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)
-
CAXII-IN-4
0 ImagesCat. No.: HY-187173CAXII-IN-4 is a human carbonic anhydrase XII (hCA XII) inhibitor with Ki values of 4.9, 3079, 62.5 and 58.4 nM against hCA XII, hCA I, hCA II and hCA IX, respectively, showing high selectivity toward tumor-associated hCA XII. CAXII-IN-4 binds to the active site of hCA XII via a classic sulfamide binding mode, coordinates with Zn2+, forms a hydrogen bond with Ser133, and stabilizes the enzyme complex to reduce structural deviation. CAXII-IN-4 possesses both lipophilicity and polarity, and is predicted to have superior membrane permeability and oral absorbability. CAXII-IN-4 can be used in studies related to tumor-associated carbonic anhydrase inhibition.
-
Carbonic anhydrase-IN-40
0 ImagesCat. No.: HY-187383Carbonic anhydrase-IN-40 is a human carbonic anhydrase I/II inhibitor, with an IC50 of 16.900 nM against hCA I and an IC50 of 4.682 nM against hCA II. Carbonic anhydrase-IN-40 binds to the active site of the enzyme, coordinates with the catalytic zinc ion, forms π-π stacking interactions with active site residues, and makes hydrophobic contacts with the hydrophobic pocket. Carbonic anhydrase-IN-40 can serve as a lead compound for studies related to carbonic anhydrase inhibitors.
-
hCAIX/XII-IN-8
0 ImagesCat. No.: HY-156181CAS No.: 59994-64-8hCAIX/XII-IN-8 (compound 3g) is a potent human (carbonic anhydrase) CA IX and XII inhibitor, with Ki values of 8.5 and 6.7 nM, respectively. hCAIX/XII-IN-8 shows particularly strong inhibitory activity against the tumor-associated membrane-bound isoforms, hCA IX and XII, while maintaining a high selectivity ratio over cytosolic off-target isoforms hCA I and II.
-
Carbonic anhydrase-IN-35
0 ImagesCat. No.: HY-175638Carbonic anhydrase-IN-35 is a selective carbonic anhydrase (CA) inhibitor. Carbonic anhydrase-IN-35 potently inhibits tumor-associated hCA IX (Ki = 0.6 nM) and hCA XII (Ki = 2.2 nM). Carbonic anhydrase-IN-35 induces apoptosis in MCF-7 cells by elevating Bax, reducing Bcl-2, and downregulating CDK4/6. Carbonic anhydrase-IN-35 exhibits potent cytotoxicity against MCF-7 (IC50 = 0.3975 μM normoxic/0.6575 μM hypoxic), MCF-7-ADR (IC50> = 0.3975 μM normoxic/4.488 μM hypoxic), MDA-MB-231, and 4T1 breast cancer cells. Carbonic anhydrase-IN-35 can be used for the study of breast cancer.
-
hCAIX-IN-21
0 ImagesCat. No.: HY-159128CAS No.: 3047757-55-8hCAIX-IN-21 (compound 16c) is a potent hCAIX inhibitor with KI values of 5.2, 3.5, 12.6, 13600 nM for hCAIX, hCA II, hCA XII, hCA I, respectively. hCAIX-IN-21 inhibits cathepsin B enzyme activity.
-
Multi-target kinase-IN-11
0 ImagesCat. No.: HY-189488Multi-target kinase-IN-11 (compound 2a) is a potent multi-target inhibitor of Cholinesterase and Carbonic Anhydrase. Multi-target kinase-IN-11 inhibits AChE, BChE, hCA I, and hCA II with IC50 values of 2.78, 4.88, 0.94, and 4.15 μM, respectively. Multi-target kinase-IN-11 inhibits these enzymes through hydrogen bonding and electrostatic interactions with active site residues. Multi-target kinase-IN-11 can be used for research on Alzheimer's disease.
-
CAII-IN-11
0 ImagesCat. No.: HY-180916CAII-IN-11 (Compound A1) is a dual-target compound that contains a hCA II inhibitor (IC₅₀ = 2 nM) portion and a NO donor portion. CAII-IN-11 also has inhibitory activity against hCA IX, hCA XII, and hCA I, with IC50 values of 6, 3, and 152 nM respectively. CAII-IN-11 significantly increases the intracellular cGMP level in human trabecular meshwork cells. CAII-IN-11 reduces the apoptosis of retinal ganglion cells by reducing oxidative stress (ROS levels), inhibiting astrocytes and the NLRP3 inflammasome activation. CAII-IN-11 has hypotensive activity in rabbit models and can be used for the study of glaucoma.
-
CAI/II-IN-8
0 ImagesCat. No.: HY-161507CAS No.: 3036136-18-9CAI/II-IN-8 (Compound 8) is a hydrazide derivative based on 4-hydroxybenzaldehyde. CAI/II-IN-8 primarily targets human carbonic anhydrase isomerase I (hCA I) and II (hCA II) for inhibition (IC50 = 21.35 ± 0.39 nM (CA I); 7.12 ± 0.12 nM (CA II)). CAI/II-IN-8 inhibits AChE and BChE as well(IC50 = 46.27 ±0.75 nM (AChE); 43.38 ± 0.83 nM (BChE)). ..
-
hCAIX/XII-IN-15
0 ImagesCat. No.: HY-173394CAS No.: 69141-46-4hCAIX/XII-IN-15 (Compound 17β) is an inhibitor of hCA IX and hCA XII, with Kis of 0.42 and 4.37 μM respectively. hCAIX/XII-IN-15 has pro-apoptotic effect in multiple myeloma cells.
-
hCA-I/hCA-II-IN-1
0 ImagesCat. No.: HY-174835hCA-I/hCA-II-IN-1 (Compound P4) is a potent dual human carbonic anhydrase I (hCA-I) and human carbonic anhydrase II (hCA-II) inhibitor with Ki values of 0.22 μM and 0.33 μM, respectively. hCA-I/hCA-II-IN-1 can be used in research on diseases related to CA enzymes such as glaucoma, hypertension, and ulcers.
-
hCAIX/XII-IN-9
0 ImagesCat. No.: HY-162063hCAIX/XII-IN-9 (compound 8) is a potent carbonic anhydrase (CA) inhibitor with Ki values of 1658 nM, 184.8 nM, 8.9 nM, 64.8 nM for hCA I, hCA II, hCA IX, and hCA XII, respectively.
-
CAI/II-IN-4
0 ImagesCat. No.: HY-147925CAS No.: 2480284-01-1CAI/II-IN-4 (compound 6d) is a potent dual hCA I/II inhibitor with Ki values of 16.95, 15.22 and 27.04 nM for hCA I, hCA II and hCA Ⅸ, respectively. CAI/II-IN-4 has anti-hypoxia activities and low toxicity. CAI/II-IN-4 can be used for acute mountain sickness (AMS) research.
-
CAI/II-IN-1
0 ImagesCat. No.: HY-146385CAS No.: 2422028-82-6CAI/II-IN-1 (Compound 3h) is a human carbonic anhydrase I and II (hCA I/II) inhibitor with IC50 values of 0.047 µM and 0.024 µM against hCA I and hCA II, respectively.
-
HCAIX-IN-1
0 ImagesCat. No.: HY-146206CAS No.: 2389034-65-3HCAIX-IN-1 is a selective HCAIX inhibitor with a Ki value of 3.3 nM for hCA IX. HCAIX-IN-1 can be used in the study of solid tumors.
-
Carbonic anhydrase inhibitor 20
0 ImagesCat. No.: HY-161374CAS No.: 3034045-43-4Carbonic anhydrase inhibitor 20 (compound 11) is an inhibitor of piperazinosulfonamide carbonic anhydrase (Carbonic Anhydrase). The Ki of Carbonic anhydrase inhibitor 20 for hCA I, hCA II, hCA IX, and hCA XII are 47.6 nM, 36.5 nM, 8.3 nM, and 2.7 nM respectively.
-
CAII-IN-13
0 ImagesCat. No.: HY-181238CAII-IN-13 is a human carbonic anhydrase inhibitor, with a Ki of 65.9 nM against human carbonic anhydrase II and a Ki of 968.4 nM against human carbonic anhydrase I. CAII-IN-13 functionally inhibits the catalytic activities of human carbonic anhydrase II and human carbonic anhydrase I. CAII-IN-13 satisfies the Lipinski's rule of five and may possess physicochemical properties and pharmacokinetic profiles associated with in vivo bioavailability.
-
CAI/II-IN-12
0 ImagesCat. No.: HY-175972CAI/II-IN-12 is a potent and hCAI (IC50 = 7.12 μM, Ki = 9.26 μM) and hCAII (IC50 = 10.62 μM, Ki = 11.72 μM) dual inhibitor. CAI/II-IN-12 has a strong affinity for the active sites of CYP17A1, hCAI, and hCAII enzymes. Compound CAI/II-IN-12 exhibits rapid conformational stabilization, particularly in the CYP17A1 complex. CAI/II-IN-12 can be used for the study of prostate cancer therapy and glaucoma.
