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Chemical Structure : kt-3283
Catalog No.: PC-21009Not For Human Use, Lab Use Only.
kt-3283 is a novel bi-functional PARP-HDAC inhibitor with IC50 of 0.338 nM, 2.19 nM and 1.89 uM for PARP1, PARP2 and HDACs, respectively.
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kt-3283 is a novel bi-functional PARP-HDAC inhibitor with IC50 of 0.338 nM, 2.19 nM and 1.89 uM for PARP1, PARP2 and HDACs, respectively.
kt-3283 displayed enhanced cytotoxicity in Ewing sarcoma models, compared to FDA-approved PARP (olaparib) and HDAC (vorinostat) inhibitors.
The kt-3283-induced cytotoxicity was associated with strong S and G2/M cell cycle arrest in nanomolar concentration range and elevated DNA damage as assessed by γH2AX tracking and comet assays.
kt-3283 showed efficacy in lower concentrations than olaparib and vorinostat and kt-3283 inhibited colonization of Ewing sarcoma cells in the ex vivo PuMA model.
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| Appearance | Solid | |
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10 mM in DMSO |
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