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BI-D1870 | BI-D1870 : ATP competitive inhibitor of RPS6KA1, RPS6KA2, RPS6KA3, RPS6KA6
RATINGS:
Cellular Use: (3 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
RPS6KA1
  • IC50:31 nM RPS6KA1
  • IC50:1 uM
RPS6KA2
  • IC50:18 nM
  • IC50:1 uM
RPS6KA3
  • IC50:24 nM
  • IC50:1 uM
RPS6KA6
  • IC50:15 nM
  • IC50:1 uM
ATP competitive
10-1,000 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - MST2 0.86 uM, GSK3 beta 1.59 uM, MARK3 2.20 uM, CSNK2A1 0.45 uM, AURKB 0.34 uM, PLK1 0.10 uM

Potency Assay Off-Target:
BI-D1870 showed little activity against 50 off-target kinases in vitro

Potency
Cellular
In Vitro

RPS6KA1

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1042/BJ20061088

RPS6KA2

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1042/BJ20061088

RPS6KA3

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1042/BJ20061088

RPS6KA6

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1042/BJ20061088

Orthogonal Probes def

A1LU8
BIX-02565

Chemical Information

Molecular Formula C19H23F2N5O2
SMILEs CC(C)CCN1c2nc(Nc3cc(F)c(O)c(F)c3)ncc2N(C)C(=O)C1C
InChI InChI=1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)
Molecular weight 391.18 Da
AlogP 3.421400000000001
HBond acceptors 7
HBond donors 2
Atoms 51

References

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Expert Reviews

by SERP
(on 18 May 2016 )
Cellular Use Rating
Although the initial paper was excellent, and many studies have used this compound to uncover interesting biology, more data has come to light recently. A recent paper discloses a new RSK inhibitor,...
by SERP
(on 19 May 2017 )
Cellular Use Rating
In Model Organisms
I agree with the previously posted comments. In addition to LJI308, analog LJH685 has been co-crystallized with RPS6KA3 N-terminal domain (pdb 4nus). However, commercial availability is unknown as of...
by SERP
(on 18 Jun 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
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