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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 98296-23-2
- 分子式: C25H23N5O8
- 分子量:521.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
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.
化学情報
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CAS 番号 98296-23-2
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分子量 521.49
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PDE-I2 関連分類
HY-188175 関連分類
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