THZ1 Hydrochloride

产品编号: DC10042 Featured
THZ1 Hydrochloride
结构式
此产品仅供科研所需,我们不出售给病人
​我们将匹配市场上最好的价格给您
Email:order@dcbio.cn
免费咨询电话:4008862077
我们的合作伙伴:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
中国地区超过5000个高品质化合物库存
应用领域
THZ1 Hydrochloride 是有效,选择性的共价 CDK7 抑制剂,IC50 为 3.2 nM。THZ1 Hydrochloride 还抑制相关的激酶 CDK12 和 CDK13,并下调 MYC 表达。
Cas No.:
名称:
别名:
SMILES:
分子式:
分子量:
纯度: >98%
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nM; inhibits Jurkat cell's proliferation with IC50 of 50 nM. IC50 value: 3.2 nM (Kd For CDK7) Target: CDK7 THZ1 Hydrochloride has the unprecedented ability to target a remotecysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity For CDK7. Cancer cell-line profiling indicates that a subset of cancer cell lines, including human T-cell acute lymphoblastic leukaemia (T-ALL), have exceptional sensitivity to THZ1 Hydrochloride. Genome-wide analysis in Jurkat T-ALL cells shows thatTHZ1 Hydrochloride disproportionally affects transcription of RUNX1 and suggests that sensitivity to THZ1 Hydrochloride may be due to vulnerability conferred by the RUNX1 super-enhancer and the key role of RUNX1 in the core transcriptional regulatory circuitry of these tumour cells. Pharmacological modulation of CDK7 kinase activity may thus provide an approach toidentify and treat tumour types that are dependent on transcription For maintenance of the oncogenic state.For the detailed information of THZ1 Hydrochloride, the solubility of THZ1 Hydrochloride in water, the solubility of THZ1 Hydrochloride in DMSO, the solubility of THZ1 Hydrochloride in PBS buffer, the animal experiment (test) of THZ1 Hydrochloride, the cell expriment (test) of THZ1 Hydrochloride, the in vivo, in vitro and clinical trial test of THZ1 Hydrochloride, the EC50, IC50,and Affinity of THZ1 Hydrochloride, Please contact DC Chemicals.
In Vivo:
In Vitro:
References:
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
产品编号 产品名称 应用领域
DC10042 THZ1 Hydrochloride THZ1 Hydrochloride 是有效,选择性的共价 CDK7 抑制剂,IC50 为 3.2 nM。THZ1 Hydrochloride 还抑制相关的激酶 CDK12 和 CDK13,并下调 MYC 表达。
DC27001 SR-4835 SR-4835 是有效,高选择性和 ATP 竞争性的 CDK12/CDK13 双重抑制剂 (CDK12:IC50=99 nM,Kd=98 nM;CDK13:Kd=4.9 nM)。SR-4835 与破坏 DNA 的化学疗法和 PARP 抑制剂协同作用,并引起三阴性乳腺癌 (TNBC) 细胞凋亡。