ML-323

ML-323

Catalog Number:
L002369925APE
Mfr. No.:
APE-B1317
Price:
$228
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      • Overview
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          Background

          IC50: ML-323 is a highly potent and selective inhibitor of USP1-UAF1 with IC50 value of 76 nM.ML-323 is an inhibitor of USP1-UAF1 with remarkable selectivity and relatively low cytotoxicity to the human cells. [1] USP1-UAF1 is closely linked to the DNA damage response and is recently suggested as a strategy for overcoming drug resistance during antitumor therapy. [1]In vitro: Studies in H596 cells showed that ML-323 blocked the deubiquitination of PCNA and FANCD2 via suppressing USP1–UAF1 activity. It was reported that ML-323 potently inhibited USP1-UAF1 with IC50 values of 76 nM and 174 nM in ubiquitin-rhodamine (Ub-Rho) assay and orthogonal gel-based assay, respectively. In addition, by targeting TLS and FA, two major DNA damage response pathways, ML-323 increased cisplatin cytotoxicity both in NSCLC H596 cells and U2OS osteosarcoma cells. Moreover, this agent exhibited a high selectivity to human DUBs, deSUMOylase, deneddylase and unrelated proteases. [1]In vivo: So far, no in vivo study has been conducted.Clinical trial: So far, no clinical trial has been conducted.

      • Properties
        • Alternative Name
          (E)-1-(4-(1H-1,2,3-triazol-1-yl)phenyl)-N-(2-(2-isopropylphenyl)-5-methylpyrimidin-4(3H)-ylidene)methanamine
          CAS Number
          1572414-83-5
          Molecular Formula
          C23H24N6
          Molecular Weight
          384.48
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥12.34 mg/mL in EtOH; ≥15.05 mg/mL in DMSO; ≥2.25 mg/mL in H2O
          Storage
          Store at -20°C

          * For Research Use Only

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