Cat. No. | Product Name | Target | Signaling Pathways |
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T74631 |
RNA polymerase II-IN-2
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RNA polymerase II-IN-2 (compound 20iii)是高效的RNA polymerase II (Pol II)抑制剂,其Ki值为74.1 nM。该化合物对癌细胞展现出细胞毒性,其对CHO和HEK293细胞的毒性分别为α-amanitin的2倍和5倍。 | |||
T63368 | CDK7-IN-2 | ||
CDK7-IN-2 是 CDK7 的有效抑制剂。其中 CDK7 利用 RNA 聚合酶 II (RNAPII) 的 Rbpl 亚基的磷酸化参与转录起始过程,其与细胞周期和转录活性的时间控制有关。CDK7 对癌症疾病,尤其是侵袭性和难以治疗的癌症具有研究潜力。 | |||
T36745 |
cDPCP
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cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when ad... | |||
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 ... |