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.
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- CAS No.: 98296-23-2
- Formule: C25H23N5O8
- Masse moléculaire:521.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
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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Masse moléculaire 521.49
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDE-I2 Related Classifications
HY-188175 Related Classifications
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