细胞周期相关配体
The cell cycle is a sequence of events that occur in a cell in the preparation for cell division. It is a two-step process: interphase and mitotic (M) phase. The interphase step is divided into three different phases: G1 phase, S phase, and G2 phase. Cell cycle checkpoints are integral components of DNA repair that coordinate the restoration of DNA structure. When some genes (such as the cell cycle inhibitors, RB, p53, etc) mutate, they may cause the cell uncontrollable proliferation, which leads to tumor formation. At the same time, the cells which are actively undergoing the cell cycle can be efficiently targeted by cancer therapy. Their DNA is exposed during the division and hence susceptible to damage by drugs. It makes molecular targets related to the cell cycle attractive for cancer medicinal chemistry research.
Cell Cycle Related Ligands Library contains 469 small ligands, some representative molecules are given below: LDC000067, Cdl9 inhibitor; HLM-008182, Plk3 inhibitor; CDK12-In-2, Cdk12 and Cdk13 inhibitor; Palbociclib, CDK2, CDK4, CDK6 and CDK7 inhibitor.
Related terms: poly(ADP-ribose) polymerase, aurora kinase, MDM2 proto-oncogene, cyclin dependent kinase, tankyrase, checkpoint kinase, polo like kinase, CXCR4
Cell cycle and related molecular targets (Created by BioRender.com)
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Highlights
LDC000067, Cdl9 inhibitor,
HLM-008182, Plk3 inhibitor,
CDK12-In-2, Cdk12 and Cdk13 inhibitor,
Palbociclib, CDK2, CDK4, CDK6 and CDK7 inhibitor,
Product Features
A set of 469 cell cycle relevant molecules with sub-10 micromolar activity coefficients values for HTS/HCS programs.
The library is composed of ligands that target all major pharmaceutically relevant cell cycle related targets.
Cancer Immunology Related Ligands Library covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
Calculated structural diversity of the collection: 0.85.
Comprehensive documentation with structures, trivial names, synonyms, activity coefficients values, types of action on target and references to original literature.
NMR and LCMS validated purity.
All the compounds are available in stock for hit follow-up.
The library is continuously updated.
Product Details
Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
Container: 384-well microplates;
Storage: - 18 °C;
Shipping: Dry ice.
Utility
High throughput screening (HTS);
High content screening (HCS);
Cherry picking.
