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Jingzhaotoxin-XII (JzTx-XII) TFA is a specific Kv4.1 channel inhibitor with an IC50 of 0.363 μM. Jingzhaotoxin-XII TFA interacts with the channels by modifying the gating behavior .
hCAIX/XII-IN-7 (compound 3e) is a potent hCA IX and XII inhibitor with Kis of 3.2 nM, 9.2 nM, 503.7 nM and 59 nM for hCA I, hCA II, hCA IX and hCA XII, respectively. hCAIX/XII-IN-7 has the potential for hypoxic tumors research .
hCAIX/XII-IN-9 (compound 8) is a potent carbonic anhydrase (CA) inhibitor with Ki values of 1658 nM, 184.8 nM, 8.9 nM, 64.8 nM for hCA I, hCA II, hCA IX, and hCA XII, respectively .
hCAIX/XII-IN-6 is an orally active carbonic anhydrase (CA) inhibitor. hCAIX/XII-IN-6 inhibits human CA isoforms hCA I, II, IV, IX, and XII with Ki values of 6697 nM, 2950 nM, 4093 nM, 4.1 nM and 7.7 nM, respectively. hCAIX/XII-IN-6 can be used for the research of rheumatoid arthritis (RA) .
hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research .
Jingzhaotoxin-XII (JzTx-XII) is a specific Kv4.1 channel inhibitor with an IC50 of 0.363 μM. Jingzhaotoxin-XII interacts with the channels by modifying the gating behavior .
hCA XII-IN-6 (compound 4d) is a potent hCA XII inhibitor with a Ki value of 84.2 nM. hCA XII-IN-6 has anti-proliferative activity. hCA XII-IN-6 can be used in research of cancer .
hCAIX/XII-IN-1 is a potent CAIX/XII inhibitor with the KI values of 0.48 µM and 0.83 µM for CAIX and CAXII, respectively. hCAIX/XII-IN-1 shows antiproliferative activity in vitro. hCAIX/XII-IN-1 induces apoptosis in MCF-7 cells .
hCAIX/XII-IN-11 (Compound 6c) is an inhibitor of hCA IX and hCA XII with a Ki value of 0.7 μM for both the isoforms. hCAIX/XII-IN-11 can be used for anticancer research .
hCAIX/XII-IN-15 (Compound 17β) is an inhibitor of hCA IX and hCA XII, with Kis of 0.42 and 4.37 μM respectively. hCAIX/XII-IN-15 has pro-apoptotic effect in multiple myeloma cells .
hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis .
hCAIX/XII-IN-10 (compound DK-8) is a carbonic anhydrase inhibitor. hCAIX/XII-IN-10 has potent inhibitory activity against tumor-associated membrane-bound isoforms hCA IX and XII, with Ki values of 32.5 nM and 29.2 nM .
hCAIX/XII-IN-8 (compound 3g) is a potent human (carbonic anhydrase) CA IX and XII inhibitor, with Ki values of 8.5 and 6.7 nM, respectively. hCAIX/XII-IN-8 shows particularly strong inhibitory activity against the tumor-associated membrane-bound isoforms, hCA IX and XII, while maintaining a high selectivity ratio over cytosolic off-target isoforms hCA I and II .
hCAIX/XII-IN-13 is an inhibitor of human carbonic anhydrases (hCA). hCAIX/XII-IN-13 shows good inhibitory activity against the tumor-related CA subtypes IX and XII, with Ki values of 0.08 µM and 0.06 µM, respectively. Under hypoxic conditions, hCAIX/XII-IN-13 can restore the cytotoxicity of Doxorubicin (HY-15142A) on MCF-7 cells, increasing G2/M phase cell cycle arrest and apoptosis .
hCAIX/XII-IN-4 (compound 6c) is a potent CAIX/XII inhibitor with the Ki values of 4.5 nM, 23.6 nM, >10000 nM and >10000 nM for CAXII, CAIX, CAI and CAⅡ, respectively .
(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury .
hCA XII/II/IX-IN-1 (Compound 3) is a potent human carbonic anhydrase (hCA) inhibitor with IC50 values of 2.6, 0.004, 0.005 and 0.001 μM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA XII/II/IX-IN-1 shows anticancer activity .
Dipsacus saponin XII (compound 6) is a triterpenoid saponin that stimulates the proliferation of UMR106 cells and increases alkaline phosphatase activity in UMR106 cells (4 μM) .
hCAIX/XII-IN-2 (compound 6a) is a potent and selective hCAIX and hCAXIIinhibitor with Ki values of >10000, >10000, 30.0, 3.6 nM for hCAI, hCAII, hCAIX and hCAXII, respectively .
hCAIX/XII-IN-3 (compound 6q) is a potent and selective hCAIX and hCAXIIinhibitor with Ki values of >10000, >10000, 66.2, 4.4 nM for hCAI, hCAII, hCAIX and hCAXII, respectively .
hCAII/XII-IN-1 (compound 4l) is a potent inhibitor of hCAXII and hCAII, with Kis of 8.4 and 9.4 nM, respectively. hCAXII-IN-11 plays an important role in cancer research .
hCAXII-IN-2 (compound 5i) is a potent human carbonic anhydrase XII (hCA XII) and hCA IX inhibitor with Ki values of 84.2 nM and 268.5 nM, respectively. hCAXII-IN-2 shows less active against hCA I and hCA II .
Carbonic anhydrase inhibitor 33 (11D) is a dual inhibitor of CA (Carbonic anhydrase) IX/XII and CDK6, with Ki values of 19.7 nM and 26.1 nM for hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 33 (11D) induces G1 arrest and apoptosis. Carbonic anhydrase inhibitor 33 (11D) can be used in the research for NSCLC .
SH7s is a potent carbonic anhydrases inhibitor, with Kis of 15.9 and 55.2 nM for hCA IX and hCA XII, respectively. SH7s is also a hypoxia-mediated chemo-sensitizing agent in colorectal cancer cells .
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .
Carbonic anhydrase inhibitor 7 (compound 5b) is a potent inhibitor of human carbonic anhydrase (hCA), with Kis of 6.5 nM, 7.1 nM, 72.1 nM, and 255.8 nM for hCA IX, hCA II, hCA XII and hCA I, respectively .
Carbonic anhydrase inhibitor 6 (compound 9b) is a potent inhibitor of human carbonic anhydrase (hCA), with Kis of 9.7 nM, 35.2 nM, 88.5 nM, and 91.8 nM for hCA IX, hCA II, hCA XII and hCA I, respectively .
CDK2-IN-11 (compound 9d) is a potent CDK2 inhibitor with an IC50 of 6.4 μM, and KI values of 23.4 nM, 56.3 nM and 44.3 nM for hCA II, hCA IX and hCA XII, respectively. CDK2-IN-11 can be used for researching anticancer .
Carbonic anhydrase inhibitor 18 (Compound 9) is a human carbonic anhydrase (hCA) isoform inhibitor, with Kis of 604.8, 333.6, 1.9 and 6.7 nM for hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 18 can be used for the research of cancer .
hCAIX-IN-11 (Compound 5d) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 32.7 and 623.5 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
hCAIX-IN-10 (Compound 6i) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 61.5 and 586.8 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
Carbonic anhydrase inhibitor 29 (Compound 5d) is an inhibitor targeting carbonic anhydrase IX (CA IX) and XII (CA XII), with inhibition constants (Ki) of 26.6 nM for CA IX and 10.9 nM for CA XII. Carbonic anhydrase inhibitor 29 can be used in anticancer research .
CAXII-IN-1 (Compound 17) is a selective CA XII inhibitor with Ki values of 3.8 nM and 56.0 nM against hCA XII and hCA IX, respectively. CAXII-IN-1 shows antitumor activity .
D-Pro-Phe-Arg-Chloromethylketone, a inhibitor of coagulation factor XII and plasma kallikrein, plays an important role in thrombosis and inflammation .
hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual Carbonic Anhydrase(CA) IX/XII with Ki values of 4.7 nM and 8.3 nM for hCA XII and hCA IX, respectively. hCA/VEGFR-2-IN-1 (compound 13a) is a potent VEGFR-2 inhibitor with IC50 values 26.3 nM. hCA/VEGFR-2-IN-1 has anticancer activity .
hCA/VEGFR-2 IN-5 (compound 9) is an indolone-phenylsulfonamide and a potential dual inhibitor of cancer-related hCA IX/XII and VEGFR-2. The IC50 values of hCA/VEGFR-2-IN-5 for VEGFR-2, hCA IX and hCA XII are 0.38 μM, 40 and 3.2 nM, respectively. hCA/VEGFR-2-IN-5 has antitumor activity .
These compounds show selective inhibition on tumor related subtypes HCA IX and XII, and are also considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research .
(E)-Dehydrodiconiferyl alcohol behaves as good hCA IX and hCA XII dual inhibitors . And (E)-Dehydrodiconiferyl alcohol suppresses the NF-κB nuclear translocation in connective tissue of healing area .
hCAI/II-IN-9 is a carbonic anhydrase inhibitor with inhibitory activity against human carbonic anhydrase isoforms I, II, IX, and XII. The inhibition constants (Ki) of hCAI/II-IN-9 for hCA I are in the range of 7.9-894 nM, for hCA II are in the range of 7.5-1645 nM, for hCA IX are in the range of 5.0-240 nM, and for hCA XII are in the range of 0.47-2.83 nM. hCAI/II-IN-9 may have potential applications in inhibiting a variety of pathologies involving these carbonic anhydrase isoforms .
Carbonic anhydrase inhibitor 24 (Compound 11) is a human carbonic anhydrase (carbonic anhydrase) inhibitor. Ki values of Carbonic anhydrase inhibitor 24 for hCAs IX and XII were 10.7 and 7.5 nM, respectively .
Indan-5-sulphonamide (Compd 1) is a carbonic anhydrase inhibitor and anticonvulsant agent, with Ki values of 0.039 nM (hCA XII), 6.5 nM (hCA XIV) and 5.1 nM (hCA XIV), respectively .
Carbonic anhydrase inhibitor 11 (compound VI) is a potent, selective carbonic anhydrase inhibitor. Carbonic anhydrase inhibitor 11 shows Ki values of 40, 39, 200 and 900 nM against CA II, IX, and XII, respectively .
Carbonic anhydrase inhibitor 5 is a potent and selective human carbonic anhydrase (hCA) inhibitor with IC50s of 42.9, 47,6 and 6.7 nM for hCA II, hCA IX and hCA XII, respectively .
HCAIX-IN-1 (compound 21e) is a potent and selective HCAIX inhibitor with KIs of 694.9, 126.6, 3.3, 9.8 nM for hCA I, hCA II, hCA IX, hCA XII, respectively .
hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells .
Carbonic anhydrase inhibitor 19 (compound 26a) inhibits the Glaucoma related isoforms hCA II and hCA XII with Kis of 9.4 nM and 6.7 nM, respectively. Carbonic anhydrase inhibitor 19 reveals an intraocular pressure (IOP) lowering effect .
hCA/VEGFR-2-IN-4 (compound 15b) is an indolinylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-4 inhibits VEGFR-2 (IC50=0.811 μM) and has high binding activity to hCAs, with Ki of 3.8 nM (hCA XII), 6.2 nM (hCA IX), 19.8 nM (hCA II), and 35.5 nM (hCA I), respectively. hCA/VEGFR-2-IN-4 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-2 inhibits VEGFR-2 (IC50=204 nM) and has high binding activity to hCAs, with Kis of 3.6 nM (hCA IX), 16.1 nM (hCA II), 16.7 nM (hCA XII), and 75.3 nM (hCA I), respectively. hCA/VEGFR-2-IN-2 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
hCAII-IN-2 (Compound 11f) is a cytosolic human carbonic anhydrase (hCA) inhibitor with Ki values of 261.4, 3.8, 19.6 and 45.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively .
U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model .
hCAIX-IN-21 (compound 16c) is a potent hCAIX inhibitor with KI values of 5.2, 3.5, 12.6, 13600 nM for hCAIX, hCA II, hCA XII, hCA I, respectively. hCAIX-IN-21 inhibits cathepsin B enzyme activity .
Carbonic anhydrase inhibitor 20 (compound 11) is an inhibitor of piperazinosulfonamide carbonic anhydrase (Carbonic Anhydrase). The Ki of Carbonic anhydrase inhibitor 20 for hCA I, hCA II, hCA IX, and hCA XII are 47.6 nM, 36.5 nM, 8.3 nM, and 2.7 nM respectively .
hCAII-IN-9 is a potent carbonic anhydrase inhibitor with IC50s of 1.18 μM (hCA II), 0.17 μM (hCA IX), and 2.99 μM (hCA XII), respectively. hCAII-IN-9 has no blood-brain barrier permeability .
Heparin calcium (MW 15000-19000) is an anticoagulant which binds reversibly to antithrombin III (ATIII) to form a heparin-antithrombin III complex. The complex binds to and irreversibly inactivates thrombin and other activated clotting factors IX, X, XI, and XII and prevents the transformation of fibrinogen to fibrin .
Heparin (Nadroparin) calcium (MW 3600-5000) is an anticoagulant which binds reversibly to antithrombin III (ATIII) to form a heparin-antithrombin III complex. The complex binds to and irreversibly inactivates thrombin and other activated clotting factors IX, X, XI, and XII and prevents the transformation of fibrinogen to fibrin .
hCAII-IN-3 (Compound 16) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 403.8, 5.1, 10.2 and 5.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-2 shows anticancer activity .
Furagin (Standard) is the analytical standard of Furagin. This product is intended for research and analytical applications. Furagin (Furazidine) is an analogue of Nitrofurantoin (HY-A0090) and has antibacterial activity. Furagin also inhibits human carbonic anhydrases (Kis: 260 and 57 nM for hCA IX and XII, respectively) .
hCA IX-IN-1 (Compound 6f) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 331.4, 28.4, 9.4 and 17.8 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-1 shows anticancer activity .
hCAXII-IN-10 (Compound 18b) is a dual inhibitor of human carbonic anhydrase isoform XII (hCAXII) and cathepsin B, with a Ki value of 2.2 nM. hCAXII-IN-10 can inhibit the role of hCAXII in providing tumors with a pH microenvironment conducive to tumor growth, and is expected to be used in the study of tumor diseases .
Compounds 6b and 14g showed significant inhibitory effect on tumor related subtype HCA IX with low nanomolar potency, while 6k was effective on HCA XII. Compounds 6b, 14g and 6k can be considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
Coumalic acid is an inhibitor of human carbonic anhydrase (hCA) (KI = 0.073 μM for hCA IX; KI = 0.083 μM for hCA XII). Coumalic acid is a valuable platform compound which can be prepared from malic acid. Coumalic acid can be used in the flavorings, fragrances and cosmetics industries, as polymer components, and pharmaceutical scaffolds. Coumalic acid displays antibronchial and antimalarial activity .
CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity .
HDAC-IN-87 (Compound XII6) is a nonselective HDAC inhibitor, with pIC50 of 6.9 (HDAC4) and 5.8 (HDAC6) respectively. HDAC-IN-87 has fungicidal activity against P. sorghi and P. pachyrhizi. HDAC-IN-87 shows an acute oral LD50 of greater than 500 mg/kg in male and female rats .
CAIX/CAXII-IN-4 (Compound 7h) is the inhibitor for carbonic anhydrase (CA) that binds CA IX, CA XII and CA II with Ki of 1.324 μM, 0.435 μM and 3.035 μM. CAIX/CAXII-IN-4 exhibits board-spectrum antitumor efficacy, inhibits the proliferation of CNS cancer U251 with GI50 of 0.361 μM .
Carbonic anhydrase inhibitor 14 (Compound 8b) is a carbonic anhydrase (CA) inhibitor with Ki values of 1203, 99.7, 9.4 and 27.7 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 14 can also inhibit CDK2 with an IC50 of 20.3 μM. Carbonic anhydrase inhibitor 14 shows antitumor activity .
Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
4-(Chloromethyl)-7-hydroxycoumarin (compound 4) is a hydroxycoumarin derivative with potent antioxidant effect and high hydroxyl radical-scavenging property. 4-(Chloromethyl)-7-hydroxycoumarin contains a methyl group and a chlorine group in the heterocyclic ring. A series of coumarins incorporating hydroxy-, chloro- and/or chloromethyl-moieties has been investigated as potent inhibitors of the zinc enzyme carbonic anhydrase, expecially tumor-associated isoforms CA IX and XII .
COX-2-IN-31 (compound 7b) is an orally active and dual inhibitor of COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM). COX-2-IN-31 also inhibits transmembrane hCA IX(Ki=48.9 nM) and hCA XII(Ki=5.8 nM) activity. COX-2-IN-31 exhibits anti-inflammatory and analgesic activity .
hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research .
hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy .
Enpp/Carbonic anhydrase-IN-2 (compound 1i) is a potent Enpp and carbonic anhydrase inhibitor with IC50s 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-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 and 8.5 nM for hCA IX and hCA XII, respectively. In addition to inhibiting hCA activity, hCAIX-IN-23 releases NO, exhibiting dual antitumor activity. hCAIX-IN-23 induces apoptosis by regulating mitochondrial caspase activity and the ferroptosis pathway (ferroptosis) through the downregulation of hCA IX and iron-regulatory protein expression. hCAIX-IN-23 is useful for renal cancer research .
Chlorthalidone Impurity G (Chlorthalidone EP Impurity G) is a potential impurity found in commercial preparations of chlorthalidone with moderate antihypertensive effects. Chlorthalidone is a thiazide diuretic that inhibits the Na+/Cl- cotransporter in the distal tubule of the kidney, thereby preventing sodium and chloride reabsorption, resulting in decreased plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including isoenzymes CAVB, VII, IX, XII, and XIII (Kis=2.8-23 nM) and to a lesser extent CAI, CAII, IV, VA, and VI (Ki=138-1,347 nM), mediating vasodilatory activity.
hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity. hCA/Wnt/β-catenin-IN-1 also inhibits Wnt/β-catenin signaling pathway. hCA/Wnt/β-catenin-IN-1 inhibits cancer cell viability, including the NCI/ADR-RES DOX-resistant cell line .
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect .
Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor of carbonic anhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), and has anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 67 has IC50s of 10.4 μM and 50 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 67 binding to different isoforms of carbonic anhydrase 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 of carbonic anhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), with anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 68 has IC50s of 12.6 μM and 60 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 68 binding to different isoforms of carbonic anhydrase are 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII) .
CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
Heparin (Nadroparin) calcium (MW 3600-5000) is an anticoagulant which binds reversibly to antithrombin III (ATIII) to form a heparin-antithrombin III complex. The complex binds to and irreversibly inactivates thrombin and other activated clotting factors IX, X, XI, and XII and prevents the transformation of fibrinogen to fibrin .
Heparin calcium (MW 15000-19000) is an anticoagulant which binds reversibly to antithrombin III (ATIII) to form a heparin-antithrombin III complex. The complex binds to and irreversibly inactivates thrombin and other activated clotting factors IX, X, XI, and XII and prevents the transformation of fibrinogen to fibrin .
Jingzhaotoxin-XII (JzTx-XII) TFA is a specific Kv4.1 channel inhibitor with an IC50 of 0.363 μM. Jingzhaotoxin-XII TFA interacts with the channels by modifying the gating behavior .
D-Pro-Phe-Arg-Chloromethylketone, a inhibitor of coagulation factor XII and plasma kallikrein, plays an important role in thrombosis and inflammation .
Jingzhaotoxin-XII (JzTx-XII) is a specific Kv4.1 channel inhibitor with an IC50 of 0.363 μM. Jingzhaotoxin-XII interacts with the channels by modifying the gating behavior .
Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research .
Coumalic acid is an inhibitor of human carbonic anhydrase (hCA) (KI = 0.073 μM for hCA IX; KI = 0.083 μM for hCA XII). Coumalic acid is a valuable platform compound which can be prepared from malic acid. Coumalic acid can be used in the flavorings, fragrances and cosmetics industries, as polymer components, and pharmaceutical scaffolds. Coumalic acid displays antibronchial and antimalarial activity .
Dipsacus saponin XII (compound 6) is a triterpenoid saponin that stimulates the proliferation of UMR106 cells and increases alkaline phosphatase activity in UMR106 cells (4 μM) .
(E)-Dehydrodiconiferyl alcohol behaves as good hCA IX and hCA XII dual inhibitors . And (E)-Dehydrodiconiferyl alcohol suppresses the NF-κB nuclear translocation in connective tissue of healing area .
CA12 (or carbonic anhydrase 12) plays a crucial role in the reversible hydration of carbon dioxide, catalyzing its conversion into bicarbonate ions and protons. This enzymatic activity is essential for key physiological processes, including regulating pH and maintaining acid-base balance. CA12/Carbonic Anhydrase 12 Protein, Human (HEK293, His) is the recombinant human-derived CA12/Carbonic Anhydrase 12 protein, expressed by HEK293 , with C-His labeled tag.
Coagulation factor XII (F12) is a serum glycoprotein that plays multiple roles in initiating blood coagulation, fibrinolysis, and the production of bradykinin and angiotensin. It is involved in these complex processes, including cleavage of prekallikrein to form kallikrein, which subsequently cleaves factor XII initially to α-factor XIIa and then, after trypsin cleavage, to β-factor XIIa. Coagulation Factor XII/F12 Protein, Pig (His) is the recombinant pig-derived Coagulation Factor XII/F12 protein, expressed by E. coli , with N-6*His labeled tag.
CA12 (or carbonic anhydrase 12) plays a crucial role in the reversible hydration of carbon dioxide, catalyzing its conversion into bicarbonate ions and protons. This enzymatic activity is essential for key physiological processes, including regulating pH and maintaining acid-base balance. CA12/Carbonic Anhydrase 12 Protein, Human (P.pastoris, His) is the recombinant human-derived CA12/Carbonic Anhydrase 12 protein, expressed by P. pastoris , with N-6*His labeled tag.
Carbonic Anhydrase 12 Protein, Mouse (HEK293, His), a recombinant Mouse Carbonic Anhydrase 12 produced in HEK293 cells, has a His tag at the N-terminus. Hypoxic tumors overexpress two carbonic anhydrases (CA), CA IX and XII, involved in complex processes connected to tumorigenesis (pH regulation, metabolism, invasion, and dissemination of the tumor).
Coagulation factor XII (F12) is a serum glycoprotein that plays multiple roles in initiating blood coagulation, fibrinolysis, and the production of bradykinin and angiotensin. It is involved in these complex processes, including cleavage of prekallikrein to form kallikrein, which subsequently cleaves factor XII initially to α-factor XIIa and then, after trypsin cleavage, to β-factor XIIa. Coagulation Factor XII/F12 Protein, Pig (P. pastoris, His) is the recombinant pig-derived F12/Coagulation Factor XII, Pig, expressed by P. pastoris , with N-6*His labeled tag.
hCAIX-IN-21 (compound 16c) is a potent hCAIX inhibitor with KI values of 5.2, 3.5, 12.6, 13600 nM for hCAIX, hCA II, hCA XII, hCA I, respectively. hCAIX-IN-21 inhibits cathepsin B enzyme activity .
hCAXII-IN-10 (Compound 18b) is a dual inhibitor of human carbonic anhydrase isoform XII (hCAXII) and cathepsin B, with a Ki value of 2.2 nM. hCAXII-IN-10 can inhibit the role of hCAXII in providing tumors with a pH microenvironment conducive to tumor growth, and is expected to be used in the study of tumor diseases .
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