ca xii

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.

hA2A/hCA XII modulator 1 is a potent antagonist of the hA2A adenosine receptor (hA2AAR), a triazolopyrazine that acts on hA2AAR (Ki: 6.4 nM), hA1AR (Ki: 4.819 μM), and hA3AR (Ki>30 μM). hA2A/hCA XII modulator 1 Also a potent inhibitor of human carbonic anhydrase XII (hCA XII), capable of acting on hCA XII (Ki: 6.2 nM), hCA II (Ki: 46 nM), hCA IX (Ki: 466 nM) and hCA I (Ki: 8.351 μM). hA2A/hCA XII modulator 1 exhibits potential for cancer research.

hCA XII/II/IX-IN-1 is a potent inhibitor of human carbonic anhydrase (hCA), acting on hCA I (IC50: 2.6 μM), hCA II (IC50: 0.004 μM), hCA IX (IC50: 0.005 μM), and hCA XII (IC50: 0.001 μM). hCA XII/II/IX-IN-1 exhibited anticancer effects.

Compound 4d, known as hCA XII-IN-6, is a potent inhibitor of human carbonic anhydrase XII (hCA XII) with a Ki value of 84.2 nM and exhibits anti-proliferative effects, making it useful in cancer research [1].

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).

CAIX Inhibitor S4 (S4) is an effective inhibitor of carbonic anhydrase IX/XII with a Ki of 7 nM and 2 nM, respectively. The Kis for CA II and CA I are 546 and 5600 nM.

hCAI/II-IN-6 is a selective and orally active inhibitor of human carbonic anhydrase (CA). hCAI/II-IN-6 inhibited hCA I, hCA II, hCA VII, and hCA XII with Ki values of 220, 4.9, 6.5, and ＞50,000 nM. hCAI/II-IN-6 showed anticonvulsant activity in vivo. hCAI/II-IN-6 can be used to study epilepsy. hCAI/II-IN-6 showed anticonvulsant activity in vivo. hCAI/II-IN-6 can be used to study epilepsy.

Enpp/Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.07, 0.74, 0.33, 0.68, respectively.Enpp/Carbonic anhydrase-IN-2 induced apoptosis.Enpp/Carbonic anhydrase-IN-2 has antiproliferative activity against cancer cells and low cytotoxicity against normal cells.

hCAIX-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 nM for hCA IX and 8.5 nM for hCA XII. It not only inhibits hCA activity but also releases NO, exerting dual anti-tumor effects. By reducing the expression of hCA IX and iron regulatory proteins, hCAIX-IN-23 regulates mitochondrial caspase activity and the ferroptosis pathway, thereby inducing apoptosis. This compound is utilized in research focused on renal cancer.

hCAIX XII-IN-14 (Compound 1i) is an inhibitor of hCAIX and hCAXII, with Ki values of 9.4 nM for hCAII, 5.6 nM for hCAIX, and 6.3 nM for hCAXII.

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.

M 12325 is used in the production of furosemide; rhinitis and occupational asthma were observed in workers from a lasamide production line.

Carbonic anhydrase inhibitor33 (11D) is a dual inhibitor that targets both CA (carbonic anhydrase) IX/XII and CDK6. It exhibits Ki values of 19.7 nM for hCA IX and 26.1 nM for hCA XII. Additionally, Carbonic anhydrase inhibitor33 (11D) can induce G1 phase cell cycle arrest and apoptosis, making it relevant for research in non-small cell lung cancer (NSCLC).

hCAIX/XII-IN-9 (compound 8) is a potent inhibitor of carbonic anhydrase (CA), with Ki values of 1658 nM for hCA I, 184.8 nM for hCA II, 8.9 nM for hCA IX, and 64.8 nM for hCA XII.

Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor targeting Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib. It exhibits anti-inflammatory and analgesic properties. The IC50 values for COX-1 and COX-2 are 10.4 μM and 50 nM, respectively. The Ki values for binding to various Carbonic Anhydrase isoforms are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII).

Anti-inflammatory agent 68 (compound 7b) is a dual inhibitor that targets Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib, exhibiting anti-inflammatory and analgesic properties. The IC50 values of Anti-inflammatory agent 68 for COX-1 and COX-2 are 12.6 μM and 60 nM, respectively. It binds to different Carbonic Anhydrase isoforms with Ki values of 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII).

hCAXII-IN-9 (Compound 3I) is a selective hCAXII inhibitor with Ki values of 28 nM for hCAXII, 7192.6 nM for hCAI, 188.6 nM for hCAII, and greater than 100000 nM for hCAIX. This compound may be utilized in anti-tumor research.

Carbonic anhydrase inhibitor20 (compound 11) is an inhibitor of piperazine-based sulfonamide carbonic anhydrase (Carbonic Anhydrase). It has Ki values of 47.6 nM, 36.5 nM, 8.3 nM, and 2.7 nM for hCA I, hCA II, hCA IX, and hCA XII, respectively.

CAIX/CAXII-IN-2 (compound 23) is a CAIX/CAXII inhibitor, exhibiting Ki values of 8.9 nM for CAIX and 5.3 nM for CAXII. It is applicable in cancer research.

hCA/VEGFR-2-IN-5 (compound 9) is an indolinone phenylsulfonamide and a potential dual inhibitor of hCA IX/XII and VEGFR-2, which are associated with cancer. The compound has IC50 values of 0.38 μM for VEGFR-2, 40 nM for hCA IX, and 3.2 nM for hCA XII. It exhibits antitumor activity.

MDK-4683, also known as CA IX/XII Inhibitor, is a hCA IX and hCA XII inhibitor.

Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) and, to a lesser extent, CAI, CAII, IV, VA, and VI (Kis = 138-1,347 nM), which may mediate its sustained vasodilatory activity. Dietary administration of chlorthalidone (8 mg per animal per day) reduces arterial hypertension and prevents or reduces ventricular hypertrophy induced by deoxycorticosterone acetate (DOCA) in salt-hypertensive rats. Formulations containing chlorthalidone have been used alone or in combination with other antihypertensive agents to lower arterial blood pressure and as adjuvants to address edema caused by cardiac or renal disorders.

Furagin (Furazidine) is a Nitrofuran derivative with anti-infective activity used for urinary tract infections.

hCAIX/XII-IN-5 (Coumarin 9a) is an inhibitor of carbonic anhydrase (CA) with excellent selectivity for hCA IX/XII, displaying Kis of 93.3 nM and 85.7 nM over hCA I and hCA II, respectively. It exhibits anti-proliferative activities in cancer cells, delaying the cell cycle and inducing apoptosis [1].