Search Result
Results for "
human+carbonic+anhydrase
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0553
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- HY-77036
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Furagin
1 Publications Verification
Furazidine; Furazidin
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Antibiotic
Bacterial
Carbonic Anhydrase
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Infection
Cancer
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Furagin (Furazidine), an analogue of Nitrofurantoin (HY-A0090), is an antibiotic with antibacterial activity against ESKAPE pathogens with MIC values of 0-32 µg/mL. Furagin inhibits human Carbonic anhydrases . Furagin is promising for research of cancer and urinary tract infections (UTIs) .
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- HY-32004
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Endogenous Metabolite
Parasite
Hydroxycarboxylic Acid Receptor (HCAR)
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Infection
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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 .
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- HY-109056
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R-1206
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Drug Intermediate
HIV
Reverse Transcriptase
Carbonic Anhydrase
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Infection
Cancer
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Elsulfavirine (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine is used in studies related to HIV-1 infection and liver cancer .
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- HY-W013316
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Carbonic Anhydrase
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Endocrinology
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Lasamide is a potent human Carbonic Anhydrase inhibitor with Ki values of 7.54 and 2.76 nM for hCAXII and hCAIX, respectively .
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- HY-W008343
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Endogenous Metabolite
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Metabolic Disease
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1,3-Dimethyluracil is a pyrimidone derives from a uracil. 1,3-Dimethyluracil found occasionally in human urine. 1,3-Dimethyluracil shows inhibition activity against hCA I and hCA II (human carbonic anhydrase) with Ki of 316.2 μM and 166.4 μM, respectively .
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- HY-W012168
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Carbonic Anhydrase
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Metabolic Disease
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4-Chloro-3-sulfamoylbenzoic acid is a weak inhibitor of human carbonic anhydrase isoforms hCA I, hCA II, hCA IV, and hCA IX, and a synthesis intermediate for carbonic anhydrase inhibitors. 4-Chloro-3-sulfamoylbenzoic acid is the major metabolite of tripamide detected in tissues, urine, and feces of rats and rabbits following Tripamide (HY-106570) administration. 4-Chloro-3-sulfamoylbenzoic acid can be used for the study of carbonic anhydrase inhibition and species differences in drug metabolism .
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- HY-147986
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Carbonic Anhydrase
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Cancer
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hCA I-IN-2 (Compound 6d) is a selective human carbonic anhydrase I (hCA I) inhibitor with Ki values of 18.8, 375.1, 1721 and 283.9 nM against hCA I, hCA II, hCAIX and hCAXII, respectively .
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- HY-147985
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Carbonic Anhydrase
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Cancer
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hCA I-IN-1 (Compound 6q) is a human carbonic anhydrase I (hCA I) inhibitor with Ki values of 38.3, 716.4, 940.1 and 192.8 nM against hCA I, hCA II, hCAIX and hCAXII, respectively .
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- HY-147984
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Carbonic Anhydrase
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Cancer
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hCAXII-IN-3 (Compound 6o) is a selective human carbonic anhydrase XII (hCAXII) inhibitor with a Ki of 10.0 nM .
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- HY-144376
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Carbonic Anhydrase
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Cancer
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Carbonic anhydrase inhibitor 4 is carbonic anhydrase photoprobe/inhibitor. Carbonic anhydrase inhibitor 4 is against human carbonic anhydrases (hCA I-XIV) with Ki values of 640-1166 nM .
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- HY-175847
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Carbonic Anhydrase
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Cancer
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hCA-I/ HCA-II-IN-2 (compound 5 k) is an effective inhibitor of human carbonic anhydrase I (hCA-I) and II (hCA-II). The IC50 for hCA I and hCA II are 89.25 and 54.50 nM respectively .
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- HY-B0553S
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L584601-d6
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Isotope-Labeled Compounds
Carbonic Anhydrase
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Inflammation/Immunology
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Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders .
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- HY-77036R
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Furazidine (Standard); Furazidin (Standard)
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Reference Standards
Antibiotic
Bacterial
Carbonic Anhydrase
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Infection
Cancer
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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) .
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- HY-178017
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Cholinesterase (ChE)
Carbonic Anhydrase
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Neurological Disease
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BChE/hCA II-IN-1 (Compound 20) is a dual-functional inhibitor of Butyrylcholinesterase (BChE) and human carbonic anhydrase II (hCA II) with IC50s of 76.50 and 10.69 μM for BChE and hCA II, respectively. BChE/hCA II-IN-1 can be used for neurodegenerative diseases like Alzheimer's and glaucoma research .
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- HY-174252
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DNA/RNA Synthesis
HSV
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Infection
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HSV-1/HSV-2-IN-3 inhibits the herpes-simplex-virus (HSV) helicase-primase complex, blocking the coordinated DNA-unwinding and primer-synthesis steps required for viral genome replication. HSV-1/HSV-2-IN-3 exhibits an EC50 of 7.0 nM against HSV-2 in a gD-immunofluorescence cell assay containing 2 % FBS and 57.5 nM when 10 % human serum is present. HSV-1/HSV-2-IN-3 achieves an EC50 of 1.1 nM in a qPCR replication assay. HSV-1/HSV-2-IN-3 shows strong selectivity over human carbonic-anhydrase off-targets (IC50 ≈ 2.9 µM for hCA II and > 35 µM for hCA I). HSV-1/HSV-2-IN-3 can be studied in anti-HSV research .
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- HY-174835
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Carbonic Anhydrase
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Cardiovascular Disease
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hCA-I/hCA-II-IN-1 (Compound P4) is a potent dual human carbonic anhydrase I (hCA-I) and human carbonic anhydrase II (hCA-II) inhibitor with Ki values of 0.22 μM and 0.33 μM, respectively. hCA-I/hCA-II-IN-1 can be used in research on diseases related to CA enzymes such as glaucoma, hypertension, and ulcers .
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- HY-147353
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Carbonic Anhydrase
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Others
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Phenylsulfamide (Compound 10) is a human carbonic anhydrase-II (hCA-II) inhibitor with a Kd of 45.50 μM and a Ki of 79.60 μM .
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- HY-159568
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Carbonic Anhydrase
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Cancer
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hCAIX-IN-22 is a highly selective inhibitor of human carbonic anhydrase (hCA) isoform XII (Ki=9.7 nM) with anticancer activity .
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- HY-W013316R
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Reference Standards
Carbonic Anhydrase
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Endocrinology
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Lasamide (Standard) is the analytical standard of Lasamide. This product is intended for research and analytical applications. Lasamide is a potent human Carbonic Anhydrase inhibitor with Ki values of 7.54 and 2.76 nM for hCAXII and hCAIX, respectively .
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- HY-172103
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Carbonic Anhydrase
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Others
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hCAI/II-IN-10 (Compound 5d) is a human carbonic anhydrase I and II (hCA I and hCA II) inhibitor with IC50 values are 4.32 and 3.89 nM respectively .
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- HY-W306065
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Carbonic Anhydrase
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Cancer
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hCAI/II/XII-IN-1 (compound 7) is a human carbonic anhydrase hCAI/II/XII inhibitor, with Ki values of 78.5, 9.1, 605, 7.7 and 3.7 nM .
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- HY-161686
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-144268
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Carbonic Anhydrase
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Cancer
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hCAII-IN-7 (Compound R-13) is a potent human carbonic anhydrase (hCA) inhibitor with Kis of 60.7, 320.7, 2298, and 35.2 nM for hCA I, II, IV and IX, respectively .
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- HY-144639
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- HY-146385
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Carbonic Anhydrase
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Cancer
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hCAI/II-IN-1 (Compound 3h) is a human carbonic anhydrase I and II (hCA I/II) inhibitor with IC50 values of 0.047 µM and 0.024 µM against hCA I and hCA II, respectively .
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- HY-144641
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-144640
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-146355
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-147829
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-12155
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Sodium Channel
Calcium Channel
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Neurological Disease
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JNJ-26990990 is a broad-spectrum antiepileptic agent with oral activity. JNJ-26990990 can inhibit voltage-gated Na + channels and N-type Ca 2+ channels, but has a very weak inhibitory effect on human carbonic anhydrase-II (IC50 = 110 μM) .
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- HY-146008
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-163268
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-146007
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-159129
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Ser/Thr Protease
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Cancer
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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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- HY-W008343R
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Reference Standards
Endogenous Metabolite
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Metabolic Disease
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1,3-Dimethyluracil is a pyrimidone derives from a uracil. 1,3-Dimethyluracil found occasionally in human urine. 1,3-Dimethyluracil shows inhibition activity against hCA I and hCA II (human carbonic anhydrase) with Ki of 316.2 μM and 166.4 μM, respectively .
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- HY-144264
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Carbonic Anhydrase
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Endocrinology
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hCAII-IN-6 (Compound S-13) is a potent human carbonic anhydrase II (hCA II) inhibitor with a Ki of 4.4 nM. hCAII-IN-6 also inhibits other hCAs isoforms I, IV and IX, with Ki values of 9.2 nM, 480.2 nM and 14.7 nM, respectively. hCAII-IN-6 can be used for glaucoma research .
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- HY-147799
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-B0553R
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- HY-W748430
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Furazidine-13C3; Furazidin-13C3
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Isotope-Labeled Compounds
Carbonic Anhydrase
Bacterial
Antibiotic
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Infection
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Furagin- 13C3 (Furazidine- 13C3) is the 13C-labeled Furagin (HY-77036). Furagin (Furazidine), an analogue of Nitrofurantoin (HY-A0090), is an antibiotic with antibacterial activity against ESKAPE pathogens with MIC values of 0-32 μg/mL. Furagin inhibits human Carbonic anhydrases . Furagin is promising for research of cancer and urinary tract infections (UTIs) .
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- HY-156181
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Carbonic Anhydrase
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Cancer
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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 .
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- HY-W074975R
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5-Amino-1,3,4-thiadiazole-2-sulfonamide (Standard)
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Carbonic Anhydrase
Reference Standards
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Cancer
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CL 5343 (Standard) is the analytical standard of CL 5343. This product is intended for research and analytical applications. CL 5343 (5-Amino-1,3,4-thiadiazole-2-sulfonamide) is an inhibitor of human carbonic anhydrase B (HCA-B). CL 5343 can serve as a CA9 ligand to achieve the targeted delivery of maytansinoid to the cell membrane of SKRC52 renal cancer cells .
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- HY-148135
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Carbonic Anhydrase
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Neurological Disease
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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 .
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- HY-162000
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Apoptosis
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Cancer
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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 .
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- HY-168030
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Apoptosis
Ferroptosis
Carbonic Anhydrase
Reactive Oxygen Species (ROS)
Caspase
Mitochondrial Metabolism
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Cancer
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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 .
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- HY-147955
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Carbonic Anhydrase
Cholinesterase (ChE)
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Neurological Disease
Metabolic Disease
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hCAI/II-IN-5 (compound MZ8) is a potent hCA I and hCA II (human carbonic anhydrase isoenzymes I and II) inhibitor, with IC50 values of 37.88 and 45.23 nM, respectively. hCAI/II-IN-5 also shows inhibition profile against α-Glycosidase and AChE, with IC50 values of 48.98 and 420.14 nM, respectively. hCAI/II-IN-5 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy .
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- HY-161507
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Carbonic Anhydrase
Cholinesterase (ChE)
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Metabolic Disease
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hCAI/II-IN-8 (Compound 8) is a hydrazide derivative based on 4-hydroxybenzaldehyde. hCAI/II-IN-8 primarily targets human carbonic anhydrase isomerase I (hCA I) and II (hCA II) for inhibition (IC50 = 21.35 ± 0.39 nM (hCA I); 7.12 ± 0.12 nM (hCA II)). hCAI/II-IN-8 inhibits AChE and BChE as well(IC50 = 46.27 ±0.75 nM (AChE); 43.38 ± 0.83 nM (BChE)). . .
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- HY-147954
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Carbonic Anhydrase
Cholinesterase (ChE)
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Neurological Disease
Metabolic Disease
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α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy .
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- HY-146979
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Adenosine Receptor
Carbonic Anhydrase
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Cancer
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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 .
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- HY-181238
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Carbonic Anhydrase
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Others
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CAII-IN-13 is a human carbonic anhydrase inhibitor, with a Ki of 65.9 nM against human carbonic anhydrase II and a Ki of 968.4 nM against human carbonic anhydrase I. CAII-IN-13 functionally inhibits the catalytic activities of human carbonic anhydrase II and human carbonic anhydrase I. CAII-IN-13 satisfies the Lipinski's rule of five and may possess physicochemical properties and pharmacokinetic profiles associated with in vivo bioavailability .
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- HY-W015675R
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Reference Standards
Endogenous Metabolite
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Metabolic Disease
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Lasamide (Standard) is the analytical standard of Lasamide. This product is intended for research and analytical applications. Lasamide is a potent human Carbonic Anhydrase inhibitor with Ki values of 7.54 and 2.76 nM for hCAXII and hCAIX, respectively .
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- HY-181510
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Carbonic Anhydrase
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Others
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CAII-IN-14 (Compound 3o) is a human carbonic anhydrase II (hCA II) inhibitor with a Ki value of 1.65 nM. CAII-IN-14 also inhibits hCA I(Ki = 6.15 nM) and hCA IX(Ki = 5.43 nM). CAII-IN-14 exhibits predicted drug-like properties .
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- HY-183590
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Carbonic Anhydrase
Apoptosis
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Cancer
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CAIX/XII-IN-17 is a selective human carbonic anhydrase IX/XII (CA IX/XII) inhibitor with Ki values of 25.1 nM (hCA IX) and 35.2 nM (hCA XII). CAIX/XII-IN-17 induces apoptosis in pancreatic cancer cells. CAIX/XII-IN-17 can be used for the research of breast cancer, pancreatic cancer .
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- HY-183591
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Carbonic Anhydrase
Apoptosis
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Cancer
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CAIX/XII-IN-18 is a selective human carbonic anhydrase IX/XII (CA IX/XII) inhibitor with Ki values of 28.1 nM (hCA IX) and 11.6 nM (hCA XII). CAIX/XII-IN-18 induces apoptosis in breast cancer cells. CAIX/XII-IN-18 can be used for the research of breast cancer, pancreatic cancer .
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- HY-179467
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PROTACs
Carbonic Anhydrase
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Cancer
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PROTAC hCAII degrader-1 is a potent PROTAC human carbonic anhydrase II (hCAII) degrader with an DC50 of 0.5 nM in HEK293 cells. PROTAC hCAII degrader-1 recruits cereblon (CRBN) E3 ubiquitin ligase to form a ternary complex. PROTAC hCAII degrader-1 enables ubiquitination and subsequent proteasomal degradation of hCAII .
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- HY-109056A
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R-1206 sodium
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HIV
Drug Intermediate
Reverse Transcriptase
Carbonic Anhydrase
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Infection
Cancer
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Elsulfavirine sodium (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine sodium also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine sodium and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine sodium is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine sodium exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine sodium is used in studies related to HIV-1 infection and liver cancer .
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- HY-182007
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Carbonic Anhydrase
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Cancer
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CA IX-IN-5 (compound 9) is a human carbonic anhydrase IX (hCA IX) inhibitor with a Ki of 7.4 nM against hCA IX and 25.0 nM against hCA II.CA IX-IN-5 functionally inhibits hCA IX and hCA II isoenzymes, with selectivity for hCA IX over hCA II.CA IX-IN-5 can be used for the research of breast, colorectal, glioblastoma, lung, head and neck, and cervical cancers .
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- HY-109056R
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R-1206 (Standard)
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Reference Standards
Drug Intermediate
HIV
Reverse Transcriptase
Carbonic Anhydrase
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Infection
Cancer
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Elsulfavirine (Standard) is the analytical standard of Elsulfavirine (HY-109056). This product is intended for research and analytical applications. Elsulfavirine (R-1206) is an orally active human carbonic anhydrase (carbonic anhydrase, CA) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). Elsulfavirine also targets and blocks the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocks SREBP-1-mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine and Lenvatinib (HY-10981) produces a synergistic anti-tumor effect. Elsulfavirine is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase, and inhibits HIV-1 replication. Elsulfavirine exhibits a Ki of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV. Elsulfavirine is used in studies related to HIV-1 infection and liver cancer .
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- HY-182426
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Carbonic Anhydrase
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Neurological Disease
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NCX-278 is a human carbonic anhydrase inhibitor with a 13 nM Ki for hCA II, 410 nM Ki for hCA I, 181 nM Ki for hCA IV, and selective inhibition of hCA II over hCA IV. NCX-278 is a potent and effective stimulator of NO/sGC/cGMP signaling with an EC50 of 2.05 lM. NCX-278 exerts NO-mediated vascular relaxant effects. NCX-278 lowers intraocular pressure in normotensive rabbits. NCX-278 can be used for the research of open-angle glaucoma .
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- HY-129986
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Endogenous Metabolite
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Others
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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 .
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- HY-182245
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Microtubule/Tubulin
Carbonic Anhydrase
Apoptosis
MDM-2/p53
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Cancer
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Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer .
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- HY-B0553S
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Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders .
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- HY-W748430
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Furagin- 13C3 (Furazidine- 13C3) is the 13C-labeled Furagin (HY-77036). Furagin (Furazidine), an analogue of Nitrofurantoin (HY-A0090), is an antibiotic with antibacterial activity against ESKAPE pathogens with MIC values of 0-32 μg/mL. Furagin inhibits human Carbonic anhydrases . Furagin is promising for research of cancer and urinary tract infections (UTIs) .
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- HY-159129
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Azide
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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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