CA I
CA I is a cytosolic carbonic anhydrase isozyme that catalyzes reversible CO2 hydration to bicarbonate and protons, supporting acid-base balance, respiration, CO2/HCO3- transport, and pH homeostasis[1]. Mechanistically, CA isoforms participate in ion transport and electrolyte secretion, and several isoforms form functional metabolons with anion exchangers or Na+/HCO3- cotransporters[1]. In experimental disease contexts, cytosolic CA I, CA II, and CA XIII are down-regulated in colorectal cancer tissue compared with matched normal mucosa, supporting their evaluation in tumor biology models[2]. Compared with related isoforms, CA I is cytosolic, whereas CA IX and CA XII are membrane-associated tumor-related isoforms, and CA VA/VB are mitochondrial targets linked to metabolic drug-design studies[1]. This distinction is critical because CA IX inhibition addresses hypoxic tumor pH regulation, whereas CA I studies more directly model cytosolic CO2/HCO3- conversion and erythrocyte-associated enzyme pharmacology[1][3]. For experimental applications, hydroperoxides, alcohols, acetates, bromophenols, and selected clinical drugs inhibit hCA I and hCA II in vitro, providing chemical tools for isoform-comparative inhibitor profiling[4][5][6].
References:
- [1]. Magometschnigg D. Angiotensin-Rezeptor-Blocker--Bedeutung für die Hochdrucktherapie [Angiotensin receptor blockers--significance for the therapy of hypertension]. Wien Med Wochenschr. 2001;151(7-8):153-6. German. PMID: 11450162. et al. Angiotensin-Rezeptor-Blocker--Bedeutung für die Hochdrucktherapie [Angiotensin receptor blockers--significance for the therapy of hypertension]. Wien Med Wochenschr. 2001;151(7-8):153-6. German. [Content Brief]
- [2]. Kummola L, et al. Expression of a novel carbonic anhydrase, CA XIII, in normal and neoplastic colorectal mucosa. BMC Cancer. 2005 Apr 18;5:41. [Content Brief]
- [3]. Jiang R, et al. Effectiveness of exercise on perinatal depression and anxiety symptoms: A network meta-analysis and dose-response analysis. Int J Gynaecol Obstet. 2026 Jun;173(3):1308-1324. [Content Brief]
- [4]. Kose LP, et al. The human carbonic anhydrase isoenzymes I and II inhibitory effects of some hydroperoxides, alcohols, and acetates. J Enzyme Inhib Med Chem. 2016 Dec;31(6):1248-53. [Content Brief]
- [5]. Taslimi P, et al. The effects of some bromophenols on human carbonic anhydrase isoenzymes. J Enzyme Inhib Med Chem. 2016 Aug;31(4):603-7. [Content Brief]
- [6]. Güller U, et al. In vitro and in silico interactions of antiulcer, glucocorticoids and urological drugs on human carbonic anhydrase I and II isozymes. Biopharm Drug Dispos. 2022 Apr;43(2):47-56. [Content Brief]
-
CA I Related Products (68)
Related Products (68)
-
Recombinant Proteins (1)
-
AChE/hCA I-IN-1
0 ImagesCat. No.: HY-170560CAS No.: 155140-19-5AChE/hCA I-IN-1 (Compound L3) is the inhibitor for acetylcholinesterase (AChE) and carbonic anhydrase (CA), that inhibits AChE, hCA I and hCA II with IC50 of 302, 265 and 283 nM, respectively.
-
CAI/II-IN-2
0 ImagesCat. No.: HY-147922CAS No.: 2480283-75-6CAI/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. CAI/II-IN-2 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity.
-
Carbonic anhydrase/AChE-IN-1
0 ImagesCat. No.: HY-161142CAS No.: 3029817-10-2Carbonic anhydrase/AChE-IN-1 (compound 16) is a carbonic anhydrase and AChE inhibitor with Kis of 24.42 nM, 19.95 nM, and 5.07 nM for hCA I, hCA II, and AChE, respectively.
-
CAI/II-IN-3
0 ImagesCat. No.: HY-147923CAS No.: 2480283-93-8CAI/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. CAI/II-IN-3 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity.
-
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.
-
CAI/II-IN-5
0 ImagesCat. No.: HY-147955CAS No.: 2428389-67-5CAI/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. CAI/II-IN-5 also shows inhibition profile against α-Glycosidase and AChE, with IC50 values of 48.98 and 420.14 nM, respectively. CAI/II-IN-5 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy.
-
CAII/lX-IN-1
0 ImagesCat. No.: HY-181689CAS No.: 2955799-99-0CAII/lX-IN-1 (compound 14 (21,301,644)) is an inhibitor belonging to the N-acyl sulfonamides class, which selectively targets Carbonic Anhydrase IX and II. The IC50 values of CAII/lX-IN-1 against hCA-IX and hCA-II are 1.2 μM and 6.7 μM, respectively, with corresponding Ki values of 0.9 and 4.8.
-
hCA I-IN-4
0 ImagesCat. No.: HY-169962CAS No.: 3054159-56-4hCA I-IN-4 (Compound 14) is the inhibitor for carbonic anhydrase and cholinesterase, that inhibits hCA I, hCA II, AChE, and BChE with Ki of 29.94 nM, 17.72 nM, 21.21 nM, and 7.65 nMrespectively. hCA I-IN-4 exhibits cytotoxicity in BT-549 with IC50 of 16.59 μM.
-
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.
-
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.
-
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.
-
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.
-
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.
-
hCA I-IN-3
0 ImagesCat. No.: HY-158372hCA I-IN-3 (compound 24), an aryl ether derivative, is a potent carbonic anhydrase inhibitor. hCA I-IN-3 can inhibit carbonic anhydrase hCA I and hCA II isoenzymes, with IC50 values of 4.77 and 9.66 nM, respectively. hCA I-IN-3 can be used for cancer research.
-
DPP IV/hCA II-IN-1
0 ImagesCat. No.: HY-151578CAS No.: 2836996-95-1DPP 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.
-
NCX-278
0 ImagesCat. No.: HY-182426CAS No.: 1202697-61-7NCX-278 is a human carbonic anhydrase inhibitor with a 13 nM Ki for hCA II, 410 nM Ki for hCA I, 181 nM Ki for hCA IV, and selective inhibition of hCA II over hCA IV. NCX-278 is a potent and effective stimulator of NO/sGC/cGMP signaling with an EC50 of 2.05 lM. NCX-278 exerts NO-mediated vascular relaxant effects. NCX-278 lowers intraocular pressure in normotensive rabbits. NCX-278 can be used for the research of open-angle glaucoma.
-
hCAII-IN-10
0 ImagesCat. No.: HY-161282hCAII-IN-10 (compound 11d) is hCA II inhibitor with the IC50s of 14 nM and 29.2 μM for hCA II and hCA I, respectively. hCAII-IN-10 inhibits cell growth against HT-29 cells with the IC50 of 74 μM. hCAII-IN-10 shows strongly lowered intraocular pressure in the glaucomatous rabbit eye model.
-
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.
-
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.
