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Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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SKU | Size | Availability | Price | Qty |
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I650808-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,850.90 | |
I650808-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $550.90 | |
I650808-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,650.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader , blocks both the catalytic activity and scaffolding effects of PARP1. |
Storage Temp | Store at -20°C,Argon charged |
Shipped In | Ice chest + Ice pads |
Product Description | iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1 In Vitro iRucaparib-AP6 (0-10 μM; 24 hours) decreases PARP-1 level in a dose dependent manner, exhibits a half-maximal degrading concentration (DC 50 ) of 82 nM (D max = 92%). iRucaparib-AP6 (0-20 μM; 24 hours) induces degradation of PARP1 at low concentrations. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Primary rat neonatal cardiomyocyte cells Concentration: 0.001 μM; 0.01 μM; 0.1 μM; 1 μM; 10 μM Incubation Time: 24 hours Result: Decreased PARP-1 level in primary rat neonatal cardiomyocyte cells. Western Blot AnalysisCell Line: Primary rat neonatal cardiomyocyte cells Concentration: 0.05 μM; 0.1 μM; 0.2 μM; 0.5 μM; 1 μM; 2 μM; 5 μM;10 μM; 20 μM Incubation Time: 24 hours Result: Induced robust PARP1 degradation at concentrations as low as 50 nM. Form:Solid IC50& Target:PARP1 82 nM (DC 50 ) |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 2-(2,6-dioxopiperidin-3-yl)-4-[2-[2-[2-[2-[2-[2-[2-[[4-(6-fluoro-9-oxo-3,10-diazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13)-tetraen-2-yl)phenyl]methyl-methylamino]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]isoindole-1,3-dione |
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INCHI | InChI=1S/C46H55FN6O11/c1-52(29-30-5-7-31(8-6-30)42-33-11-12-49-43(55)35-27-32(47)28-37(50-42)40(33)35)14-16-60-18-20-62-22-24-64-26-25-63-23-21-61-19-17-59-15-13-48-36-4-2-3-34-41(36)46(58)53(45(34)57)38-9-10-39(54)51-44(38)56/h2-8,27-28,38,48,50H,9-26,29H2,1H3,(H,49,55)(H,51,54,56) |
InChi Key | YHMDCINUVWULST-UHFFFAOYSA-N |
Canonical SMILES | CN(CCOCCOCCOCCOCCOCCOCCNC1=CC=CC2=C1C(=O)N(C2=O)C3CCC(=O)NC3=O)CC4=CC=C(C=C4)C5=C6CCNC(=O)C7=C6C(=CC(=C7)F)N5 |
Isomeric SMILES | CN(CCOCCOCCOCCOCCOCCOCCNC1=CC=CC2=C1C(=O)N(C2=O)C3CCC(=O)NC3=O)CC4=CC=C(C=C4)C5=C6CCNC(=O)C7=C6C(=CC(=C7)F)N5 |
PubChem CID | 138857977 |
Molecular Weight | 886.96 |
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Solubility | DMSO : 50 mg/mL (56.37 mM; Need ultrasonic) |
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