FORX-864
FORX-864 is an irreversible covalent inhibitor of RAD52. FORX-864 covalently modifies adjacent cysteines and occupies the ssDNA-binding groove, blocking ssDNA binding. FORX-864 has a target IC50 of 5 nM and 7 nM for human RAD52. FORX-864 inhibits RAD52-dependent single-strand annealing in cells without cytotoxicity and lacks activity in RAD52 knockout cells. FORX-864 can be used for research related to RAD52-mediated diseases.
For research use only. We do not sell to patients.
- Formula: C36H33FN4O7S2
- Molecular Weight:716.80
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | IC50 |
0.96 μM
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Inhibition of RAD52-dependent single-strand annealing in U2OS SA-GFP wild-type reporter cells assessed by flow cytometry for mKate2+/GFP+ SSA-positive cells after 72 hrs incubation.
Inhibition of RAD52-dependent single-strand annealing in U2OS SA-GFP wild-type reporter cells assessed by flow cytometry for mKate2+/GFP+ SSA-positive cells after 72 hrs incubation.
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42854208 |
In Vitro
FORX-864 achieves essentially complete covalent mono-labeling of RAD52 at both 5 equivalents and 1 equivalent in intact MS experiments; and it exhibits efficient covalent inactivation of RAD52, with a kinact/KI of 2.3 × 105 M-1 s-1[1].
FORX-864 (1 µM; 4 h) shows limited proteome-wide off-target reactivity in U2OS cells by ABPP, although no RAD52 C64 peptide is detected[1].
FORX-864 (72 h) inhibits RAD52-dependent SSA in U2OS SA-GFP wild-type cells with an IC50 of 0.96 µM; moreover, it does not reduce the viability of U2OS SA-GFP wild-type cells under the SSA assay conditions[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 716.80
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Formula C36H33FN4O7S2
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SMILES
C=CC(NC1=CC=C(C(F)=C1)CC2=C(SC(C3=CC=CC(OCCN(C)CCOC4=CC=CC(C5=NC(C)=C(S5)C(O)=O)=C4)=C3)=N2)C(O)=O)=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)
FORX-864 Related Classifications
HY-190864 Related Classifications
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