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  2. Ligands for E3 Ligase HIV
  3. 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)).

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OICR409946

OICR409946 Chemical Structure

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Description

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))[1].

In Vitro

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.

Molecular Weight

1393.09

Formula

C64H70Cl4F4N8O14

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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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.

Purity & Documentation
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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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Product Name:
OICR409946
Cat. No.:
HY-183988
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