cdk1-in-1

CDK1-IN-7 is a potent inhibitor of CDK1 with an IC50 value of 161.2 nM for CDK1 CycB. CDK1-IN-7 induces apoptosis in a p53-dependent manner via the apoptosis-intrinsic pathway. CDK1-IN-7 selectively acts on tumour tissue and has potential anti-proliferative effects. CDK1-IN-7 is a potential CDK1-IN-7 is a potential targeted anti-tumour agent.

KDM1 CDK1-IN-1 (compound 4) is a potent inhibitor of KDM1 (IC50: 0.096 μM) and CDK1 (IC50: 0.078 μM), blocking the cell cycle of HOP-92 cells in the G2 M phase and inducing apoptosis. It is highly cytotoxic to CCRF-CEM cells (IC50: 16.34 μM), HOP-92 cells (IC50: 3.45 μM), and Hep-G2 cells (IC50: 7.79 μM).

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].

CDK1 Cyc B-IN-1 (Compound 5) is a potent inhibitor of the CDK1 Cyc B complex with an IC50 value of 97 nM. This compound induces apoptosis and G2 M cell cycle arrest, halting cancer cell proliferation, and exhibits a wide-ranging cytotoxic effect on various cancer cell lines [1].

Avotaciclib (BEY1107) is a potent, orally active cyclin-dependent kinase 1 (CDK1) inhibitor, suitable for research in locally advanced or metastatic pancreatic cancer.

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.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK p38 MAPK signaling pathways in the murine macrophages.

AG-024322 is a potent ATP-competitive inhibitor targeting pan-CDK, effectively inhibiting cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range (1-3 nM).

CDKI-83 is a potent CDK9 inhibitor. The compound shows effective anti-proliferative activity in human tumour cell lines with GI50 <1 μM, and is capable of inducing apoptosis in A2780 human ovarian cancer cells as determined by the activated caspase-3, Annexin V PI double staining and accumulated cells at the sub-G1 phase of cellcycle. The research results suggest that combined inhibition of CDK9 and CDK1 may result in the effective induction of apoptosis and CDKI-83 has the potential to be developed as an anti-cancer agent.

CDK4 6-IN-14 is a potent, highly selective inhibitor of Cyclin-Dependent Kinases 4 and 6 (CDK4 6), with inhibition concentrations (IC50s) of 10 nM and 16 nM, respectively. It shows over 60-fold selectivity for CDK4 6 compared to CDKs 1, 2, 7, and 9, and exhibits significant selectivity against 205 other kinases.

Avotaciclib hydrochloride, a CDK1 inhibitor, is the hydrochloride salt of Avotaciclib and exhibits potential therapeutic use in specific malignancies, including pancreatic cancer, characterized by abnormal and pronounced CDK1 expression [1].

QR-6401, a selective macrocyclic CDK2 inhibitor, is orally active with IC50 values of 0.37 nM for CDK2 E1, 10 nM for CDK9 T1, 22 nM for CDK1 A2, 34 nM for CDK6 D3, and 45 nM for CDK4 D1. It exhibits potent antitumor activity in the OVCAR3 ovarian cancer xenograft model, indicating its potential for use in cancer research [1].

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.

PLK1-IN-10 (Compound 4Bb), an orally active inhibitor of the PLK1 PBD (polo-box domain), inhibits the interaction between PLK1 and the cell division regulator protein 1 (PRC1) and reduces the protein expression of the CDK1-Cyclin B1 complex. Additionally, PLK1-IN-10 interacts with glutathione (GSH), enhancing cellular oxidative stress and promoting cell death [1].

Desmethylglycitein (6,7,4'-Trihydroxyisoflavone) , is a novel inhibitor of PKCα in suppressing solar UV-induced matrix metalloproteinase 1, which has antioxidant, and anti-cancer activities.