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Synonyms:
SC83288
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | SC83288 is a Plasmodium falciparum PfDNMT2 inhibitor with an IC50 of 7 μM. It disrupts the epigenetic regulation in Plasmodium falciparum, inhibiting DNA replication and nuclear division, which arrests asexual blood-stage development and induces the formation of condensed forms. It does not affect cytokinesis or parasite egress post-nuclear division. SC83288 is applicable in malaria-related studies. |
| In vitro | SC83288 effectively inhibits the intraerythrocytic growth of wild-type Plasmodium falciparum (3D7) with an IC50 of 8 nM over 72 hours, whereas the PfATP6 F972Y mutant strain (E4) shows significant drug resistance with an IC50 reaching 5 μM. SC83288 at 100 nM for 15 minutes is transported in an ATP-dependent manner by PfATP6, particularly targeting the PfATP6 F972Y mutant, which exhibits enhanced transport efficiency subject to competitive inhibition by Ca2+. The compound at 50 nM over 0-60 minutes is taken up about 100-fold by wild-type 3D7 strain and E4 mutant-infected red blood cells via new permeation pathways induced by the parasite, with no difference observed between the two strains. At 30 nM for 0-52 hours, SC83288 interrupts DNA replication when administered from early ring to trophozoite stages in wild-type Plasmodium falciparum Dd2 and 3D7 blood-stage parasites, though it is ineffective against the E4 (PfATP6 F972Y mutant) strain. Treatment with SC83288 at 5-10 nM for 4.5 hours induces upregulation of gene transcription linked to epigenetic regulation, mitosis, and stress response in Plasmodium falciparum 3D7 trophozoites. When applied at 40 nM for 12 hours, SC83288 disrupts methylation-related metabolism in Plasmodium falciparum 3D7 trophozoites but has no effect on the E4 (PfATP6 F972Y mutant) lineage. SC83288 at 80 nM for 4 hours reduces global RNA m6A and DNA m5C methylation levels in trophozoites and inhibits DNA methyltransferase activity, which can be reversed by SAM. |
| In vivo | SC83288 (5 mg/kg; administered daily for 3 consecutive days) effectively cures malignant Plasmodium falciparum infections in humanized NOD/SCID mice. |
| Molecular Weight | 629.71 |
| Formula | C27H31N7O7S2 |
| Cas No. | 1237645-43-0 |
| Smiles | O=C(OC)N1CCN(C(=N)C=2C=CC=C(C2)NC(=O)NC3=CC=C(C=C3)S(=O)(=O)NCC4=CC=C(C=C4)S(=O)(=O)N)CC1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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