cdk in 2

CDK-IN-2 (CDK inhibitor II) is a potent and specific CDK9 inhibitor (IC50: <8 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 and 8 (IC50 > 1000 nM), CDK1 (IC50: 8.63 nM), CDK2 (IC50: 0.30 nM), and CDK4, 6, and 7 (IC50 > 1000 nM). CDK HDAC-IN-2 can arrest the cell cycle in the G2 M phase and induce apoptosis, demonstrating excellent anti-proliferative and significant anti-tumor effects.

Cdk1 2 Inhibitor III is a selective inhibitor of Cdk1 2 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.

CDK9-IN-2 is a specific CDK9 inhibitor with an IC50 of 5 nM in the A2058 skin cell line (72 hours) and 7 nM in the H929 multiple myeloma cell line (72 hours).

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

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.

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.

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

CDK2-IN-18 (compound 8q) serves as a powerful inhibitor of CDK 2 E and CDK 4 D1, showing IC50 values of 8 nM and 46 nM, respectively. It effectively inhibits tumor cell proliferation [1].

EGFR CDK2-IN-2 (compound 6a) is a dual inhibitor targeting EGFR and CDK-2, with IC50 values of 19.6 nM and 87.9 nM, respectively. It induces apoptosis in MCF-7 cells and arrests cell cycle progression in the S phase, demonstrating notable anticancer activity with an IC50 of 0.39 μM [1].

CDK1 2 4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78, and 0.87 μM for CDK1, CDK2, and CDK4, respectively. It can be used in cancer research to arrest the cell cycle at the G2 M phase and induce apoptosis, elevating Bax, caspase-3, and P53 levels while decreasing Bcl-2 levels [1].

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.

CDK2 Bcl2-IN-1 (compound 1) is a saponin-based inhibitor of CDK-2 (IC50=117.6 nM) with potent cytotoxic effects on cancer cells, also inhibiting Bcl-2 and promoting apoptosis in A549 lung cancer cells [1].

CDK2-IN-7 is a CDK2 inhibitor for treating cancer (IC50 < 50 nM).

EGFR CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC50 values of 71.7 nM and 113.7 nM, respectively. It induces apoptosis in MCF-7 cells, arrests the cell cycle in the S phase, and exhibits significant anti-cancer cell toxicity, inhibiting MCF-7 cells with an IC50 of 3.16 μM [1].

CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and specific inhibitor of the CDK7 enzyme, exhibiting significant anti-cancer properties.

CDK2-IN-26, also known as compound 9, effectively inhibits CDK 2 [1].

CDK4 6-IN-2 is a potent inhibitor of CDK4 and CDK6 [IC50s: 2.7 and 16 nM].

CDK2-IN-8 is a potent CDK2 inhibitor (IC50 = 1.74 μM) that exhibits antiproliferative activity and can be used for melanoma research.

CDK2-IN-9 is a potent CDK2 inhibitor (IC50: 0.63 μM) with anti-proliferative effects, capable of blocking the cell cycle in S and G2 M phases and inducing apoptosis, showing potential for melanoma research.

CDK2 4-IN-1 (compound B-4a) serves as both a CDK2 4 inhibitor and a microtubule polymerization inhibitor, making it useful in cancer research.

CDK4-IN-2 (A17) is a potent CDK4 inhibitor with K i and IC 50 values below 10 nM, used in cancer research [1].

CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor targeting CDK5 p25 (IC50: 0.2 nM) and CDK2 CycA (IC50: 23 nM).

CDK2-IN-12 (compound 10b) is a potent inhibitor of CDK2 (IC50: 11.6 μM) and exhibits inhibition of hCA subtypes I, II, IX, and XII with KI values of 3534, 638.4, 44.3, and 48.8 nM, respectively. Additionally, CDK2-IN-12 shows anti-cancer effects.

SHP2 CDK4-IN-1 (compound 10) is a dual inhibitor targeting SHP2 and CDK4, with oral activity and high potency, showing IC50 values of 4.3 nM for SHP2 and 18.2 nM for CDK4. It induces G0 G1 arrest, inhibits proliferation of TNBC cell lines, and demonstrates significant antitumor efficacy in the EMT6 syngeneic mouse model. This compound is valuable for research into triple-negative breast cancer (TNBC) [1].

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].

CDK2-IN-23 (Compound 17), a selective and highly potent inhibitor of CDK2 (IC 50 = 0.29 nM), demonstrates pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. This compound is utilized in cancer research [1].

CDK2 degrader1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. It binds to cerebellum, inducing ubiquitination of CDK2 followed by proteasomal degradation pathway. CDK2 degrader1 is utilized in the research of multiple cancers.

CDK2-IN-19 (Compound 32) is a selective, orally active CDK2 inhibitor (K i: 0.18 nM) that demonstrates anticancer activity in mice with OVCAR3 tumors [1].

GSK-3 CDK5 CDK2-IN-1 is an imidazole derivative compound that inhibits cdk5, cdk2, and GSK-3.it has demonstrated applications in cancer research and the study of neurodegenerative diseases [1].

PROTAC CDK2/9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

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

CDK1-IN-2 (cdk1 inhibitor 2) is a CDK1 inhibitor with IC50 of 5.8 μM. A broad-spectrum kinase profiling of CDK1-IN-2 revealed nonselective inhibition of several kinases.

CDK2, a eukaryotic S/T protein kinase family member, catalyzes the phosphoryl transfer from ATP γ-phosphate to the hydroxyl of serine or threonine (denoted as S0/T0) in a protein substrate.

CDK7-IN-2 is a potent inhibitor of CDK7, which plays a role in transcription initiation via phosphorylation of the Rbpl subunit of RNA polymerase II (RNAPII). CDK7 is linked to the temporal control of the cell cycle and transcriptional activity, and has research potential for aggressive and difficult-to-treat cancers.

EGFR HER2 CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR (IC50:191.08 nM), HER2 (IC50:132.65 nM), and CDK9 (IC50:113.98 nM), demonstrating significant anti-tumor effects.

EGFR/CDK2-IN-1, an inhibitor of both EGFR and CDK2, demonstrates effective cytotoxicity towards MCF7 and HepG2 cells, suggesting its potential application in cancer research.

CDK2 degrader2 is a PROTAC class CDK2 degrader that targets the CDK2 protein for ubiquitination, facilitating its degradation via the ubiquitin-proteasome pathway (UPP). It effectively degrades CDK2 in MKN1 cells, with a DC50 value of less than 100 nM and an average Dmax greater than 75% (Red: CBM; Blue: DIM; Black: linker).

CDK7 ligand 2 (Compound A6) is a CDK7 ligand utilized in the synthesis of PROTACs.

Cdk2 Cyclin Inhibitory Peptide II (Tat-LDL), a CDK2 inhibitor, exhibits dose-dependent cytotoxic effects on U2OS osteosarcoma cells [1].

PROTAC CDK9/CycT1 Degrader-2 inhibits CDK9 with an IC50 of 45 nM [1].

CDK2-IN-11 (compound 9d) is a potent inhibitor of CDK2 (IC50: 6.4 μM) and acts on hCA II (Ki: 23.4 nM), hCA IX (Ki: 56.3 nM), and hCA XII (Ki: 44.3 nM). CDK2-IN-11 can be used in anticancer studies.

EGFR HER2 CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR, HER2, and CDK9, with IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively, and exhibits significant anti-tumor effects.

EGFR/HER2/CDK9-IN-2 are potent inhibitors of EGFR/HER2/CDK9, and they exhibited significant antitumor effects with IC50s of 145.35, 129.07 and 117.13 nM, respectively.

PROTAC CDK9 degrader-2 (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].

HDAC1 2 and CDK2-IN-1 (compound 14d) are potent inhibitors of HDAC1, HDAC2, and CDK2 with IC50 values of 70.7, 23.1, and 0.80 μM, respectively. HDAC1 2 and CDK2-IN-1 can block the cell cycle and induce apoptosis, demonstrating good anti-tumor effects in vivo.