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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-kt-3283
kt-3283

Chemical Structure : kt-3283

CAS No.:

kt-3283 (kt3283)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量
分子式
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

参考文献

1. Louise Ramos, et al. Clin Cancer Res. 2023 Jun 6;CCR-22-3897.

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