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Cat. No. | Product Name | Target | Signaling Pathways |
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T69931 |
MFH290
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MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation ... | |||
T82758 | CDK9-Cyclin T1 PPI-IN-1 | CDK | Cell Cycle/Checkpoint |
CDK9-Cyclin T1 PPI-IN-1 (Compound B19) 是CDK9-Cyclin T1蛋白-蛋白相互作用的选择性抑制剂。该化合物能够有效抑制TNBC MDA-MB-231细胞系的细胞增殖(IC50: 0.044 μM),诱导细胞凋亡,同时降低CDK9的转录活性并减少RNA Pol II CTD ser2的磷酸化,有效地抑制了4T1移植瘤模型小鼠中肿瘤的生长。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T17143 |
Toyocamycin
丰加霉素,Vengicide |
Apoptosis; Others; IRE1; Antibiotic; Antifungal | Apoptosis; Cell Cycle/Checkpoint; Microbiology/Virology; Others |
Toyocamycin (Vengicide) 是放线菌类产生的腺苷类似物,为 X 盒结合蛋白 1 (XBP1) 抑制剂,抑制 IRE1α 诱导的 ATP 依赖性 XBP1 mRNA 的断裂,IC50值为 80 nM。它还诱导凋亡。 |