MMV022224
MMV022224 is an antimalarial agent that acts by selectively binding to and inhibiting the enzymatic activity of PfPK6. MMV022224 disrupts hemoglobin catabolism, induces peptide accumulation, and targets the ring and trophozoite stages of Plasmodium falciparum. MMV022224 can be used in malaria-related research.
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- CAS 番号: 2581277-82-7
- 分子式: C25H28N4
- 分子量:384.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
MMV022224 (72 h) potently inhibits the growth of P. falciparum (3D7) asexual blood stage parasites with an EC50 of 217 nM[1].
MMV022224 potently inhibits P. falciparum asexual blood stage parasites with an EC50 of 390 nM and liver stage parasites with an EC50 of 800 nM[1].
MMV022224 (0.01-100 μM; 30 min) binds with highest affinity to PfPK6 (IC50 = 161 nM) among a cohort of essential P. falciparum kinases, including PfCLK3 and PfPI(3,4)K, and demonstrates low-affinity binding to additional parasite kinases[1].
MMV022224 (10 μM; 30 min pre-incubation) directly interacts with PfPK6 and PfCLK3 in P. falciparum 3D7 asexual blood stage lysates[1].
MMV022224 inhibits recombinant PfPK6 enzymatic activity with an IC50 of 800 nM, confirming it acts as a PfPK6 inhibitor[1].
MMV022224 does not increase susceptibility in PfPK6 knockdown P. falciparum, indicating PfPK6 inhibition is not the sole driver of the compound's antimalarial activity[1].
MMV022224 (8 h) potently inhibits Plasmodium falciparum 3D7-A10 ring and trophozoite stages (but not schizonts) and induces a unique metabolomic profile marked by increased peptide levels, indicating disruption of downstream hemoglobin catabolism[2].
MMV022224 (72h) exposure increases peptide levels in Plasmodium falciparum 3D7-MR4 trophozoites, indicating a unique mode of action targeting downstream hemoglobin catabolism[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2581277-82-7
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分子量 384.52
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分子式 C25H28N4
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SMILES
CN(C)CC1=CC=C(C2=CC3=C(C4=CC=C(CN(C)C)C=C4)C=CN=C3N2)C=C1
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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.
純度とドキュメンテーション
参考文献
[1]. Syed AJ, et al. Using Unbiased Chemical Proteomics Approaches to Explore the Target Landscape of the Resistance Refractory 7-Azaindole MMV022224 in Plasmodium falciparum. ACS Infect Dis. 2026 Jun 25. [Content Brief]
[2]. Murithi JM, et al. Combining Stage Specificity and Metabolomic Profiling to Advance Antimalarial Drug Discovery. Cell chemical biology. 2020 Feb 20;27(2):158-171.e3. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)