Description
C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).
Product information
CAS Number: 192718-06-2
Molecular Weight: 293.25
Formula: C17H8FNO3
Chemical Name: 2-(4-fluorophenyl)-4H,9H-naphtho[2,3-d][1,3]oxazole-4,9-dione
Smiles: O=C1C2N=C(OC=2C(=O)C2=CC=CC=C12)C1C=CC(F)=CC=1
InChiKey: ULJDFEYQOPCCPM-UHFFFAOYSA-N
InChi: InChI=1S/C17H8FNO3/c18-10-7-5-9(6-8-10)17-19-13-14(20)11-3-1-2-4-12(11)15(21)16(13)22-17/h1-8H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : < 1 mg/mL (insoluble or slightly soluble). H2O : < 0.1 mg/mL (insoluble).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Pretreatment of USP1/UAF1 with C527 resulted in inhibition of its enzyme activity with an IC50 of 0.88±0.03 μM. 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. Pretreatment of cells with the C527 causes an enhancement in the cytoxicity of mitomycin C and camptothecin. C527 treatments 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.
Products are for research use only. Not for human use.
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