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THZ1

CAS No. : 1604810-83-4

MCE 国际站：THZ1

产品活性：THZ1 是有效，选择性的共价 CDK7 抑制剂，IC₅₀ 为 3.2 nM。THZ1 还抑制相关的激酶 CDK12 和 CDK13，并下调 MYC 表达。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

In Vitro: THZ1 inhibits Jurkat cell and Loucy cell with IC₅₀ of 50 nM, and 0.55 nM, respectively. THZ1 (9, 27, 83, 250, 750, and 2500 nM) inhibits CDK12 but at higher concentrations compared to CDK7. THZ1 (1 μM) irreversibly inhibits RNAPII CTD and CAK phosphorylation. THZ1 (2.5 μM) irreversibly inhibits RNAPII CTD phosphorylation by covalently targeting a unique cysteine located outside the kinase domain of CDK7 in Hela S3 cells. THZ1 (250 nM) causes decreased cellular proliferation and an increase in apoptotic index with concomitant reduction in anti-apoptotic proteins, most notably MCL-1 and XIAP in T-ALL cell lines.
?All genotypically-distinct human (hSCLC) cell lines exhibit high sensitivity to THZ1, with an IC₅₀ in the range of 5-20 nM.

In Vivo: THZ1 (10 mg/kg) demonstrates potent killing of primary chronic lymphocytic leukemia (CLL) cells and anti-proliferative activity against primary TALL cells and in vivo against a human T-ALL xenograft.
?THZ1 (10 mg/kg, i.v.) inhibits tumor growth in a mouse model of human MYCN-amplified NB and shows no toxicity.
?THZ1 (10?mg/kg, i.p.) completely suppresses oesophageal squamous cell carcinoma tumour growth in vivo without loss of body weight or other common toxic effects.

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