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VH298 | VH298 : Protein-protein inhibitor of VHL
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
VHL
  • Kd:90 nM
  • Kd:80 nM
Protein-protein interaction
10-100 μM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
In Dundee MRC-PPU Express Screen of 50 kinases, VH298 did not substantially inhibit any kinases a ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
In chemoproteomic MS assays using an immobilized, linkable analogue of VH298, RBX1, CUL2, VHL, an ...

Potency
Cellular
In Vitro

VHL

Mode of Action: Protein-protein interaction

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/ncomms13312

Negative Control Compounds

cisVH298

Orthogonal Probes def

CM11

Chemical Information

Molecular Formula C27H33N5O4S
SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(C#N)CC2)C(C)(C)C)cc1
InChI InChI=1S/C27H33N5O4S/c1-16-21(37-15-30-16)18-7-5-17(6-8-18)12-29-23(34)20-11-19(33)13-32(20)24(35)22(26(2,3)4)31-25(36)27(14-28)9-10-27/h5-8,15,19-20,22,33H,9-13H2,1-4H3,(H,29,34)(H,31,36)/t19-,20+,22-/m1/s1
Molecular weight 523.23 Da
AlogP 2.5312
HBond acceptors 9
HBond donors 3
Atoms 70

Vendors

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Expert Reviews

by SERP
(on 29 Dec 2016 )
Cellular Use Rating
Aqueous solubility data should be provided for this probe.
by SERP
(on 3 Jan 2017 )
Cellular Use Rating
A useful probe that blocks VHL:HIF-a interaction.
The probe is soluble in DMSO at concentrations >100 mM.
Author note: Regarding "Aqueous solubility data should be provided for this probe." We have now measured the solubility of this probe. VH298 was soluble at 250 uM in water (unbuffered solution)...
by SERP
(on 12 Jun 2017 )
Cellular Use Rating
A selective probe that inhibits the VHL-HIFa interaction. There is a large difference between FP, ITC, and SPR-determined affinity and cell-based activity (recommended for use at 10-100 uM). I recommend...
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