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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-CT1113
CT1113

Chemical Structure : CT1113

CAS No.: 2523435-18-7

CT1113 (CT-1113)

货号: PC-22261Not For Human Use, Lab Use Only.

CT1113 is a potent, selective small molecule USP25/USP28 inhibitor with IC50 of 26.1 nM/3.9 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CT1113 is a potent, selective small molecule USP25/USP28 inhibitor with IC50 of 26.1 nM/3.9 nM, respectively.
CT1113 displays no activity against other deubiquitinases and SENP1 at 1 uM.
CT1113 strongly destabilize NOTCH1 and inhibit the growth of T-ALL cells.
Inhibition of USP28 by CT1113 resulted in increased ubiquitination of the ICN1 protein in T-ALL cell lines (Jurkat and MOLT-4).
CT1113 induces apoptosis in T-ALL cells with or without mutant NOTCH1.
CT1113 significantly inhibited leukaemia progression in Jurkat xenograft, inhibits NOTCH1-driven T-cell leucaemogenesis.
CT1113 demonstrated anti-leukaemia efficacy in a NOTCH1-independent patient-derived T-ALL xenograft.

物理化学性质&存储条件

分子量 463.60
分子式 C25H29N5O2S
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

N-[(3R)-7-(3,8-Diazabicyclo[3.2.1]oct-3-yl)-3,4-dihydro-2H-1-benzopyran-3-yl]-6-methyl-3-(methylamino)thieno[2,3-b]pyridine-2-carboxamide

参考文献

1. Jin Peng, et al. Signal Transduct Target Ther. 2022 Dec 8;7(1):393.

2. Jieyu Xu, et al. Br J Haematol. 2024 Apr 29. doi: 10.1111/bjh.19492.

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