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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

Publications

Cross 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 public comments)
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