ca-ii

CA-II/Dkk1-IN-1 (Compound 5d) is a dual inhibitor of CA-II and Dkk1, with an IC50 of 6.90 nM for CA-II. It exhibits significant antioxidant activity and exceptional DNA binding capability. CA-II/Dkk1-IN-1 is applicable in cancer research, including esophageal cancer, renal cancer, and lung cancer.

CA-II/TNAP-IN-1 is a novel 1,3-disubstituted thiourea derivative that acts as a dual inhibitor of carbonic anhydrase II (CA-II) and tissue-nonspecific alkaline phosphatase (TNAP). The compound is an essential tool for investigating cancer metabolism and enzyme-mediated tumor microenvironment regulation, aiming to enhance anti-tumor efficacy by jointly inhibiting key enzymes involved in pH regulation and mineralization.

U-104 (NSC-213841) is an effective carbonic anhydrase (CA) inhibitor for CA IX( Ki=45.1 nM) and CA XII(Ki=4.5 nM).

CAII-IN-12 (compound 6c) is a potent and selective inhibitor of carbonic anhydrase (CA) II and VII, with inhibition constants hCA II Ki= 47.8 nM and hCA VII Ki= 3.6 nM, and exhibits antiepileptic activity. It is selective for hCA I with a Ki of 370 nM. In mouse models of epilepsy induced by Pentylenetetrazol and Pilocarpine, CAII-IN-12 demonstrates strong anticonvulsant effects. Additionally, it increases the expression of KCC2 in the hippocampus, maintains neuronal integrity, and reduces mTOR activity. CAII-IN-12 is applicable for epilepsy research.

CAII-IN-11 (Compound A1) is a dual-targeted compound that includes an hCA II inhibitor segment (IC₅₀= 2 nM) and a NO donor component. It also shows inhibitory activity against hCA IX, hCA XII, and hCA I, with IC₅₀ values of 6, 3, and 152 nM, respectively. CAII-IN-11 significantly elevates cGMP levels in human trabecular meshwork cells. Furthermore, it reduces apoptosis of retinal ganglion cells by decreasing oxidative stress (ROS levels), inhibiting astrocytes, and NLRP3 inflammasome activation. In a rabbit model, CAII-IN-11 demonstrates intraocular pressure-lowering activity, making it a potential candidate for glaucoma research.

CAII-IN-1 (compound 3n) is a thiosemicarbazide derivative that acts as a potent and selective inhibitor of carbonic anhydrase-II (CA-II), with an IC50 value of 10.3 μM for bovine CA-II. This compound (CAII-IN-1) is useful in research on carbonic anhydrase-associated biological disorders [1].

CAII-IN-3 (compound 3h) is a thiosemicarbazone derivative that potently inhibits carbonic anhydrase-II (CA-II), exhibiting an IC50 value of 13.4 μM [1].

CAII-IN-2 (compound 3g) is a thiosemicarbazide derivative. CAII-IN-2 is a potent, selective carbonic anhydrase-II (CA-II) inhibitor with an IC50 of 12.1 μM for bovine CA-II. CAII-IN-2 has research value in carbonic anhydrase related biological disorders.

CAII/CAXII-IN-1 (compound 8d) is an inhibitor of CAII and CAXII, with IC50 values of 0.38 µM for CAII and 0.61 µM for CAXII.

CAII/VII-IN-1 is an orally active inhibitor of hCA II (KI= 12.3 nM) and hCA VII (KI= 22.6 nM), showing no significant activity towards hCA I. In vivo, it demonstrates excellent neuroprotective properties in a Pilocarpine-induced epilepsy model. It upregulates KCC2 and inhibits mTOR, contributing to its neuroprotective effects. CAII/VII-IN-1 exhibits no significant neurotoxicity or changes in liver and kidney function, making it a useful compound for epilepsy research.

hCA-I/hCA-II-IN-1 (Compound P4) is a potent dual inhibitor of human carbonic anhydrase I (hCA-I) and human carbonic anhydrase II (hCA-II), with Ki values of 0.22 μM and 0.33 μM respectively. hCA-I/hCA-II-IN-1 is useful for research into diseases related to CA enzymes, including glaucoma, hypertension, and ulcers.

hCA-I/hCA-II-IN-2 (compound 5 k) is a potent inhibitor of human carbonic anhydrase I (hCA-I) and II (hCA-II), with IC50 values of 89.25 nM and 54.50 nM, respectively, for hCA I and hCA II.

Dorzolamide hydrochloride (MK507 hydrochloride) is the hydrochloride salt form of dorzolamide, an inhibitor of carbonic anhydrase, a zinc-containing enzyme that catalyzes the rapid conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. Distributed throughout many cells and tissues, various carbonic anhydrases play important roles in mineral and metabolic homeostasis.

Methazolamide (CL 8490) is a carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.

Brinzolamide (AL-4862) is a Carbonic Anhydrase Inhibitor. Its mechanism of action involves inhibiting the enzyme Carbonic Anhydrase.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Histone acetyltransferase p300 Inhibitor 4c is a 2-aminothiazole derivative. Histone acetyltransferase p300 Inhibitor 4c inhibited hCA I, hCA II, AChE and BChE with Ki values of 0.008 ± 0.001, 0.124 ± 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 µM. 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 μM.

hCAII-IN-8 is a highly selective inhibitor of carbonic anhydrase (CA) with an IC50 value of 0.18 μM for hCA II.

Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent inhibitor of Enpp and carbonic anhydrase, exhibiting IC50s of 1.36, 1.35, 3.00, 0.88, and 1.02 µM for NPP1, NPP2, NPP3, CA-II, and CA-IX respectively. Enpp/Carbonic anhydrase-IN-1 also demonstrates selective antiproliferative activity for cancer cells.

hCAII-IN-9 is a potent carbonic anhydrase inhibitor with IC50 values of 1.18 μM for hCA II, 0.17 μM for hCA IX, and 2.99 μM for hCA XII. It is not blood-brain barrier permeable.

hCAI/II/IV-IN-28(WAY-638358) is a potent carbonic anhydrase inhibitor with potential anticonvulsant activity.

CAⅡ-IN-1 (compound 2i) is an inhibitor of the CA Ⅱ isozyme, exhibiting an IC50 of 0.44 µM. This compound is utilized in metabolic research.

hCA I-IN-4 (Compound 14) is an inhibitor of carbonic anhydrase and cholinesterase, effectively inhibiting hCA I, hCA II, AChE, and BChE with Ki values of 29.94 nM, 17.72 nM, 21.21 nM, and 7.65 nM, respectively. It also demonstrates cytotoxicity in BT-549 cells, with an IC50 of 16.59 μM.

AChE/hCA I-IN-1 (Compound L3) is an inhibitor of acetylcholinesterase (AChE) and carbonic anhydrase (CA), effectively inhibiting AChE, hCA I, and hCA II with IC50 values of 302 nM, 265 nM, and 283 nM, respectively.