Chemical Probes logo
d9A-2 | d9A-2 : Degrader (PROTAC) of SLC9A1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SLC9A1
  • EC50:< 1uM
Degrader (PROTAC)
250-500 nM
250-750 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity for the degradation of SLC9A1 over other SLC9 family members. HAP1 cells, overexpressin ...
Selectivity Assessment Description:
SLC9A1 demonstrated the most efficient degradation. d9A-2 prompted degradation of the closely relate ...

Potency
Cellular
In Vitro

SLC9A1

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2020.04.003

Chemical Information

Molecular Formula C46H54FN7O9
SMILEs Cc1cc(-c2ccc(C(=O)NCCOCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)cc2N2CCC(c3[nH]cnc3C)CC2)ccc1F
InChI InChI=1S/C46H54FN7O9/c1-29-26-32(7-9-36(29)47)34-8-6-33(27-39(34)53-16-12-31(13-17-53)42-30(2)50-28-51-42)43(56)49-15-19-61-21-23-63-25-24-62-22-20-60-18-14-48-37-5-3-4-35-41(37)46(59)54(45(35)58)38-10-11-40(55)52-44(38)57/h3-9,26-28,31,38,48H,10-25H2,1-2H3,(H,49,56)(H,50,51)(H,52,55,57)
Molecular weight 867.40 Da
AlogP 0.0
HBond acceptors 16
HBond donors 4
Atoms 117

References

Publications

Cross References

canSAR

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 28 Dec 2023 )
Cellular Use Rating
CRBN recruiting PROTAC d9A-2 is currently (December 2023) the best available degrader of for studying the biology of SLC9 transporters, although it has certain drawbacks. Based on the data in the original...
by SERP+
(on 31 Oct 2024 )
Cellular Use Rating
There seems to be a variability of the optimal dosing depending on pH and cell line used.
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