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BIX-02565 | Inhibitor of RPS6KA3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (1 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
RPS6KA3
  • IC50:1 nM
  • IC50:20 nM
20 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - LRRK2 16 nM, PRKD1 35 nM

Potency Assay Off-Target:
In a panel of 20 kinases, BIX-02565 inhibited six of them with IC50 < 1 uM. In an expanded panel of ...
Selectivity Assessment Description:
Outside target family: Tested in a panel of 68 receptors, ion channels, and protein targets for o ...

Potency
Cellular
In Vitro

RPS6KA3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2011.10.029

In Vivo Validations

Rat
Dose: 1,3, 10 (IV) mg/Kg; , 30, 100, 300 (PO) mg/Kg
Route of delivery: Intravenous, Oral

Reference: --

Orthogonal Probes def

BI-D1870

Chemical Information

Molecular Formula C26H30N6O2
SMILEs C[C@@H]1CCNC(=O)c2cc3ccc(C(=O)Nc4nc5ccccc5n4CCCN(C)C)cc3n21
InChI InChI=1S/C26H30N6O2/c1-17-11-12-27-25(34)23-15-18-9-10-19(16-22(18)32(17)23)24(33)29-26-28-20-7-4-5-8-21(20)31(26)14-6-13-30(2)3/h4-5,7-10,15-17H,6,11-14H2,1-3H3,(H,27,34)(H,28,29,33)/t17-/m1/s1
Molecular weight 458.24 Da
AlogP 3.8895000000000026
HBond acceptors 8
HBond donors 2
Atoms 64

Vendors

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Expert Reviews

by SERP
(on 17 Mar 2021)
Cellular Use Rating
In Model Organisms
This compound is not recommended for use in vivo due to cardiotoxicity relating to its off-target effects on adrenergic receptors. Compounds with no off-target cardiotoxicity were later derived from...
by SERP
(on 30 Jul 2021)
Cellular Use Rating
The compound has potential off-target activity on LRRK2 and PRKD1. The patent review (PMID: 27410995) describes how binding to the adrenergic receptors may result in a lethal decrease of heart rate...
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