cdk7 in 1

CDK7-IN-1 is an analog derived from YKL-5-124 and functions as an inhibitor of cyclin-dependent kinase 7 (cdk7). It exhibits strong inhibitory activity, with an IC50 value of less than 100 nM (WO 2016105528 A2, Compound 215).

CDK7 9-IN-1 is a specific inhibitor of cyclin-dependent kinases 7 9 (CDK7 9). It specifically targets CDK7, while also displaying inhibitory activity against CDK9. CDK7 9-IN-1 demonstrates excellent inhibitory potency against CDK7, with IC50 values of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. Furthermore, CDK7 9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. Its application in cancer research makes it valuable for such investigations.

CDK7 12-IN-1 是一种 CDK7 12 的选择性抑制剂，作用于 CDK7 (IC50: 3 nM) 和 CDK 12 (IC50: 277 nM)。抑制 CDK7 和 CDK12 是一种有效抑制肿瘤生长的有效。

THZ2 (CDK7-IN-1) 是 THZ1 的类似物，是一种有效的选择性 CDK7 抑制剂 ，IC50值为 13.9 nM。它有治疗三阴性乳腺癌的潜力。

CDK7-IN-12 是有效的CDK7抑制剂，在调控转录和细胞周期中起关键作用。CDK7-IN-12可以有效抑制体外和体内恶性肿瘤的增殖。CDK7-IN-12 在癌症疾病中具有研究潜力。

CDK7-IN-13 是一种嘧啶基衍生化合物，是一种 CDK7 的有效抑制剂。CDK7-IN-13 具有潜力进行多种癌症的研究（尤其是转录失调的癌症）。

CDK7-IN-14 是一种嘧啶基衍生化合物，是一种 CDK7 的有效抑制剂。CDK7-IN-14 具有潜力进行多种癌症（尤其是转录失调的癌症）的研究。

CDK7-IN-15 是嘧啶基衍生化合物，也是 CDK7 的有效抑制剂。CDK7-IN-15 对多种癌症具有研究潜力，尤其是转录失调的癌症。

CDK7-IN-18 是嘧啶基衍生化合物，是 CDK7 的有效抑制剂。CDK7-IN-18 表现出多种癌症的研究潜力，尤其是转录失调的癌症。

CDK7-IN-17 是嘧啶基衍生化合物，也是 CDK7 的有效抑制剂。CDK7-IN-17 对多种癌症，尤其是转录失调的癌症表现出研究潜力。

CDK7 9 tide is peptide substrate for CDK7 or CDK9[1]. [1]. Robert T, et, al. Development of a CDK10 CycM in vitro Kinase Screening Assay and Identification of First Small-Molecule Inhibitors. Front Chem. 2020 Feb 27; 8:147.

CDK7-IN-16 (compound 9) 是一种 CDK 7 的有效抑制剂 (IC50: 1-10 nM)。CDK7-IN-16 能够用于研究抗癌，特别是转录异常的癌症。

Ibulocydine is a potent CDK inhibitor. Ibulocydine has high activity against Cdk7 cyclin H Mat1 and Cdk9 cyclin T. Ibulocydine inhibited the growth of HCC cells more effectively than other Cdk inhibitors, including olomoucine and roscovitine, whereas ibulocydine as well as the other Cdk inhibitors and BMK-Y101 minimally influenced the growth of normal hepatocyte cells. Ibulocydine induced apoptosis in HCC cells, most likely by inhibiting Cdk7 and Cdk9. In vitro treatment of HCC cells with ibulocydine rapidly blocked phosphorylation of the carboxyl-terminal domain (CTD) of the large subunit of RNA polymerase II, a process mediated by Cdk7 9. Anti-apoptotic gene products such as Mcl-1, survivin, and X-linked IAP (XIAP) are crucial for the survival of many cell types, including HCC. Following the inhibition of RNA polymerase II phosphorylation, ibulocydine caused rapid down-regulation of Mcl-1, survivin, and XIAP, thus inducing apoptosis. Furthermore, ibulocydine effectively ind......

CDK7-IN-21 (compound A22) 是一种有效的 CDK7抑制剂。

CDK7-IN-22 (compound 101)为CDK7选择性抑制剂，具备抗肿瘤活性。

SHR5428为口服选择性非共价CDK7抑制剂，显示出高效CDK7酶活性抑制（IC50=2.3 nM）。它还有效抑制MDA-MB-468细胞系中的三阴性乳腺癌细胞活性（IC50=6.6 nM）。

CDK7-IN-25 (CY-16-1)为一CDK-7抑制剂，具有极低的半抑制浓度(IC50<1nM)，主要用于癌症研究领域。

HDAC1 CDK7-IN-1（compound 8e）是一款针对CDK7和HDAC1的双重抑制剂，其IC50值分别为893 nM 和248 nM 。该化合物能有效抑制MDA-MB-231、MCF-7、A549及HCT-116等多种癌细胞系的生长。此外，HDAC1 CDK7-IN-1在HCT-116细胞中诱发了细胞周期阻滞与凋亡（apoptosis）现象，并能够抑制其细胞迁移能力。