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NIBR-LTSi | NIBR-LTSi : Inhibitor of LATS1, LATS2
RATINGS:
Cellular Use: (1 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
LATS1
  • IC50:1.41 nM
  • IC50:2160 nM
LATS2
      Inhibitor
      up to 5 uM

      Selectivity

      In Vitro Selectivity Assessment
      Potency Assay Off-Target:
      NIBR-LTSi revealed partial activity in the competitive in vitro binding assay for only three other k ...

      Potency
      Cellular
      In Vitro

      LATS1

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1016/j.stem.2024.03.003

      LATS2

      Mode of Action: Inhibitor

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1016/j.stem.2024.03.003

      In Vivo Validations

      Mouse
      Dose: 1 mg/Kg IV, 10 mg/Kg PO
      Route of delivery: Intravenous, Oral
      Plasma half life: 9.4 ± 1.2 h
      Bioavailability: 61 ± 4.2 %

      DOI Reference: 10.1016/j.stem.2024.03.003

      Chemical Information

      Molecular Formula C18H20N4O
      SMILEs c1cc(Nc2ccc(O[C@@H]3CCCNC3)cc2)c2cc[nH]c2n1
      InChI InChI=1S/C18H20N4O/c1-2-15(12-19-9-1)23-14-5-3-13(4-6-14)22-17-8-11-21-18-16(17)7-10-20-18/h3-8,10-11,15,19H,1-2,9,12H2,(H2,20,21,22)/t15-/m1/s1
      Molecular weight 308.16 Da
      AlogP 3.4373000000000005
      HBond acceptors 5
      HBond donors 3
      Atoms 43

      References

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      Expert Reviews

      by SERP
      (on 10 Jun 2024 )
      Cellular Use Rating
      In Model Organisms
      Please note that the PK of this compound has been evaluated only in mice.
      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria