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TP-021 | TP-021 : Inhibitor of BCL6
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 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
BCL6
  • IC50:100 nM
  • IC50:720 nM
Inhibitor
1-10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
TP-021 and TP-021n show no significant inhibition at 1 μM in Takeda in house kinase panel (344 targe ...

Potency
Cellular
In Vitro

BCL6

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmc.2017.07.037

In Vivo Validations

Mouse
Dose: 0.1 mg/kg IV, 1 mg/kg PO
Route of delivery: Oral, Intravenous
Systemic clearance: 630 mL/h*Kg
Cmax: 233 ng/mL
Tmax: 2.0 h
Area Under the Curve:: 1.27 ug*h/mL
Bioavailability: 79.9%
Volume of Distribution at Steady-State: 1505 mL/Kg

DOI Reference: 10.1016/j.bmc.2017.07.037

Negative Control Compounds

TP-021n

Orthogonal Probes def

BI-3802
BI-3812

Chemical Information

Molecular Formula C20H20ClN3O5
SMILEs O=C1CCc2cc(Nc3cc(OC4CCOCC4)c([N+](=O)[O-])cc3Cl)ccc2N1
InChI InChI=1S/C20H20ClN3O5/c21-15-10-18(24(26)27)19(29-14-5-7-28-8-6-14)11-17(15)22-13-2-3-16-12(9-13)1-4-20(25)23-16/h2-3,9-11,14,22H,1,4-8H2,(H,23,25)
Molecular weight 417.11 Da
AlogP 4.434300000000003
HBond acceptors 8
HBond donors 2
Atoms 49

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Expert Reviews

No SERP comments found for TP-021

Probe TP-021 is in the process of SERP review.

Please continue to check back for new reviews and commentary.