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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

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 public 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)

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