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CCT251545 | CCT251545 ATP competitive inhibitor of CDK19, CDK8
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK19
  • IC 50:6 nM
  • IC 50:5 nM
CDK8
  • IC 50:5 nM
  • IC 50:23 nM
ATP competitive
35-350 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC 50 - GSK3alpha: 462 nM, GSK3beta: 690 nM, PRKCQ: 122 nM

Potency Assay Off-Target:
Millipore panel (activity assay), CEREP
Selectivity Assessment Description:
The probe was tested at 1 uM across 293 kinases; the probe inhibited 6 out of the 293 kinases tested ...

Potency
Cellular
In Vitro

CDK19

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.1952

CDK8

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.1952

In Vivo Validations

Mouse, Rat
Dose: 0.2 mg/kg (IV), 0.5 mg/kg (PO)
Route of delivery: Intravenous, Oral
Plasma half life: 0.55 h M, 0.97 h R
Systemic clearance: 31 (M), 26 (R) mL/min/kg
Organ of interest (O): SW620 human colon cancer xenograft
Target engagement assay: NCr athymic mice bearing established SW620 xenografts were treated with CCT251545 at 70 mg/kg bid for days 0-7 and 10-14. Target engagement was demonstrated by clear reduction of phospho-STAT1(SER727) level at 2 and 6 h after the last dose.

Reference: --

Negative Control Compounds

Compound 7 and 9 (Nat. Chem. Biol. 2015, 11, 973-980)

Orthogonal Probes def

MSC2530818
Cortistatin A

Chemical Information

Molecular Formula C23H24ClN5O
SMILEs Cn1cc(-c2ccc(-c3cncc(Cl)c3N3CCC4(CCNC4=O)CC3)cc2)cn1
InChI InChI=1S/C23H24ClN5O/c1-28-15-18(12-27-28)16-2-4-17(5-3-16)19-13-25-14-20(24)21(19)29-10-7-23(8-11-29)6-9-26-22(23)30/h2-5,12-15H,6-11H2,1H3,(H,26,30)
Molecular weight 421.17 Da
AlogP 0.0
HBond acceptors 6
HBond donors 1
Atoms 54

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

by SERP
(on 10 Mar 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 15 Mar 2017 )
Cellular Use Rating
In Model Organisms
CCT251545 was optimized from a phenotypic screening hit for inhibitors of WNT pathway activity. Impressively, this optimization was done without the benefit of structure-based design. CCT251545 has...
by SERP
(on 18 Mar 2017 )
Cellular Use Rating
In Model Organisms
CCT251545 is a high-affinity ligand of CDK8 and CDK19 with biochemical IC50s for these targets of 7 and 6 nM, respectively. The compound exhibits high selectivity compared with other targets, as demonstrated...

Portal Comments

Added: 03/05/2022CCT251545 and an analogue have been independently profiled using a panel of cell-permeable energy transfer probes to quantify target occupancy for all 21 human CDKs in live cells (Wells...

(last updated: 14 Aug 2025)

Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria