AGB1 chemical structure
Chemical structureResearch use only
CAT. NO. DC48369Featured

AGB1

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TotalUS$750
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Product overview

Description & Application

AGB1 is a fast, highly selective, and potent bump-and-hole (B&H)-PROTAC degrader for BromoTag. AGB1 exhibits degradation for Ab:Brd4BD2 L387A and Ab: BromoTag-Brd2 with pDC50s of 7.8 and 7.9. AGB1 exhibits binary affinity to VHL (Kd=125 nM). AGB1 exhibits favorable pharmacokinetic profile in mice with the DC50, 6 h of ∼13 nM.

ParameterValue
Chemical NameAGB1
CAS No.2776190-62-4
SynonymsAGB1,AGB-1,AGB 1
FormulaC51H63ClN8O9S2
M.Wt1031.68
SMILESClC1=CC=C(C=C1)C2=N[C@H](C3=NN=C(N3C4=C2C(C)=C(C)S4)C)[C@@H](CC)C(OCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(NCC6=CC=C(C=C6)C7=C(C)N=CS7)=O)=O)=O)=O
Purity>97%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

AGB1 is a fast, highly selective, and potent bump-and-hole (B&H)-PROTAC degrader for BromoTag. AGB1 exhibits degradation for Ab:Brd4BD2 L387A and Ab: BromoTag-Brd2 with pDC50s of 7.8 and 7.9. AGB1 exhibits binary affinity to VHL (Kd=125 nM). AGB1 exhibits favorable pharmacokinetic profile in mice with the DC50, 6 h of ∼13 nM.

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

Bond AG, Craigon C, Chan KH, Testa A, Karapetsas A, Fasimoye R, Macartney T, Blow JJ, Alessi DR, Ciulli A. Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins. J Med Chem. 2021 Oct 28;64(20):15477-15502. doi: 10.1021/acs.jmedchem.1c01532. Epub 2021 Oct 15. PMID: 34652918; PMCID: PMC8558867.

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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