PDE-I2
PDE-I2 is a precursor small molecule of the naturally derived duocarmycin family that retains the sequence-specific DNA-binding property of this family but lacks the DNA-alkylating cyclopropyl warhead structure characteristic of this class of drugs. PDE-I2 inhibits the proliferation of blood-stage Plasmodium falciparum. PDE-I2 arrests Plasmodium falciparum development at the schizont stage, accompanied by defects in nuclear segregation, MTOC formation, IMC biogenesis, and plasma membrane invagination. PDE-I2 is useful for malaria-related research.
For research use only. We do not sell to patients.
- CAS No.: 98296-23-2
- Formula: C25H23N5O8
- Molecular Weight:521.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
PDE-I2 is an inhibitor of P. falciparum proliferation and exhibits selectivity, with toxicity to human cell lines more than 1000-fold lower than that to P. falciparum[1].
PDE-I2 blocks P. falciparum at the schizont stage, and treatment for 4 h induces malaria parasite DNA damage and impairs malaria parasite DNA replication, with its activity dependent on the active DNA replication process of P. falciparum[1].
PDE-I2 does not affect the development of non-replicating gametocytes, but impairs DNA replication in gametocytes after activation; it causes severe defects in nuclear division, inner membrane complex biogenesis, and parasite plasma membrane formation in Plasmodium falciparum[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 98296-23-2
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Molecular Weight 521.49
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Formula C25H23N5O8
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SMILES
O=C(O)C1=CC=2C(N1)=C(OC)C(O)=C3C2CCN3C(=O)C4=CC=5C(N4)=C(OC)C(O)=C6C5CCN6C(=O)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDE-I2 Related Classifications
HY-188175 Related Classifications
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