caix

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.

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/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.

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.

STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). It induces ferroptosis by elevating reactive oxygen species (ROS) and lipid peroxides. This compound also inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 is applicable for research in triple-negative breast cancer (TNBC).

CAIX-IN-4 (Compound 8b) is a selective inhibitor of carbonic anhydrase IX (CAIX) with an IC50 value of 0.32 μM. It holds potential for research in cancer, such as renal cell carcinoma.

CAIX/CAXII-IN-3 (compound 11) serves as an inhibitor for CAIX/CAXII, exhibiting an IC50 value of less than 65 nM. Additionally, this compound effectively inhibits the proliferation of human melanoma cells.

hCAIX/XII-IN-4 (compound 6c) is a highly potent inhibitor of CAIX/XII, exhibiting Ki values of 4.5 nM for CAXII, 23.6 nM for CAIX, and >10000 nM for both CAI and CAⅡ, respectively [1].

hCAIX-IN-8 (compound 7i) is a highly potent and selective inhibitor of hCAIX with an IC50 value of 0.024 μM, and also inhibits CAII and CAVA with IC50 values of 1.99 μM and 1.10 μM, respectively. It exhibits anti-proliferative effects, low toxicity, reduces epithelial-to-mesenchymal transitions, promotes apoptosis, and inhibits cell migration and colonization potential [1].

hCAIX/XII-IN-1, a potent inhibitor of both CAIX and CAXII, exhibits KI values of 0.48 μM for CAIX and 0.83 μM for CAXII, respectively. This compound demonstrates antiproliferative activity in vitro and induces apoptosis in MCF-7 cells [1].

hCAIX-IN-12 is an effective hCAIX inhibitor, IC50 for CAIX and CAII is 0.74 and 10.78 μM , respectively. hCAIX-IN-12 inhibits cell proliferation and induces apoptosis. HCAIX-IN-12 can increase the generation of ROS. HCAIX-IN-12 has research potential in colorectal cancer (CRC).

hCAIX-IN-13 (Pt2), a Carbonic Anhydrase IX (CAIX) inhibitor, demonstrates a notable IC50 value of 6.57 μM, efficiently impeding cancer cell growth and promoting apoptosis. It is valuable for cancer research [1].

hCAIX/XII-IN-13 functions as an inhibitor targeting specific human carbonic anhydrases (hCA) IX and XII, crucial in tumor-related processes. Demonstrating efficacy, this compound offers inhibitory K i values of 0.08 µM for IX and 0.06 µM for XII. Additionally, under hypoxic conditions, hCAIX/XII-IN-13 enhances the effectiveness of Doxorubicin on MCF-7 cells by promoting G2/M phase cell cycle arrest and increasing apoptosis.

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.

hCAIX/XII-IN-15 (Compound 17β) is an inhibitor of hCA IX and hCA XII, exhibiting Ki values of 0.42 and 4.37 μM, respectively. It demonstrates a pro-apoptotic effect in multiple myeloma cells.

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.

hCAIX/XII-IN-10 (compound DK-8) is an inhibitor of Carbonic Anhydrase, showing potent inhibitory activity against the tumor-associated membrane-bound isoforms hCA IX and XII, with Ki values of 32.5 nM and 29.2 nM, respectively.

hCAIX-IN-20 (compound APBS-5m) is a potent inhibitor of carbonic anhydrase IX (hCA IX), with a Ki of 2.7 nM, playing a significant role in cancer research.

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].

hCAIX-IN-5 was a selective hCAIX inhibitor, inhibiting hCAI, hCAII, hCAIV, and hCAIX with Ki values of >10000, >10000, 130.7, and 829.1 nM, respectively.

hCAIX-IN-7 (compound 6c) is a potent and selective inhibitor of the tumor-associated isoform hCAIX, with inhibition constants (KIs) of >10000 nM for hCAI and hCAII, 43.0 nM for hCAIV, and 410.6 nM for hCAIX [1].

hCAIX/XII-IN-2 (compound 6a) is a potent and selective inhibitor of hCAIX and hCAXII, with Ki values of >10000 nM for hCAI and hCAII, and 30.0 nM and 3.6 nM for hCAIX and hCAXII respectively [1].

Compounds 6B and 14g demonstrated significant inhibitory effects on the tumor-related subtype [HCA IX] with low nanomolar potency, while 6K was effective on [HCA XII]. These compounds can be considered leading molecules for developing future cancer therapeutic drugs based on new mechanisms of action.