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SJ46421

Chemical Structure : SJ46421

CAS No.: 3086104-53-9

SJ46421

Catalog No.: PC-24902Not For Human Use, Lab Use Only.

SJ46421 is a specific JQ1-based KLHDC2 PROTAC protein degrader of BRD3, induces selective BRD3 degradation in cells, promotes selective cooperative ternary complex formation with BRD3BD2 with IC50 of 7.8 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SJ46421 is a specific JQ1-based KLHDC2 PROTAC protein degrader of BRD3, induces selective BRD3 degradation in cells, promotes selective cooperative ternary complex formation with BRD3BD2 with IC50 of 7.8 nM.
SJ46421 selectively inhibits KLHDC2 substrate ubiquitylation.
SJ46421 promotes polyubiquitylation of the BD2 domain from BRD2, BRD3, or BRD4.
SJ46421 displays two orders-of-magnitude selectivity for KLHDC2 over other KLHDC-family CRLs.

Physicochemical Properties

M.Wt 837.41
Formula C42H41ClN8O5S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-(2-(2-(8-(2-(4-(2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetyl)piperazin-1-yl)ethoxy)naphthalen-2-yl)thiazol-4-yl)acetyl)glycine

References

1. Scott DC, et al. Nat Commun. 2024 Oct 12;15(1):8829.

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