YKL-05-099 |
YKL-05-099 : Inhibitor of SIK1, SIK3, SIK2
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| SIK1 |
|
|
| SIK3 |
|
|
| SIK2 |
|
|
Inhibitor
up to 1 µM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
YKL-05-099 (1 μM) was tested for its ability to inhibit
the activity of 144 kinases at the MRC PPU I ...
Potency Cellular
In Vitro
SIK1
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acschembio.6b00217
SIK3
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acschembio.6b00217
SIK2
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acschembio.6b00217
In Vivo Validations
Mouse
Dose: 20 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
> 7 h
DOI Reference: 10.1021/acschembio.6b00217
Chemical Information
| Molecular Formula | C32H34ClN7O3 |
| SMILEs | COc1ccc(N2C(=O)N(c3c(C)cccc3Cl)Cc3cnc(Nc4ccc(C5CCN(C)CC5)cc4OC)nc32)nc1 |
| InChI | InChI=1S/C32H34ClN7O3/c1-20-6-5-7-25(33)29(20)39-19-23-17-35-31(37-30(23)40(32(39)41)28-11-9-24(42-3)18-34-28)36-26-10-8-22(16-27(26)43-4)21-12-14-38(2)15-13-21/h5-11,16-18,21H,12-15,19H2,1-4H3,(H,35,36,37) |
| Molecular weight | 599.24 Da |
| AlogP | 6.681720000000007 |
| HBond acceptors | 10 |
| HBond donors | 1 |
| Atoms | 77 |