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C527 is a potent pan DUB enzyme inhibitor with a high affinity for the USP1/UAF1 complex (IC50=0.88 μM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $29 | In Stock | |
10 mg | $48 | In Stock | |
25 mg | $88 | In Stock | |
50 mg | $142 | In Stock | |
100 mg | $227 | In Stock | |
200 mg | $333 | In Stock |
Description | C527 is a potent pan DUB enzyme inhibitor with a high affinity for the USP1/UAF1 complex (IC50=0.88 μM). |
Targets&IC50 | USP1:0.88 μM |
In vitro | C527 inhibits the DUB activity of the USP12/USP46 complex and other DUB enzymes in vitro. However, the IC50 of C527 for these DUB enzymes was higher in comparison with USP1/UAF1 complex. C527 has considerably less inhibitory effect on UCH-L1 and UCH-L3, a different subclass of DUB enzymes. C527 treatments causes an increase in the levels of Ub-FANCD2 and Ub-FANCI and it also lead to an increase in ubiquitinated forms of FANCD2 and FANCI, cause a decrease in homologous recombination activity, and sensitize cells to DNA damaging agents[1]. Pretreatment of USP1/UAF1 with C527 resulted in inhibition of its enzyme activity with an IC50 of 0.88±0.03 μM. Pretreatment of cells with the C527 causes an enhancement in the cytoxicity of mitomycin C and camptothecin. |
Molecular Weight | 293.25 |
Formula | C17H8FNO3 |
Cas No. | 192718-06-2 |
Smiles | Fc1ccc(cc1)-c1nc2c(o1)C(=O)c1ccccc1C2=O |
Relative Density. | 1.433 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||
Solubility Information | DMSO: 1.85 mg/mL (6.31 mM), Sonication is recommended. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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