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Caspase-3/7 Inhibitor I (CAS 220509-74-0)

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Alternate Names:
5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
Application:
Caspase-3/7 Inhibitor I is an inhibitor of caspase-3, caspase-7 and Caspase-9
CAS Number:
220509-74-0
Purity:
≥98%
Molecular Weight:
324.4
Molecular Formula:
C14H16N2O5S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Caspase-3/7 Inhibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (KI(app)= 60 nM) and caspase-7 (KI(app) = 170 nM). It is a weaker inhibitor of caspase-9 (KI(app) = 3.1 muM). Caspase-3/7 Inhibitor I has only a trivial effect (Ki(app) >25 muM) on the activities of caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8. It may act to inhibit apoptosis in camptothecin treated Jurkat cells (IC50 ~50 muM). Caspase-3/7 Inhibitor I has also been reported to inhibit apoptosis in chondrocytes (44% inhibition at 10 muM and 98% inhibition at 50 muM). Selectivity for caspases 3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue.


Caspase-3/7 Inhibitor I (CAS 220509-74-0) References

  1. Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality.  |  Lee, D., et al. 2000. J Biol Chem. 275: 16007-14. PMID: 10821855
  2. Potent and selective nonpeptide inhibitors of caspases 3 and 7.  |  Lee, D., et al. 2001. J Med Chem. 44: 2015-26. PMID: 11384246
  3. Necrotic death of Rhodococcus equi-infected macrophages is regulated by virulence-associated plasmids.  |  Lührmann, A., et al. 2004. Infect Immun. 72: 853-62. PMID: 14742529
  4. Cannabinoid derivatives induce cell death in pancreatic MIA PaCa-2 cells via a receptor-independent mechanism.  |  Fogli, S., et al. 2006. FEBS Lett. 580: 1733-9. PMID: 16500647
  5. Cleavage of BNIP-2 and BNIP-XL by caspases.  |  Valencia, CA., et al. 2007. Biochem Biophys Res Commun. 364: 495-501. PMID: 17961507
  6. Nitric oxide and thioredoxin type 1 modulate the activity of caspase 8 in HepG2 cells.  |  Sengupta, R., et al. 2010. Biochem Biophys Res Commun. 391: 1127-30. PMID: 20005201
  7. Real-time monitoring of cell apoptosis and drug screening using fluorescent light-up probe with aggregation-induced emission characteristics.  |  Shi, H., et al. 2012. J Am Chem Soc. 134: 17972-81. PMID: 23043485
  8. Nek5, a novel substrate for caspase-3, promotes skeletal muscle differentiation by up-regulating caspase activity.  |  Shimizu, K. and Sawasaki, T. 2013. FEBS Lett. 587: 2219-25. PMID: 23727203
  9. Targeting the XIAP/caspase-7 complex selectively kills caspase-3-deficient malignancies.  |  Lin, YF., et al. 2013. J Clin Invest. 123: 3861-75. PMID: 23979166
  10. Targeted theranostic platinum(IV) prodrug with a built-in aggregation-induced emission light-up apoptosis sensor for noninvasive early evaluation of its therapeutic responses in situ.  |  Yuan, Y., et al. 2014. J Am Chem Soc. 136: 2546-54. PMID: 24437551
  11. Peptide-Induced AIEgen Self-Assembly: A New Strategy to Realize Highly Sensitive Fluorescent Light-Up Probes.  |  Han, A., et al. 2016. Anal Chem. 88: 3872-8. PMID: 26948051
  12. A FRET probe with AIEgen as the energy quencher: dual signal turn-on for self-validated caspase detection.  |  Yuan, Y., et al. 2016. Chem Sci. 7: 4245-4250. PMID: 30155071
  13. T-helper 1-type cytokines induce apoptosis and loss of HER-family oncodriver expression in murine and human breast cancer cells.  |  Namjoshi, P., et al. 2019. Oncotarget. 10: 6006-6020. PMID: 31666931
  14. Light-up bioprobe with aggregation-induced emission characteristics for real-time apoptosis imaging in target cancer cells.  |  Ding, D., et al. 2014. J Mater Chem B. 2: 231-238. PMID: 32261611
  15. Activity-Based Probe for Ratiometric Fluorescence Imaging of Caspase-3 in Living Cells.  |  Jin, Y., et al. 2021. Anal Chem. 93: 2045-2052. PMID: 33326221

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Caspase-3/7 Inhibitor I, 1 mg

sc-293986
1 mg
$153.00

Can we use this product in vivo to reduce apoptosis? What is the recommended dose?

Asked by: Laxman
Thank you for your question. We do not recommend or support the use of our research chemicals for in vivo applications. Therefore, we can not provide a recommended dose.
Answered by: Technical Support
Date published: 2017-09-11

Is this product cell permeable?

Asked by: hawkeye11
This chemical, Caspase-3/7 Inhibitor I (CAS 220509-74-0), is cell permeable.
Answered by: Chemical Support 1
Date published: 2017-04-07

Can this product be stored in solution?

Asked by: hawkeye11
This chemical, Caspase-3/7 Inhibitor I (CAS 220509-74-0), is recommended to aliquot and freeze at -20°C. Please advise that stock solutions are stable for up to 3 months at -20°C.
Answered by: Chemical Support 1
Date published: 2017-04-07
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Rated 5 out of 5 by from L hrmannL hrmann, A. et al. (PubMed 14742529) used Caspase-3/7 Inhibitor I to distinguish apoptosis from necrosis of J774E macrophages. -SCBT Publication Review
Date published: 2015-05-25
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Caspase-3/7 Inhibitor I is rated 5.0 out of 5 by 1.
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