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].

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.

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).

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.

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.

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.

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].

CAXII-IN-1 (Compound 17) is a selective inhibitor of CA XII with antitumor activity, exhibiting Ki values of 3.8 nM for hCA XII and 56.0 nM for hCA IX [1].

Carbonic anhydrase inhibitor 14 (Compound 8b) is a potent CA inhibitor, exhibiting K i values of 1203, 99.7, 9.4, and 27.7 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. Additionally, it effectively inhibits CDK2 with an IC 50 of 20.3 μM and demonstrates significant antitumor activity [1].

HCAIX-IN-2 (compound 9d) is a selective inhibitor of carbonic anhydrase, targeting hCA IX (Ki: 24.6 nM) and hCA XII (Ki: 45.3 nM).

Carbonic anhydrase inhibitor 11 (compound VI) is a potent, selective inhibitor of carbonic anhydrase, targeting CA II (Ki: 40 nM), CA IX (Ki: 39 nM), and CA XII (Ki: 900 nM).

hCAXII-IN-4 is a selective and potent CA XII inhibitor with a Ki value of 6.4 nM for human CA XII.

Enpp Carbonic anhydrase-IN-2 is a potent Enpp and carbonic anhydrase inhibitor with IC 50 s of 1.13, 1.07, 0.74, 0.33, 0.68 for NPP1, NPP2, NPP3, CA-IX, CA-XII respectively. Enpp Carbonic anhydrase-IN-2 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp Carbonic anhydrase-IN-2 induces Apoptosis .

hCAIX XII-IN-6, an orally active carbonic anhydrase (CA) inhibitor, targets human CA isoforms hCA I, II, IV, IX, and XII with inhibition constants (K i) of 6697 nM, 2950 nM, 4093 nM, 4.1 nM, and 7.7 nM, respectively. This compound is utilized in rheumatoid arthritis (RA) research.

COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].

hCA VEGFR-2-IN-1 (compound 13a) is a potent dual inhibitor targeting both Carbonic Anhydrase (CA) IX XII and Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), exhibiting Ki values of 4.7 nM for hCA XII and 8.3 nM for hCA IX, alongside an IC50 of 26.3 nM for VEGFR-2, and demonstrating anticancer activity [1].

Compound 3e (hCAIX XII-IN-7) is a potent inhibitor of human carbonic anhydrase (hCA) isozymes IX and XII, displaying inhibitory constants (Kis) of 503.7 nM for hCA IX and 59 nM for hCA XII, while also showing activity against hCA I and II with Kis of 3.2 nM and 9.2 nM, respectively. It holds potential for research into hypoxic tumors [1].