cdk9-in-9

CDK9-IN-9 is a potent and selective CDK9 inhibitor (IC50: 1.8 nM) with anti-cancer activity. It inhibits CDK2 (IC50: 155 nM).

CDK9-IN-10 是一种有效的 CDK9 抑制剂。CDK9-IN-10 是 PROTAC CDK9 degrader-2 的配体。

CDK9-IN-7 (compound 21e) 是一种高效选择性的，具有口服活性的 CDK9 cyclin T 抑制剂 (IC50=11 nM)，与抑制其他 CDK 相比更有效 (CDK4 cyclinD=148 nM; CDK6 cyclinD=145 nM)。CDK9-IN-7 具有抗癌活性并没有明显的毒性。CDK9-IN-7 诱导非小细胞肺癌 (NSCLC) 细胞凋亡，在 G2 期阻滞细胞周期，并具有抑制非小细胞肺癌干细胞特性。

CDK9-IN-8 is a highly potent and selective CDK9 inhibitor (IC50: 12 nM).

CDK9-IN-2 是一种特异性CDK9抑制剂。它在 A2058 皮肤细胞系（72 小时）和 H929 多发性骨髓瘤细胞系（72小时）的IC50分别为 7 nM 和 5 nM。

CDK9-IN-1 是一种具有选择性和高效性的 CDK9 抑制剂，具有抗病毒活性，用于研究 PRRSV 感染。

CDK9-IN-11 是一种有效的CDK9抑制剂，可作为 PROTAC CDK9 Degrader-1 的配体。

PROTAC CDK9 degrader-9 (compound 29) 作为一种基于PROTAC技术的CDK9选择性降解剂，展现出高效的性能。该化合物主要应用于抗癌研究领域。

Zotiraciclib（又名TG02和SB1317）是一种新型小分子化合物，具有强效的CDK JAK2 FLT3抑制作用。该化合物可通过抑制周期蛋白依赖性激酶9（CDK9），耗竭Myc来治疗能穿越血脑屏障的癌症。Zotiraciclib是正在研究的众多CDK抑制剂之一，其他针对CDK9的化合物，用于治疗急性髓细胞性白血病的还包括alvocidib和atuveciclib。许多癌症中的Myc过表达是一个已知因素，其中80%的胶质母细胞性瘤展现此特性。

CDK2 9-IN-1 (compound 20a) 是一种口服活性的双重抑制剂，对CDK2和CDK9的IC50值分别为0.004 μM和0.009 μM。它通过调节G2 M细胞周期阻滞引发细胞凋亡 (Apoptosis)，并具有抗肿瘤活性。

CDK4 9-IN-1 (Compound 29) 是一种选择性双重抑制剂，针对CDK4和CDK9的IC50分别为23 nM和12 nM。该化合物有潜力用于癌症研究。

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.

CDK9-IN-12 是一种高选择性的 CDK9 抑制剂，通过 靶向 CDK9 依赖的转录过程，调控 癌基因的表达并抑制癌细胞的增殖并诱导细胞凋亡，常用于研究白血病。

CDK6 9-IN-1 (compound 66) is a potent dual inhibitor of CDK 6 and CDK 9 that can be administered orally. It exhibits inhibitory activity with IC 50 values of 40.5 nM and 39.5 nM against CDK6 and CDK9, respectively.

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.

Zotiraciclib, also known as TG02 and SB1317, is a novel small molecule potent CDK JAK2 FLT3 inhibitor. Zotiraciclib may be useful for the treatment of cancer that crosses the blood brain barrier and acts by depleting Myc through the inhibition of cyclin-dependent kinase 9 (CDK9). It is one of a number of CDK inhibitors under investigation; others targeting CDK9 for the treatment of acute myeloid leukemia include alvocidib and atuveciclib. Myc overexpression is a known factor in many cancers, with 80 percent of glioblastomas characterized by this property.

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......

CDK9-IN-26 (化合物1d) 为CDK9抑制剂，具有0.18 µM的IC50值。

LH2-051是一种通过DAT-CDK9-TFEB通路激活溶酶体生物合成和清除Aβ聚集体的溶酶体增强先导化合物。在小鼠模型中，LH2-051显示出优良的药代动力学性质，具备改善阿兹海默症症状的潜力。