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TAK-243 | Inhibitor of UBA1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
UBA1
  • Kd:>0.75 nM
  • IC50:1 ± 0.2 nM
  • EC50:12-20 nM (48-72h)
Inhibitor
0.01, 0.10 or 1.00 μM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
TAK-243 has significant biochemical inhibitory activity against closely related E1 ubiquitin-like ...

Potency
Cellular
In Vitro

UBA1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/nm.4474

In Vivo Validations

Mouse
Dose: 12.5, 18.8, 25 mg/Kg
Route of delivery: Intravenous
Plasma half life: 17.4-20.6 h
Systemic clearance: 4.99-3.89 L/h/Kg

DOI Reference: 10.1038/nm.4474

Orthogonal Probes def

ABPA3

Chemical Information

Molecular Formula C19H20F3N5O5S2
SMILEs NS(=O)(=O)OC[C@H]1C[C@@H](Nc2ccnc3cc(-c4cccc(SC(F)(F)F)c4)nn23)[C@H](O)[C@@H]1O
InChI InChI=1S/C19H20F3N5O5S2/c20-19(21,22)33-12-3-1-2-10(6-12)13-8-16-24-5-4-15(27(16)26-13)25-14-7-11(17(28)18(14)29)9-32-34(23,30)31/h1-6,8,11,14,17-18,25,28-29H,7,9H2,(H2,23,30,31)/t11-,14-,17-,18+/m1/s1
Molecular weight 519.09 Da
AlogP 0.0
HBond acceptors 10
HBond donors 5
Atoms 54

Vendors

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Expert Reviews

by SERP
(on 20 May 2021)
Cellular Use Rating
In Model Organisms
TAK-243 is a potent inhibitor of UAE which demonstrates complete inhibition of cellular ubiquitylation and sub-micromolar anti-proliferative activity against multiple cancer cell lines. Robust antitumor...
by SERP
(on 11 Jun 2021)
Cellular Use Rating
In Model Organisms
TAK-243 is a potent inhibitor of UBA1 with cellular activities consistent with the proposed mechanism of action. TAK-243 shows anti-tumor activity in mouse xenograft studies at doses at or below the...
by SERP
(on 31 May 2023)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
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