| Company Name: |
BOC Sciences |
| Tel: |
1-631-485-4226; 16314854226 |
| Email: |
info@bocsci.com |
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| | IVACHTIN Basic information |
| Product Name: | IVACHTIN | | Synonyms: | IVACHTIN;2-[4-Methyl-8-(morpholin-4-ylsulfonyl)-1,3-dioxo-1,3-dihydro-2H-pyrrolo[3,4-c]quinolin-2-yl]ethylacetate;2-(4-methyl-8-morpholin-4-ylsulfonyl-1,3-dioxopyrrolo[3,4-c]quinolin-2-yl)ethyl acetate;modest,reversibl,Inhibitor,noncompetitive,Caspase,caspases,nonpeptide,inhibit,apoptosis,Ivachtin,selectivity,staurosporininduced;1H-Pyrrolo[3,4-c]quinoline-1,3(2H)-dione, 2-[2-(acetyloxy)ethyl]-4-methyl-8-(4-morpholinylsulfonyl)-;2-(4-Methyl-8-(morpholinosulfonyl)-1,3-dioxo-1,3-dihydro-2H-pyrrolo[3,4-c]quinolin-2-yl)ethyl acetate | | CAS: | 745046-84-8 | | MF: | C20H21N3O7S | | MW: | 447.46 | | EINECS: | | | Product Categories: | Inhibitor of caspase-3. | | Mol File: | 745046-84-8.mol |  |
| | IVACHTIN Chemical Properties |
| Boiling point | 665.0±65.0 °C(Predicted) | | density | 1.459±0.06 g/cm3(Predicted) | | storage temp. | Desiccate at +4°C | | solubility | Limited solubility, soluble in DMSO or DMF | | pka | 1.87±0.20(Predicted) | | form | Off-white solid | | color | off-white | | InChI | 1S/C20H21N3O7S/c1-12-17-18(20(26)23(19(17)25)7-10-30-13(2)24)15-11-14(3-4-16(15)21-12)31(27,28)22-5-8-29-9-6-22/h3-4,11H,5-10H2,1-2H3 | | InChIKey | MWXJJTMEUGWKKY-UHFFFAOYSA-N |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | IVACHTIN Usage And Synthesis |
| Uses | Ivachtin is a potent, cell-permeable, reversible, non-competitive inhibitor of caspase-3. | | Definition | ChEBI: Acetic acid 2-[4-methyl-8-(4-morpholinylsulfonyl)-1,3-dioxo-2-pyrrolo[3,4-c]quinolinyl]ethyl ester is a pyrroloquinoline. | | General Description | A cell-permeable, non-peptidyl pyrroloquinoline compound that acts as a potent, reversible, and non-competitive inhibitor of caspase-3 (IC50 = 23 nM) with larger than 10-fold greater selectivity towards caspase-3 than caspases-1, -2, and -4 through -10. Shown to display higher anti-apoptotic activity than Z-VAD-FMK (Cat. No. 627610) in preventing Staurosporine- (Cat. No. 569397) induced apoptosis in human Jurkat T cells. | | Biological Activity | ivachtin is a potent inhibitor of caspase-3 with ic50 value of 23 nm [1].caspase-3 is a member of the cysteine-aspartic acid protease family and interacts with caspase-8 and caspase-9. sequential activation of caspases plays an important role in cell apoptosis.ivachtin is a potent and reversible inhibitor of caspase-3 in a noncompetitive way. ivachtin was the most potent inhibitor against caspase-3, but the selectivity versus the remaining caspases was modest. in human jurkat t cells treated with 10 μm staurosporin, ivachtin protected cells in a higher level, which suggested that ivachtin had a good cell permeability and antiapoptotic activity [1]. | | Biochem/physiol Actions | Cell permeable: yes | | references | [1]. kravchenko dv, kuzovkova ya, kysil vm, et al. synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors. j med chem, 2005, 48(11): 3680-3683. |
| | IVACHTIN Preparation Products And Raw materials |
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