cdk-in-2

CDK-IN-2 (CDK inhibitor II) 是一种有效且特异性的 CDK9 抑制剂，IC50小于8 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。

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。

CDK4 6-IN-2 是一种CDK4和CDK6抑制剂，IC50分别为 2.7 和 16 nM。

CDK2-IN-4 是选择性的CDK2抑制剂，对 CDK2 cyclin A 的IC50值为 44 nM，选择性高出 CDK1 cyclin B 的 2,000 倍 (IC50=86 μM)。

CDK-IN-14 (B34) 作为一种CDK2抑制剂（IC50=0.097 μM），展现出对抗肝癌的效果。该化合物在阻断 HepG-2 癌细胞的细胞周期中，通过caspase介导的途径促进细胞凋亡（apoptosis）。

Protein kinase inhibitor 11 (Compound I-96) 是一种蛋白激酶抑制剂，能够抑制PIM-1、CDK-2、GSK-3和SRC的活性。此化合物被期望应用于癌症、免疫性疾病和神经退行性疾病的研究。

Amsilarotene (TAC101) 是口服有活性的合成类视黄醇，对视黄酸受体 α (RAR-α) 具有选择性亲和力，对 RAR-α 和 RAR-β 的 Ki=为 2.4 nM 和 400 nM。它可造成人胃癌、卵巢癌细胞及肝细胞癌的凋亡，可用于研究癌症。

GW8510是一种CDK2（细胞周期蛋白依赖性激酶2）抑制剂和RRM2（核糖核苷酸还原酶M2）抑制剂，能够影响肿瘤细胞DNA合成和抗增殖。在哺乳动物衰老模型中，GW851能够改善认知和延长寿命，可能与调控细胞周期相关蛋白p21和CDK家族基因的表达，以及改善线粒体功能有关。

CKD-712 is a nuclear factor NF-kappa B inhibitor. CKD-712 suppressed MMP-9, but not MMP-2 and other NF-κB-regulated proteins involved in cancer metastasis such as VEGF. CKD-712 induced cell cycle arrest at G2M phase by suppressing cyclin A, cyclin B and C

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).

Potent and selective CLK inhibitor (IC50 values are 28, 88 and 510 nM for CLK4, 1 and 2, respectively). Exhibits no significant activity at CLK3, DYRK, CDK or GSK3 at a concentration of 10 μM. Inhibits growth of a range of cancer cell lines in vitro at subnanomolar concentrations. Walter et al (2018) Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. PLoS One 13 e0196761 PMID:29723265

LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4 6 degrader[1].

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-IN-2 hydrochloride hydrate (Example 6) is a highly effective and specific inhibitor of the CDK7 enzyme. This compound exhibits significant anti-cancer properties.

CDK2-IN-7 is a CDK2 inhibitor for treating cancer ( IC 50 < 50 nM).

3-Methylthienyl-carbonyl-JNJ-7706621 is a highly potent and selective inhibitor of cyclin-dependent kinase (CDK). It exhibits impressive IC50 values of 6.4 nM and 2 nM for CDK1 cyclin B and CDK2 cyclin A, respectively. Additionally, 3-Methylthienyl-carbonyl-JNJ-7706621 demonstrates potent inhibition against GSK-3 (IC50 = 0.041 μM) and moderate potency towards CDK4, VEGF-R2, and FGF-R2 (IC50 = 0.11 μM, 0.13 μM, and 0.22 μM, respectively). Its applications in cancer research are noteworthy.

CDK1 2 4-IN-1 (compound 3a) 是 CDK 的有效抑制剂， 其对于 CDK1、CDK2 和 CDK4 的 IC50值分别为 1.47、0.78 和 0.87 μM。CDK1 2 4-IN-1 可用于癌症研究。CDK1 2 4-IN-1 可将细胞周期阻滞在 G2 M 期并诱导细胞凋亡。CDK1 2 4-IN-1 提高 Bax、caspase-3和 P53 的水平并降低 Bcl-2 水平。

CDK HDAC-IN-2 是有效的 HDAC CDK 双重抑制剂，能够作用于 HDAC1 (IC50: 6.4 nM)、HDAC2 (IC50: 0.25 nM)、HDAC3 (IC50: 45 nM)、HDAC6,8 (IC50>1000 nM)、CDK1 (IC50: 8.63 nM)、CDK2 (IC50: 0.30 nM)、CDK4,6,7 (IC50>1000 nM)。CDK HDAC-IN-2 能够将细胞周期停滞在 G2 M 期，并诱导细胞凋亡 (apoptosis)。CDK HDAC-IN-2 具有优异的抗增殖效果，显示出显著的抗肿瘤作用。

Riviciclib hydrochloride (P276-00) 是一种CDK 抑制剂，抑制CDK9-cyclinT1、CDK4-cyclin D1、CDK1-cyclinB 的IC50值分别为 20 nM、63 nM、79 nM。它对 Cisplatin 耐药性细胞具有抗肿瘤活性。

VMY-1-103 is a potent CDK inhibitor, is also a novel dansylated analog of purvalanol B, was shown to inhibit cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B. VMY-1-103 , but not purvalanol B, significantly decreased the proportion of cells in S phase and increased the proportion of cells in G(2) M. VMY-1-103 increased the sub G(1) fraction of apoptotic cells, induced PARP and caspase-3 cleavage and increased the levels of the Death Receptors DR4 and DR5, Bax and Bad while decreasing the number of viable cells, all supporting apoptosis as a mechanism of cell death. VMY-1-103 possesses unique antiproliferative capabilities and that this compound may form the basis of a new candidate drug to treat medulloblastoma.

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。

CDK2 Bcl2-IN-1（化合物1）为皂素类CDK-2抑制剂（IC50=117.6 nM），对癌细胞显示显著细胞毒性，并能够抑制Bcl-2，诱导A549肺癌细胞的凋亡。

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。