ser2

KB-0742 dihydrochloride 是一种有效的、选择性的、口服的 CDK9 抑制剂，具有抗肿瘤活性，对CDK9 cyclin T1的IC50为 6 nM。它对CDK9 cyclin T1具有选择性，其选择性是其他 CDK 激酶的 50 倍以上。

(D-Ser2)-Leu-Enkephalin-Thr 是阿片受体的 delta 选择性药物，具有镇痛作用。

[pSer2, pSer5, pSer7]-CTD (TFA) is a phosphorylated polypeptide at ser2, ser5, and ser7 of RNA polymerase II carboxyl terminus (CTD) and a substrate for CDK7 (cyclin-dependent protein kinase).

[pSer2, pSer5, pSer7]-CTD is a substrate for CDK7(cyclin-dependent protein kinase), a phosphorylated polypeptide at ser2, ser5, and ser7 of RNA polymerase II carboxyl terminus (CTD).

PI3K mTOR Inhibitor-9 (Compound 1) 是一种 mTOR 和 PI3K 的有效抑制剂，能够作用于 mTOR (IC50: 38 nM)、PI3Kα (IC50: 6.6 nM)、PI3Kγ (IC50: 6.6 nM) 和 PI3Kδ (IC50: 0.8 nM)。

AZ5576 racemate is a racemic mixture of AZ5576 isomers. AZ5576 is a potent, highly selective, and orally bioavailable inhibitor of Cdk9 that inhibits Cdk9 enzyme activity with an IC50 <5nM and decreases phosphorlyation of Ser2-RNAPII in cells with an IC50 of 96nM. In the MLL-fusion containing acute myeloid leukemia (AML) line, MV411, short-term treatment with AZ5576 led to a rapid dose-dependent decrease in pSer2-RNAPII with concomitant loss of Mcl1 mRNA and protein, resulting in the cleavage and activation of caspase 3 and loss of cell viability.

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。