cdc25a

Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.

Cdc25A (80-93) (human) is a polypeptide involved in regulating cell proliferation and tumorigenesis by modulating cyclin D1 expression and facilitating the G1 S phase transition, with applications in cancer research [1].

DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.

BN82002 (CDC25 Phosphatase Inhibitor I) is a synthetic inhibitor of CDC25 phophatases

NSC-672121 is an inhibitor of Cdc25A. It is also a Vitamine K3 analog.

Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.

PROTAC NSD3 degrader-1 (compound 56) is a targeted degradation agent for the Nuclear receptor binding SET domain protein NSD3. It effectively induces NSD3 degradation in NCI-H1703 and A549 lung cancer cell lines, with DC50 values of 1.43 and 0.94 μM, respectively. Additionally, it hinders H3K36 methylation, triggers apoptosis, arrests the cell cycle, and diminishes the expression of NSD3-related genes, including CDC25A, ALDH1A1, and IGFBP.

PD-321852 is a small-molecule Chk1 inhibitor, which potentiates gemcitabine-induced clonogenic death in a panel of pancreatic cancer cell lines and evaluated the relationship between endpoints associated with Chk1 inhibition and chemosensitization. Gemcitabine chemosensitization by minimally toxic concentrations of PD-321852 ranged from minimal (<3-fold change in survival) in Panc1 cells to >30-fold in MiaPaCa2 cells. PD-321852 inhibited Chk1 in all cell lines as evidenced by stabilization of Cdc25A; in combination with gemcitabine, a synergistic loss of Chk1 protein was observed in the more sensitized cell lines.

NSC305787 hydrochloride ((Rac)-NSC305787 hydrochloride is a cell membrane permeable and selective and potent small molecule dual inhibitor of Cdc25 dual specificity phosphatase and EZR that displays antitumor activity in pancreatic cancer cells and inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.NSC 663284 inhibits NSD2 (IC50 of 170 nM) enzyme activity.

M2N12 is a potent and highly selective inhibitor of cell division cycle 25C protein phosphatase (Cdc25C, IC50 = 0.09 μM) and also exhibits anti-tumor activity. Additionally, M2N12 shows promising activity against Cdc25A (IC50 = 0.53 μM) and Cdc25B (IC50 = 1.39 μM).

M5N36, a potent and selective inhibitor of Cdc25C, demonstrates IC50 values of 0.15 µM for Cdc25A, 0.19 µM for Cdc25B, and 0.06 µM for Cdc25C. It exhibits anti-proliferative activity and enhances the expression of p-CDK1 and p-CDK2.

BN82002 hydrochloride is a potent, selective, and irreversible inhibitor of the CDC25 phosphatase family, inhibiting CDC25A, CDC25B2, CDC25B3, CDC25C, and [25C-cat] with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 μM, respectively, and exhibits approximately 20-fold greater selectivity over [CD45 tyrosine phosphatase].

NSC 95397 is a potent inhibitor of Cdc25 dual specificity phosphatase(Ki of 32, 96, and 40 nM for Cdc25A, Cdc25B, and Cdc25C, respectively).