cdk1-in-2

CDK1-IN-2 (cdk1 inhibitor 2)是一种CDK1抑制剂，IC50为5.8μM。CDK1-IN-2的激酶谱显示了多种激酶的非选择性抑制。

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)。

AZD8421 是一款高效且选择性极高的 CDK2 (细胞周期依赖性激酶 2) 抑制剂，其对 CDK2 的 IC50 值为 9nM，明显优于 CDK1、CDK4 和 CDK6。此外，AZD8421 还能有效抑制 Rb 磷酸化，显示出强大的抗增殖能力。在乳腺癌和卵巢癌模型中，无论是单独使用还是与 CDK4 6 抑制剂联合治疗，AZD8421 都展示了显著的疗效。

Anticanceragent 264 (Compound 5w) 是一种抗癌剂，在多种肿瘤细胞系中展现出明显的抗增殖活性，IC50范围为7.5-33.67 μM。它能显著诱导MDA-MB-231、MIA PaCa-2和DU-145细胞系在G2 M期的细胞周期停滞，并以剂量依赖性方式降低关键细胞周期蛋白CDK1、CDK2和Cyclin B1。该化合物与分化抑制剂和DNA结合蛋白表现出良好的结合活性，适用于癌症相关领域的研究。

JH295 is a highly potent and selective inhibitor of NIMA-related kinase 2 (Nek2), exhibiting irreversible inhibition activity with an IC 50 value of 770 nM. This compound effectively inhibits cellular Nek2 using the alkylation of Cys22. Importantly, JH295 does not exhibit any inhibitory effects toward Cdk1, Aurora B, or Plk1, which are kinases involved in mitotic processes. Furthermore, JH295 has no impact on bipolar spindle assembly or the spindle assembly checkpoint mechanism.

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。

CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and Bcl-x(L). CGP74514A treatment (5 microM; 18 hr) resulted in increased p21(CIP1) expression, p27(KIP1) degradation, diminished E2F1 expression, and dephosphorylation of p34(CDC2). It also induced early (i.e., within 2 hr) inhibition of CDK1 activity and dephosphorylation of pRb, followed by pRb degradation, but did not block pRb phosphorylation at CDK2- and CDK4- specific sites. These findings indicate that the selective CDK1 inhibitor, CGP74514A , induces complex changes in cell cycle......

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。

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。

LL-K9-3是一种基于选择性疏水标记技术（HyT）的CDK9-cyclin T1复合物降解剂（DC50值分别为cyclin T1的589 nM和CDK9的662 nM）。它由CDK9抑制剂SNS 032和一个糖基连接器连接到疏水标记组成。LL-K9-3不会降解其他CDKs（CDK1、2、4、5、6和7）。在22RV1细胞中，LL-K9-3通过诱导CDK9和cyclin T1的选择性和同步降解，降低雄激素受体（AR）和cMyc的表达。

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

Cyclin-dependent kinase 2 also known as cell division protein kinase 2. The protein encoded by this gene is a member of the cyclin-dependent kinase family of Ser Thr protein kinases. This protein kinase is highly similar to the gene products of S. cerevis