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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
67 Results for "
CA-II
" in MedChemExpress (MCE) Product Catalog:
Products (67)
67 Results for "CA-II" in MCE Product Catalog:
10
10 Publications Verification
Research Areas:
TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
10
10 Publications Verification
Research Areas:
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
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Brinzolamide (AL-4862) is a selective carbonic anhydrase II inhibitor with anIC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide can be used in glaucoma disease research .
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7 Cited Publications
Cat. No.: HY-B0109A
CAS No.: 130693-82-2
Synonyms: L671152 hydrochloride; MK507 hydrochloride
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Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
2
2 Cited Publications
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Research Areas:
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 .
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Carzenide (4-Sulfamoylbenzoic acid) is the major circulating metabolite of Mafenide (HY-B0614) in plasma. Carzenide is a strong CAII competitive inhibitor. Carzenide can be used in the research of epilepsy and cervical cancer .
Research Areas:
Benzenesulphonamide (Compound 1) is a carbonic anhydrase inhibitor. Benzenesulphonamide exhibits CA II inhibitory activity. Benzenesulphonamide reduces ROS and improves the gene expression of amyloid-β40 and 42. Benzenesulphonamide is beneficial for Alzheimer's disease. Benzenesulphonamide derivatives have anticancer, anti-inflammatory, and anticonvulsant activities. Benzenesulphonamide can be used in the research of Alzheimer's disease, epilepsy, inflammatory diseases, leukemia, melanoma, lung cancer, and colon cancer .
Cat. No.: HY-76938
CAS No.: 18699-02-0
Synonyms: 4-Acetylaminophenylacetic acid; MS-932
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Actarit (4-Acetylaminophenylacetic acid) is an orally active Carbonic Anhydrase II (CAII) inhibitor with an IC50 of 422 nM. Actarit shows suppressive effects experimental autoimmune encephalomyelitis in rats. Actarit inhibits the development of type ll collagen (CII)-induced arthritis in mice by suppressing delayed-type hypersensitivity to CII. Actarit can be used for the study of Multiple Sclerosis (MS) and rheumatoid arthritis .
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Target:
Cat. No.: HY-W749867
CAS No.: 6766-87-6
Synonyms: CAlcium disodium EDTA dihydrate
Cat. No.: HY-B0109
CAS No.: 120279-96-1
Synonyms: L671152; MK507
Target:
Research Areas:
Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
Cat. No.: HY-W587805
CAS No.: 41997-13-1
Synonyms: FHxSA
Research Areas:
Perfluorohexane sulfonamide (FHxSA) is the inhibitor for carbonic anhydrase, that inhibits bovine CA and human CA II with IC50 of 0.122 and 1.38 μM. Perfluorohexane sulfonamide is a delayed-action insecticide, that can be used to control red fire ants (Solenopsis invicta). Perfluorohexane sulfonamide could be a environmental pollutant .
Cat. No.: HY-B0588A
CAS No.: 150937-43-2
Synonyms: AL-4862 hydrochloride
Target:
Research Areas:
Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with an IC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research .
Cat. No.: HY-179530
Target:
Research Areas:
CA-II/TNAP-IN-1 (compound 15) is a potent dual inhibitor against b-TNAP and b-CAII with IC50s of 0.69 and 1.25 μM, respectively. CA-II/TNAP-IN-1 exhibits anti-cancer effects. CA-II/TNAP-IN-1 can be used for cancer research .
Cat. No.: HY-151495
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Research Areas:
CAII-IN-3 (compound 3h), a thiosemicarbazones derivatives, is a potent carbonic anhydrase-II (CA-II) inhibitor with an IC50 value of 13.4 µM .
Cat. No.: HY-178362
CAS No.: 3085155-69-4
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Research Areas:
CAII/VII-IN-1 is an orally active hCA II (KI = 12.3 nM), and hCA VII (KI = 22.6 nM) inhibitor, showing no significant activity against hCA I. CAII/VII-IN-1 shows excellent neuroprotective activity in vivo Pilocarpine (HY-B0726A)-induced seizure model. CAII/VII-IN-1 can upregulate KCC2 and inhibit mTOR, exerting neuroprotective effects. CAII/VII-IN-1 does not show any significant neurotoxic effects or alterations in liver and kidney function. CAII/VII-IN-1 can be used for the study of epilepsy .
Cat. No.: HY-175219
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Research Areas:
CA-II/Dkk1-IN-1 (Compound 5d) is a dual-functional inhibitor of CA-II and Dkk1 with a IC50 of 6.90 nM for CA-II. CA-II/Dkk1-IN-1 has significantly antioxidant activity and superior DNA binding capacity. CA-II/Dkk1-IN-1 can be used for cancers research, such as esophageal, renal, and lung cancer .
Cat. No.: HY-151493
Target:
Research Areas:
CAII-IN-1 (compound 3n), a thiosemicarbazide derivative, is a potent, selective carbonic anhydrase-II (CA-II) inhibitor with an IC50 value of 10.3 µM for bovine CA-II. CAII-IN-1 can be used in research of carbonic anhydrase related biological disorders .
Cat. No.: HY-151494
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CAII-IN-2 (compound 3g), a thiosemicarbazide derivative, is a potent, selective carbonic anhydrase-II (CA-II) inhibitor with an IC50 value of 12.1 µM for bovine CA-II. CAII-IN-2 can be used in research of carbonic anhydrase related biological disorders .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
