Chemical Probes logo
OICR11029 | OICR11029 : 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
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BCL6
  • Kd:10 nM
  • IC50:375 nM
  • IC50:215 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selective against other BTB domains: BAZF (BCL6B) 1.40 uM, FAZF, PLZF, Miz1, Kaiso, LRF > 10 uM. Ou ...

Potency
Cellular
In Vitro

BCL6

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.2c00502

In Vivo Validations

Mouse
Dose: 1 mg/Kg IV, 10 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 3 h
Systemic clearance: 12 mL/min/Kg
Cmax: 4 uM
Bioavailability: 30%
Volume of Distribution at Steady-State: 0.4 L/Kg

DOI Reference: 10.1021/acsmedchemlett.2c00502

Negative Control Compounds

CANSAR4120193
Notes: IC50 41.1 uM SPR, not active in cellular assays

Chemical Information

Molecular Formula C26H25Cl2N7O5
SMILEs C[C@H]1COCCN1c1cc(NC(=O)Cn2cc(-c3cc(Cl)c(O)c(C(N)=O)c3)c3c(=O)n(C)cnc32)c(Cl)cn1
InChI InChI=1S/C26H25Cl2N7O5/c1-13-11-40-4-3-35(13)20-7-19(18(28)8-30-20)32-21(36)10-34-9-16(22-25(34)31-12-33(2)26(22)39)14-5-15(24(29)38)23(37)17(27)6-14/h5-9,12-13,37H,3-4,10-11H2,1-2H3,(H2,29,38)(H,30,32,36)/t13-/m0/s1
Molecular weight 585.13 Da
AlogP 0.0
HBond acceptors 12
HBond donors 4
Atoms 65

Expert Reviews

No SERP comments found for OICR11029

Probe OICR11029 is in the process of SERP review.

Please continue to check back for new reviews and commentary.