745046-84-8 Usage
Uses
Used in Pharmaceutical Applications:
Ivachtin is used as an anti-apoptotic agent for its ability to inhibit caspase-3, a key enzyme involved in the execution phase of apoptosis. This makes it a valuable compound in the development of therapeutic strategies to combat conditions associated with excessive or inappropriate apoptosis.
Used in Research Applications:
Ivachtin is used as a research tool for studying the role of caspase-3 in various cellular processes, particularly those related to apoptosis. Its high selectivity and potency make it an ideal compound for investigating the molecular mechanisms underlying cell death and the potential for therapeutic intervention in diseases characterized by dysregulated apoptosis.
Used in Drug Development:
Ivachtin is used as a lead compound in the development of new drugs targeting caspase-3 for the treatment of diseases with apoptotic components, such as neurodegenerative disorders, ischemic conditions, and certain types of cancer. Its cell-permeable nature and non-peptidyl structure may offer advantages in terms of drug delivery and stability compared to other caspase inhibitors.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 745046-84-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 7,4,5,0,4 and 6 respectively; the second part has 2 digits, 8 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 745046-84:
(8*7)+(7*4)+(6*5)+(5*0)+(4*4)+(3*6)+(2*8)+(1*4)=168
168 % 10 = 8
So 745046-84-8 is a valid CAS Registry Number.
745046-84-8Relevant academic research and scientific papers
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
Kravchenko, Dmitri V.,Kuzovkova, Yulia A.,Kysil, Volodymyr M.,Tkachenko, Sergey E.,Maliarchouk, Sergey,Okun, Ilya M.,Balakin, Konstantin V.,Ivachtchenko, Alexandre V.
, p. 3680 - 3683 (2007/10/03)
Synthesis, biological evaluation, and SAR dependencies for a series of novel 1,3-dioxo-2,3-dihydro-1H-pyrrolo-[3,4-c]quinoline inhibitors of caspase-3 are described. The inhibitory activity of the synthesized compounds is highly dependent on the nature of
Pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors. Synthesis and SAR of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-pyrrolo[3, 4-c]quinoline-1,3-diones
Kravchenko, Dmitri V.,Kysil, Volodymyr M.,Tkachenko, Sergey E.,Maliarchouk, Sergey,Okun, Ilya M.,Ivachtchenko, Alexandre V.
, p. 1377 - 1383 (2007/10/03)
Synthesis, biological evaluation and structure-activity relationships for a series of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-1,3-dioxo-2,3- dihydro-1H-pyrrolo[3,4-c]quinolines are described. These compounds represent a new chemotype of nonpeptid
