cdk-7-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).

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。

Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.1,2 It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 μg/ml for both).1 Roccellic acid (100 μg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.2 |1. Sweidan, A., Chollet-Krugler, M., Sauvager, A., et al. Antibacterial activities of natural lichen compounds against Streptococcus gordonii and Porphyromonas gingivalis. Fitoterapia 121, 164-169 (2017).|2. Mishra, T., Shukla, S., Meena, S., et al. Isolation and identification of cytotoxic compounds from a fruticose lichen Roccella montagnei, and it's in silico docking study against CDK-10. Rev. Bras. Farmacogn. 27(6), 724-728 (2017).

6-Chloro-2-fluoropurine is a heterocyclic building block.1,2It has been used in the synthesis of purine nucleosides that inhibit cyclin-dependent kinases (CDKs)in vitro.16-Chloro-2-fluoropurine has also been used in the synthesis of purine nucleosides that are active against HIV-1 and hepatitis B virus (HBV)in vitro.2 1.Wilson, S.C., Atrash, B., Barlow, C., et al.Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitorsBioorg. Med. Chem.19(22)6949-6965(2011) 2.Lee, K., Choi, Y., Gullen, E., et al.Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2',3'-unsaturated L-nucleosidesJ. Med. Chem.42(7)1320-1328(1999)

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-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。

CDK4 6-IN-14 是一种有效且高度选择性的 CDK4和 CDK6(CDK) 抑制剂，IC50分别为 10 nM 和 16 nM。CDK4 6-IN-14 的选择性是 CDK1、2、7 和 9 的 60 多倍，并且在其他 205 种激酶中表现出高选择性。

EGFR CDK2-IN-2（compound 6a）是一种针对EGFR和CDK-2的双重抑制剂，具有19.6 nM和87.9 nM的IC50s。该化合物能在MCF-7细胞内诱导凋亡，并在S期引发细胞周期停滞。此外，EGFR CDK2-IN-2展现出IC50为0.39 μM的显著抗癌活性，对MCF-7细胞具有强效的细胞毒性。

EGFR CDK2-IN-3（compound 4b）是一种针对EGFR与CDK-2的双重抑制剂，分别具有71.7 nM和113.7 nM的IC50s。该化合物在MCF-7细胞中能诱导凋亡，导致细胞周期在S期停滞，并显示出对癌细胞的明显毒性，其对MCF-7细胞的IC50值为3.16 μM。

EGFR CDK2-IN-4（化合物4c）是一种EGFR与CDK-2的双重抑制剂，其IC50值分别为89.6 nM和165.4 nM。该化合物在MCF-7细胞中能诱导(apoptosis)凋亡，并导致细胞周期在S期停滞。EGFR CDK2-IN-4显示出显著的抗癌细胞毒性，对MCF-7细胞的IC50为2.74 μM。

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。