CDK-IN-10 is a cell cycle protein-dependent kinase (CDK) inhibitor with potential anticancer activity for cancer research.

Cyclin-dependent kinase 5 (Cdk5) is a serine/threonine kinase that is predominantly active in neuronal tissues. With p25 or p35, Cdk5 phosphorylates a range of proteins, including histone H1 and tau. Cdk5 Substrate acetate is a synthetic peptide (PKTPKKAKKL) corresponding to a sequence of histone H1. It is phosphorylated by Cdk5 with a Km value of 5 µM.

CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM). CDK4/6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.

Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor with an IC50 value of 2.1 μM against CDK1/cyclin B.

CDK2 acetate is a member of the eukaryotic S/T protein kinase family and its function is to catalyze the phosphoryl transfer of ATP γ-phosphate to serine or threonine hydroxyl (denoted as S0/T0) in a protein substrate.

CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells.

CDK9-IN-2 is a special CDK9 inhibitor and has an IC50 of 5 nM and 7 nM in A2058 skin cell line (72 hours) and H929 multiple myeloma cell line (72 hours), respectively.

CDK9-IN-10 is a potent CDK9 inhibitor and the ligand for the PROTAC CDK9 degrader-2.

CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively.

CDK9-IN-7 is a highly selective and orally active CDK9/cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD: 148 nM; CDK6/cyclinD: 145 nM).

Cdk2 Inhibitor II is a selective and potent CDK2 inhibitor50 at 60 nM.

CDK8-IN-1 is a selective CDK8 inhibitor (IC50: 3 nM).

CDK9 inhibitor HH1 (8019-9719) is an inhibitor of the human CDK2-cyclin A2 complex with an IC50 value of 2 μM.

CDK2-IN-13 is a potent Cyclin-dependent kinase 2 (CDK2) inhibitor (IC50 value: 12 µM).CDK2-IN-13 is involved in cell cycle regulation and can arrest the cell cycle. CDK2-IN-13 prevents cell division and proliferation, induces apoptosis, and can be used in cancer research.

CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).

CDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.

CDK12-IN-2 (CDK12 inhibitor 2) is an effective and selective inhibitor of CDK12 with an IC50 of 52 nM, >100 μM, >10 μM and 16 μM for CDK12, CDK2, CDK7, and CDK9. CDK12-IN-2 can be used in studies about the function of CDK12.

CDK8-IN-13 is a CDK8 inhibitor (IC50: 51.9 nM) with potent, selective and oral activity. CDK8-IN-13 induces apoptosis and reduces the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 exhibits anti-tumour activity.

CDK2-IN-20 (compound 3b), a CDK2 inhibitor, exhibits cytotoxic effects on tumor cells with an IC50 ranging from 5.52-17.09 µM. It arrests the MCF-7 cell cycle at the S phase and induces apoptosis [1].

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC MDA-MB-231 cells with an IC50 of 0.044 μM and inducing apoptosis. This compound diminishes CDK9 transcriptional activity and downregulates phosphorylation of RNA Pol II CTD ser2. In vivo, CDK9-Cyclin T1 PPI-IN-1 effectively impedes tumor growth in a TNBC 4T1 mouse model [1].

CDK9-IN-30 is one of the Tat peptide derivatives and inhibits HIV-1 long terminal repeat-activated transcription.

CDK9-IN-29 (compound Z11) is a potent inhibitor of CDK9, exhibiting high kinase selectivity and an IC50 value of 3.20 nM. It effectively hinders cell proliferation and induces apoptosis [1].

HDAC1/CDK7-IN-1 (compound 8e) serves as a dual inhibitor targeting both CDK7 and HDAC1, with IC50 values of 893 nM and 248 nM , respectively. This compound effectively suppresses the proliferation of various cancer cell lines, including MDA-MB-231, MCF-7, A549, and HCT-116. Additionally, it triggers cell cycle arrest and apoptosis in HCT-116 cells and impedes their migration [1].

CDK/HDAC-IN-3 is an orally active dual inhibitor of HDACs and CDKs, offering potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM, respectively. This compound is applicable in the treatment of acute myeloid leukemia (AML) [1].

EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor targeting EGFR and CDK-2, demonstrating IC50 values of 89.6 nM for EGFR and 165.4 nM for CDK-2. It prompts apoptosis in MCF-7 cells and causes S phase cell cycle arrest, exhibiting substantial anti-cancer activity with an IC50 of 2.74 μM against MCF-7 cells [1].

CDK7-IN-16 (Compound 9) is a potent inhibitor of CDK 7 (IC50: 1-10 nM). CDK7-IN-16 can be used in research against cancer, particularly cancers with transcriptional abnormalities.

CDK7-IN-5, a CDK7 inhibitor with an IC 50 value of less than 100 nM, exhibits potent anticancer properties (WO2015154022A1, Compound 104).

CDK4/6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively (WO2019207463A1, example A93).

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.

CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

CDK5-IN-1 is a highly potent inhibitor of CDK5, displaying an inhibitory activity of less than 10 nM. This potent compound is specifically employed in scientific investigations relating to kidney diseases.

CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer.

EGFR/CDK2-IN-2 (compound 6a) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 19.6 nM and 87.9 nM, respectively. It promotes apoptosis in MCF-7 cells and halts cell cycle progression during the S phase. Additionally, this compound demonstrates notable anticancer activity, inhibiting MCF-7 cells with an IC50 of 0.39 μM [1].

CDK7-IN-25 (CY-16-1) is a potent CDK7 inhibitor with an IC50 value of less than 1nM, utilized in cancer research [1].

PROTAC CDK9 degrader-4 is a potent and efficacious chemical compound designed specifically to degrade CDK9, a protein involved in transcription regulation. This compound effectively targets and reduces the levels of CDK9, thereby modulating transcriptional activity.

CDK1/2/4-IN-1 (compound 3a) is a potent inhibitor of CDK with IC 50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 can be used in cancer research. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates the level of Bax, caspase-3, and P53 and decreases the level of Bcl-2 [1].

CDK7/12-IN-1 is a selective inhibitor of CDK7/12, acting on CDK7 (IC50: 3 nM) and CDK 12 (IC50: 277 nM). Inhibition of CDK7 and CDK12 is an effective inhibitor of tumour growth.

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.

CDK-IN-2 (CDK inhibitor II) is a potent and specific CDK9 inhibitor (IC50: <8 nM).

CDK-IN-6, a pyrazolo[1,5-a]pyrimidine compound, exhibits potent anticancer activities as a CDK inhibitor[1].

CDK-IN-11, a heterocyclic compound, promotes cardiomyocyte maturation [1].

CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC 50 value of 5.41 nM.

CDK2/Bcl2-IN-1 (compound 1) is a saponin-based inhibitor of CDK-2 (IC50=117.6 nM) that exhibits potent cytotoxic effects on cancer cells. Additionally, it inhibits Bcl-2 and promotes apoptosis in A549 lung cancer cells [1].

CDK7-IN-7, a highly potent and selective inhibitor of CDK7 kinase, exhibits remarkable activity with an IC50 of less than 50 nM.

CDK9-IN-13 is a potent and selective CDK inhibitor (IC50<3 nM). CDK9-IN-13 has a very short half-life in rodents.

CDK-IN-9 (compound 24) is a potent inhibitor of CDK. CDK-IN-9 is also a molecular gel that induces interaction between CDK12 and DDB1 and is able to act on CDK2/E (IC50: 4 nM). CDK-IN-9 can be used to dephosphorylate retinoblastoma protein and RNA polymerase II, thereby inducing apoptosis.

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

CDK/HDAC-IN-2 is a potent dual HDAC/CDK inhibitor that acts on HDAC1 (IC50: 6.4 nM), HDAC2 (IC50: 0.25 nM), HDAC3 (IC50: 45 nM), HDAC6,8 (IC50>1000 nM), CDK1 (IC50: 8.63 nM), CDK4,6,7 (IC50>1000 nM), CDK2 (IC50: 0.30 nM), CDK4,6,7 (IC50>1000 nM). CDK2 (IC50: 0.30 nM), CDK4,6,7 (IC50>1000 nM). CDK/HDAC-IN-2 can arrest the cell cycle in G2/M phase and induce apoptosis. CDK/HDAC-IN-2 has excellent anti-proliferative effects and shows significant anti-tumor effects.

CDK2-IN-4 is a potent and selective inhibitor of CDK2 with an IC50 of 44 nM for CDK2/cyclin A. It shows 2,000-fold selectivity over CDK1/cyclin B with IC50 of 86 uM.

CDK4/6-IN-6 is a potent CDK4/CDK6 inhibitor with Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.