CA XII
CA XII is a membrane-associated carbonic anhydrase that catalyzes reversible CO2 hydration, supporting bicarbonate/proton generation and epithelial acid-base homeostasis[1]. Mechanistically, CA XII links pH regulation with bicarbonate transport, and CA12 mutation disrupts sweat-gland salt handling through reduced catalytic activity[2]. In disease models, CA12 was first characterized as a tumor-associated carbonic anhydrase overexpressed in some renal cell cancers, while higher CA XII expression in invasive breast carcinoma correlated with better prognosis[3][4]. Compared with CA IX, CA XII performs similar catalytic chemistry but shows distinct cancer associations; in breast cancer, CA IX relates more strongly to aggressive tumor biology, whereas CA XII expression can mark lower-grade disease[4][5]. For experimental applications, CA XII inhibitors support studies of tumor pH regulation, P-glycoprotein-mediated multidrug resistance, glioblastoma temozolomide resistance, and lymphoma cell proliferation[6][7][8].
References:
- [1]. Waheed A, et al. Carbonic anhydrase XII functions in health and disease. Gene. 2017 Aug 5;623:33-40. [Content Brief]
- [2]. Muhammad E, et al. Autosomal recessive hyponatremia due to isolated salt wasting in sweat associated with a mutation in the active site of Carbonic Anhydrase 12. Hum Genet. 2011 Apr;129(4):397-405. [Content Brief]
- [3]. Türeci O, et al. Human carbonic anhydrase XII: cDNA cloning, expression, and chromosomal localization of a carbonic anhydrase gene that is overexpressed in some renal cell cancers. Proc Natl Acad Sci U S A. 1998 Jun 23;95(13):7608-13. [Content Brief]
- [4]. Watson PH, et al. Carbonic anhydrase XII is a marker of good prognosis in invasive breast carcinoma. Br J Cancer. 2003 Apr 7;88(7):1065-70. [Content Brief]
- [5]. Mboge MY, et al. Selective inhibition of carbonic anhydrase IX over carbonic anhydrase XII in breast cancer cells using benzene sulfonamides: Disconnect between activity and growth inhibition. PLoS One. 2018 Nov 19;13(11):e0207417. [Content Brief]
- [6]. Tonissen KF, et al. Carbonic anhydrase XII inhibition overcomes P-glycoprotein-mediated drug resistance: a potential new combination therapy in cancer. Cancer Drug Resist. 2021 Jun 19;4(2):343-355. [Content Brief]
- [7]. Salaroglio IC, et al. Carbonic Anhydrase XII Inhibitors Overcome P-Glycoprotein-Mediated Resistance to Temozolomide in Glioblastoma. Mol Cancer Ther. 2018 Dec;17(12):2598-2609. [Content Brief]
- [8]. Lounnas N, et al. Pharmacological inhibition of carbonic anhydrase XII interferes with cell proliferation and induces cell apoptosis in T-cell lymphomas. Cancer Lett. 2013 Jun 1;333(1):76-88. [Content Brief]
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CA XII Related Products (64)
Related Products (64)
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Recombinant Proteins (1)
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Carbonic anhydrase-IN-37
0 ImagesCat. No.: HY-180189Carbonic anhydrase-IN-37 (compound 9a) is a potent and orally active carbonic anhydrase (CA) inhibitor with Kis of 9.7 and 1.0 nM for hCA VA and hCA VB, respectively. Carbonic anhydrase-IN-37 shows anti allodynic and antihyperalgesic effects on Paclitaxel (HY-B0015)-induced neuropathic pain in mice. Carbonic anhydrase-IN-37 can be used for neuropathic pain research.
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CAIX/XII/NAMPT-IN-1
0 ImagesCat. No.: HY-181350CAIX/XII/NAMPT-IN-1 is a triple inhibitor of carbonic anhydrase IX/XII and nicotinamide phosphoribosyltransferase (NAMPT) with a hCA IX Ki of 78.1 nM, hCA XII Ki of 64.4 nM, and hNAMPT IC50 of 168 nM. CAIX/XII/NAMPT-IN-1 induces apoptosis, ROS accumulation, suppresses ERK/AKT signaling, inhibits DNA synthesis, and causes mitochondrial dysfunction. CAIX/XII/NAMPT-IN-1 exerts antiproliferative effects against multiple cancer cells under normoxic and hypoxic conditions. CAIX/XII/NAMPT-IN-1 can be used for the research of cancer, such as renal carcinoma, glioblastoma and colorectal cancer.
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CAIX/CAXII-IN-1
0 ImagesCat. No.: HY-146819CAS No.: 2439165-37-2Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
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hCAIX-IN-24
0 ImagesCat. No.: HY-152001CAS No.: 3038222-64-6hCAIX-IN-24 is a potent and selectively hCA IX inhibitor with an KI value of 32.1 nM. hCAIX-IN-24 shows anti-proliferative activity.
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hCAIX-IN-17
0 ImagesCat. No.: HY-146007hCA IX-IN-1 (Compound 6f) is a human carbonic anhydrase (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.
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hCA/VEGFR-2-IN-5
0 ImagesCat. No.: HY-163710hCA/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.
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COX-2-IN-30
0 ImagesCat. No.: HY-149269CAS No.: 1160498-08-7COX-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.
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hCAIX-IN-22
0 ImagesCat. No.: HY-159568hCAIX-IN-22 is a highly selective inhibitor of human carbonic anhydrase (hCA) isoform XII (Ki=9.7 nM) with anticancer activity.
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CA IX-IN-2
0 ImagesCat. No.: HY-159122CAS No.: 3009842-92-3CA 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.
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COX-2/CA II-1
0 ImagesCat. No.: HY-184937COX-2/CA II-1 is an orally active dual selective inhibitor targeting COX-2 and hCA II. COX-2/CA II-1 inhibits COX-2 with an IC50 value of 0.13 μM (SI = 9.25 vs COX-1) and hCA II with a Ki value of 39.1 nM (SI = 933.8 vs hCA I). COX-2/CA II-1 demonstrates significant analgesic and anti-inflammatory effects in animal models, shows improved gastric safety with reduced ulcerogenic liability, and exhibits intraocular pressure (IOP)-lowering effects in rabbit glaucoma models. COX-2/CA II-1 can be used for anti-inflammatory, analgesic and antiglaucoma research.
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Elsulfavirine sodium
0 ImagesCat. No.: HY-109056ACAS No.: 867365-40-0Synonyms: R-1206 sodiumElsulfavirine 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.
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Carbonic anhydrase inhibitor 33
0 ImagesCat. No.: HY-172899Carbonic 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.
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CA
IX-IN-6
0 ImagesCat. No.: HY-187174CA IX-IN-6 is a selective human carbonic anhydrase IX (hCA IX) inhibitor, with Ki values of 8.9, 50.7, 551, and 64.4 nM against hCA IX, hCA XII, hCA I, and hCA II, respectively. CA IX-IN-6 binds to the active site via a classic sulfamide mode, coordinates with the catalytic Zn2+ ion, forms a hydrogen bond with Thr200, and interacts with key active site residues. CA IX-IN-6 can be used in studies related to tumor-associated carbonic anhydrase inhibition.
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HCAIX-IN-2
0 ImagesCat. No.: HY-146207CAS No.: 2389034-45-9HCAIX-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.
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hA2A/hCA XII modulator 1
0 ImagesCat. No.: HY-146979CAS No.: 2548963-55-7hA2A/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 carbonic anhydrase 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.
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Anticancer agent 314
0 ImagesCat. No.: HY-182245Anticancer 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.
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BE21349
0 ImagesCat. No.: HY-184660BE21349 is a carbonic anhydrase (CA) inhibitor with Ki values of 2090, 17.1, 61.8, and 40.5 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. BE21349 exhibits submicromolar inhibitory activity against leukemia, non-small cell lung cancer, and melanoma cell lines. BE21349 can be used in cancer-related research such as leukemia, non-small cell lung cancer, and melanoma.
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CAIX/CAXII-IN-2
0 ImagesCat. No.: HY-159132CAS No.: 3067730-65-5CAIX/CAXII-IN-2 (compound 23) is a CAIX/CAXII inhibitor, with Ki values of 8.9 nM and 5.3 nM for CAIX/CAXII, respectively. CAIX/CAXII-IN-2 can be used in cancer research.
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CAIX/XII-IN-16
0 ImagesCat. No.: HY-179034CAIX/XII-IN-16 (Compound 5d) is a selective inhibitor of CA IX/XII and c-Met. CAIX/XII-IN-16‘s Ki values for hCA IX, hCA XII and CA I are 10.6, 31.8 and 2361 nM respectively, and its IC50 value for c-Met is 0.49 μM. CAIX/XII-IN-16 exhibits significantly enhanced cytotoxicity against colon cancer cells under hypoxic conditions. CAIX/XII-IN-16 causes cell cycle arrest and induces apoptosis (apoptosis). CAIX/XII-IN-16 significantly enhances the efficacy of Oxaliplatin (HY-17371) and 5-Fluorouracil (HY-90006). CAIX/XII-IN-16 can be used for studies on chemotherapy resistance related to hypoxia.
