OICR409946
OICR409946 is a self-dimerization-induced proximity-targeting chimera (SDIPTAC) targeting DCAF1, with a Kd value of 6200 nM. OICR409946 binds to DCAF1, induces head-to-tail homodimerization, sterically blocks the Vpr binding interface, prevents the recruitment of Vpr to the CRL4DCAF1 complex, and inhibits Vpr-dependent HIV replication. OICR409946 can be used in studies related to HIV infection (DCAF1 ligand: (HY-169390); Linker: (HY-130659)).
For research use only. We do not sell to patients.
- Formula: C64H70Cl4F4N8O14
- Molecular Weight:1393.09
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
OICR409946 (5-50000 nM; 240 s association, 0 s final dissociation) binds to the purified DCAF1 WDR domain with a KD value of 6200 nM; meanwhile, this compound induces the formation of stable DCAF1 dimers, with the ternary complex having a KD value of 200 nM and a residence time of 26 min[1].
OICR409946 (0.16-20 μM; 72 h) exhibits no cytotoxicity toward primary monocyte-derived macrophages even at concentrations up to 20 μM following a 72 h incubation[1].
OICR409946 (0.4-4 μM; pre-treatment for 2 hours, followed by 6 days post-infection) does not alter HIV-1 infection levels in primary monocyte-derived macrophages at concentrations of 0.4 μM or 4 μM[1].
OICR409946 (0.31-10 μM; 4 days) inhibits HIV replication in activated primary CD4+ T cells in a dose-dependent manner (significant inhibition is observed starting at 0.31 μM in Donor 2 and at 1.25 μM in Donor 1), and induces no cytotoxicity at concentrations up to 10 μM[1].
Incubation with OICR409946 (0.4-4 μM; 3 days) for 3 days does not significantly upregulate CD206 expression in primary monocyte-derived macrophages, even at the highest concentration of 4 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 1393.09
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Formula C64H70Cl4F4N8O14
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SMILES
NC(C[C@H](NC(C1=CNC(/C=C/C(NCCOCCOCCOCCOCCOCCOCCOCCOCCNC(/C=C/C2=C(C3=CC=C(Cl)C=C3F)C(C(N[C@@H](CC(N)=O)C4=CC=C(F)C(Cl)=C4)=O)=CN2)=O)=O)=C1C5=CC=C(Cl)C=C5F)=O)C6=CC=C(F)C(Cl)=C6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)