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.

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-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.

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.

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.

hCAI/II-IN-10 (Compound 5d) is an inhibitor of human carbonic anhydrase I and II (hCA I and hCA II), with IC50 values of 4.32 nM and 3.89 nM, respectively.

BChE-IN-38 (compound 13) is a potent BChE inhibitor, with Ki values of 62.05, 28.78, 14.09, and 1.15 nM for hCAI, hCAII, AChE, and BChE, respectively. BChE-IN-38 also demonstrates cytotoxic activity.

hCAII/XII-IN-1 (compound 4l) is a potent inhibitor of hCAXII and hCAII, with Ki values of 8.4 nM and 9.4 nM, respectively. It plays a significant role in cancer research.

CAIX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. It exhibits anticancer activity by inhibiting the growth of MCF-7 breast cancer cells (IC50 of 22.33 μM) and mouse fibroblast cell line 3T3, where cell viability is reduced to below 40% at a concentration of 100 μM. This compound is applicable for research in the field of cancer treatment.

CAIX/CAXII-IN-4 (Compound 7h) is an inhibitor of carbonic anhydrase (CA) that binds to CAIX, CA XII, and CAII with Ki values of 1.324 μM, 0.435 μM, and 3.035 μM, respectively. This compound exhibits broad-spectrum anti-tumor activity and inhibits the proliferation of central nervous system tumor cells U251, with a GI50 of 0.361 μM.