
  • HY-115994
    Carbonic anhydrase inhibitor 10
    		Inhibitor
    Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research.
  • HY-163710
    hCA/VEGFR-2-IN-5
    		Inhibitor
    hCA/VEGFR-2 IN-5 (compound 9) is an indolone-phenylsulfonamide and a potential dual inhibitor of cancer-related hCA IX/XII and VEGFR-2. The IC50 values of hCA/VEGFR-2-IN-5 for VEGFR-2, hCA IX and hCA XII are 0.38 μM, 40 and 3.2 nM, respectively. hCA/VEGFR-2-IN-5 has antitumor activity.
  • HY-149269
    COX-2-IN-30
    		Inhibitor
    COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect.
  • HY-159122
    CA IX-IN-2
    		Inhibitor
    CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models.
  • HY-168855
    hCAII/IX-IN-1
    		Inhibitor
    hCAII/IX-IN-1 (compound 4o) is a potent inhibitor of hCAII and hCAIX, with the Kis of 7.4 and 7.0 nM, respectively. hCAII/IX-IN-1 plays an important role in cancer research.
  • HY-120367
    DTP348
    		Inhibitor
    DTP348 is an inhibitor for carbonic anhydrase IX with a Ki of 8.3 nM in vitro and an IC50 of 19.26 μM in Xenopus oocytes. DTP348 exhibits slight toxicity in zebrafish embryos with LD50 of 3.5 mM. DTP348 can be used in the anti-cancer research.
  • HY-109056A
    Elsulfavirine sodium
    		Inhibitor
    Elsulfavirine sodium (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine sodium also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine sodium and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine sodium is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine sodium exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine sodium is used in studies related to HIV-1 infection and liver cancer.
  • HY-172899
    Carbonic anhydrase inhibitor 33
    		Inhibitor
    Carbonic anhydrase inhibitor 33 (11D) is a dual inhibitor of CA (Carbonic anhydrase) IX/XII and CDK6, with Ki values of 19.7 nM and 26.1 nM for hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 33 (11D) induces G1 arrest and apoptosis. Carbonic anhydrase inhibitor 33 (11D) can be used in the research for NSCLC.
  • HY-146207
    HCAIX-IN-2
    		Inhibitor
    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.
  • HY-179022
    CAIX/CDK-2-IN-1
    		Inhibitor
    CAIX/CDK-2-IN-1 is a dual-acting inhibitor of carbonic anhydrase IX (CA IX) and cyclin-dependent kinase-2 (CDK-2) with IC50 values of 0.29 μM and 0.32 μM. The zein nanoparticls of CAIX/CDK-2-IN-1 can induce cancer cells apoptosis. CAIX/CDK-2-IN-1 can be used for the research of cancer, such as lung cancer.
  • HY-44602
    Thioaspirine
    		Inhibitor
    Thioaspirine is a carbonic anhydrase (CA) inhibitor with Kis of 64.3 and 10.9 μM for hCA II and hCA IX, respectively. Thioaspirine effectively relieves the inflammatory pain in CFA (HY-153808)-treated mice. Thioaspirine can be used for inflammatory pain research.
  • HY-113719
    VM4-037
    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.
  • HY-151578
    DPP IV/hCA II-IN-1
    		Inhibitor
    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.
  • HY-P992322
    BAY-79-4620 Antibody
    		Modulator
    BAY-79-4620 Antibody is a potent and selective CAIX antibody with a human CAIX Kd of 3.6 nM. BAY-79-4620 Antibody yields antibody-drug conjugate (ADC) through conjugating with Monomethyl auristatin E (HY-15162) via a self-immolative enzyme-cleavable linker. BAY-79-4620 Antibody can be used for the research of cervical carcinoma, non-small cell lung carcinoma, breast carcinoma, pancreatic carcinoma, gastric carcinoma, prostate carcinoma.
  • HY-182245
    Anticancer agent 314
    		Inhibitor
    Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer.
  • HY-P11737
    IPM-N001
    		Ligand
    IPM-N001 is a carbonic anhydrase IX (CAIX) ligand with a Kd value of <0.0337 nM for hCAIX. When radio-conjugated with 68Ga, IPM-N001 serves as a CAIX-targeted radionuclide tracer. [68Ga]Ga-IPM-N001 exhibits excellent tumor uptake and significantly improves the tumor-to-background ratio in PET/CT imaging studies using OS-RC-2 tumor-bearing mice. IPM-N001 can be used for the research of clear cell renal cell carcinoma.
  • HY-144807
    Carbonic anhydrase inhibitor 9
    		Inhibitor
    Carbonic anhydrase inhibitor 9 is a potent carbonic anhydrase (CA) inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity.
  • HY-151632
    hCAIX-IN-15
    		Inhibitor
    hCAIX-IN-15 is a potent hCA IX inhibitor with a Ki value of 38.8 nM. hCAIX-IN-15 shows good broad-spectrum anticancer activity and can be used for cancer research.
Art. -Nr. Produktname / Synonyms Species Source