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EBCL-0014

Cell Cycle Related Ligands

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.

Library of Cell Cycle Related Ligands contains 448 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

Library image

Cell cycle and related molecular targets (Created by BioRender.com)

Preplated options

Dry powder/solution (DMSO)Dry powder
Number of compounds448
Comment

Highlights

Molecule highlight
EBC-46039CAS: 1073485-20-7

LDC000067, Cdl9 inhibitor, EBC-46039

Molecule highlight
EBC-07439CAS: 518303-33-8

HLM-008182, Plk3 inhibitor, EBC-07439

Molecule highlight
EBC-13127CAS: 2244987-03-7

CDK12-In-2, Cdk12 and Cdk13 inhibitor, EBC-13127

Molecule highlight
EBC-17116CAS: 571190-30-2

Palbociclib, CDK2, CDK4, CDK6 and CDK7 inhibitor, EBC-17116

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Disclaimer

All our products are for research purpose only. Any personal or non-scientific use is strictly prohibited.

Note

All the compounds with solubility below 10 mM are shipped as 2 mM solutions.

Product Features

  • A set of 448 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.
  • Cell Cycle 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.

Library Composition

Name
Occurrence in the library, times

poly(ADP-ribose) polymerase 1

34

34

Number of compounds

34

aurora kinase A

12

12

Number of compounds

12

MDM2 proto-oncogene

12

12

Number of compounds

12

cyclin dependent kinase 2

11

11

Number of compounds

11

tankyrase 2

11

11

Number of compounds

11

cyclin dependent kinase 4

9

9

Number of compounds

9

tankyrase

9

9

Number of compounds

9

aurora kinase B

8

8

Number of compounds

8

cyclin dependent kinase 1

8

8

Number of compounds

8

cyclin dependent kinase 7

8

8

Number of compounds

8

checkpoint kinase 2

7

7

Number of compounds

7

polo like kinase 1

7

7

Number of compounds

7

cyclin dependent kinase 6

7

7

Number of compounds

7

cyclin dependent kinase 5

6

6

Number of compounds

6

NIMA related kinase 2

6

6

Number of compounds

6

polo like kinase 3

6

6

Number of compounds

6

CXCR4

6

6

Number of compounds

6

cyclin dependent kinase 8

5

5

Number of compounds

5

cyclin dependent kinase 9

5

5

Number of compounds

5

poly(ADP-ribose) polymerase 2

4

4

Number of compounds

4

aurora kinase C

3

3

Number of compounds

3

cyclin dependent kinase 3

3

3

Number of compounds

3

NIMA related kinase 1

3

3

Number of compounds

3

polo like kinase 2

3

3

Number of compounds

3

ATM serine/threonine kinase

2

2

Number of compounds

2

ATR serine/threonine kinase

2

2

Number of compounds

2

polo like kinase 4

2

2

Number of compounds

2

cyclin dependent kinase 16

2

2

Number of compounds

2

histone H3 associated protein kinase

2

2

Number of compounds

2

NIMA related kinase 3

2

2

Number of compounds

2

TTK protein kinase

2

2

Number of compounds

2

cyclin dependent kinase 12

2

2

Number of compounds

2

cyclin dependent kinase 17

2

2

Number of compounds

2

NIMA related kinase 4

1

1

Number of compounds

1

NIMA related kinase 6

1

1

Number of compounds

1

cell division cycle 7

1

1

Number of compounds

1

NIMA related kinase 11

1

1

Number of compounds

1

cyclin dependent kinase 13

1

1

Number of compounds

1

poly (ADP-ribose) polymerase 3

1

1

Number of compounds

1

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