1. Epigenetics Anti-infection
  2. DNA Methyltransferase Parasite
  3. SC83288

SC83288 is a Plasmodium falciparum PfDNMT2 inhibitor with an IC50 of 7 μM. SC83288 disrupts the epigenetic regulation of malaria parasites, blocks DNA replication and nuclear division, arrests the development of the asexual blood stage, induces the formation of pyknotic morphology in malaria parasites, and does not affect cytokinesis after nuclear division or parasite egress. SC83288 is applicable to malaria-related research.

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SC83288

SC83288 Chemical Structure

CAS No. : 1237645-43-0

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Description

SC83288 is a Plasmodium falciparum PfDNMT2 inhibitor with an IC50 of 7 μM. SC83288 disrupts the epigenetic regulation of malaria parasites, blocks DNA replication and nuclear division, arrests the development of the asexual blood stage, induces the formation of pyknotic morphology in malaria parasites, and does not affect cytokinesis after nuclear division or parasite egress. SC83288 is applicable to malaria-related research[1].

In Vitro

SC83288 (72 h) potently inhibits wild-type P. falciparum 3D7 blood-stage growth with an IC50 of 8 nM, while the PfATP6F972Y mutant (E4) exhibits high resistance with an IC50 of 5 μM[1].
SC83288 (100 nM; 15 min) is transported via ATP-dependent mediation by PfATP6, particularly the PfATP6F972Y mutant, with the mutant showing enhanced transport efficiency that is competed by Ca2+[1].
SC83288 (50 nM; 0-60 min) is taken up ~100-fold by wild-type 3D7 and E4 mutant P. falciparum-infected erythrocytes via parasite-induced new permeation pathways, with no difference in uptake between the two lines[1].
SC83288 (30 nM; 0-52 h) blocks DNA replication in wild-type P. falciparum Dd2 and 3D7 blood-stage parasites when added during early ring to trophozoite stages, but has no effect on the E4 (PfATP6F972Y mutant) line[1].
SC83288 (5-10 nM; 4.5 h) treatment of P. falciparum 3D7 trophozoites induces transcriptional upregulation of genes linked to epigenetic regulation, karyokinesis, and stress responses[1].
SC83288 (40 nM; 12 h) disrupts methylation-related metabolism in P. falciparum 3D7 trophozoites, with no effect on the E4 (PfATP6F972Y mutant) line[1].
SC83288 (80 nM; 4 h) reduces global RNA m6A and DNA m5C methylation, and inhibits nuclear DNA methyltransferase activity in P. falciparum trophozoites, with the activity inhibition reversible by SAM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SC83288 (5 mg/kg; daily; 3 consecutive days) cures Plasmodium falciparum infection in humanized NOD/SCID mice, with an in vivo logPRR of 5.3[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

629.71

Formula

C27H31N7O7S2

CAS No.
SMILES

COC(N1CCN(CC1)C(C2=CC(NC(NC3=CC=C(C=C3)S(=O)(NCC4=CC=C(C=C4)S(N)(=O)=O)=O)=O)=CC=C2)=N)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SC83288
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HY-182309
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