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OTUDin3

Chemical Structure : OTUDin3

CAS No.: 441290-65-9

OTUDin3 (OTUD3 inhibitor)

Catalog No.: PC-20938Not For Human Use, Lab Use Only.

OTUDin3 (OTUD3 inhibitor) is a specific, small molecule inhibitor of deubiquitylase OTUD3, binds to OTUD3 (KD=0.32 uM) and inhibits the deubiquitinating activity of OTUD3 by interfering with Ub binding to OTUD3.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

OTUDin3 (OTUD3 inhibitor) is a specific, small molecule inhibitor of deubiquitylase OTUD3, binds to OTUD3 (KD=0.32 uM) and inhibits the deubiquitinating activity of OTUD3 by interfering with Ub binding to OTUD3.
OTUDin3 does not bind to OTUD5 in SPR assays.
OTUDin3 inhibits NSCLC cell growth with 8.1, 14.8, 6.1, and 7.4  μM in H1299, A549, H460, and H1650 cells, respectively, with no effect on normal cells, human pulmonary alveolar epithelial cells (HPAEpiC).
OTUDin3 inhibits lung cancer cell migration and invasion, and induces apoptosis.
OTUDin3 enhances degradation of GRP78 by inhibiting the deubiquitinating activity of OTUD3 and increasing GRP78 ubiquitylation.
OTUDin3 (10 mg/kg and 20 mg/kg, i.p.) inhibits the NSCLC growth in H1299 xenograft mouse models, with no obvious health problems or weight loss of mice.

Physicochemical Properties

M.Wt 508.60
Formula C29H24N4O3S
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

O=C(NC1=CC=CC(C2=NC3=CC=CC=C3N2)=C1)C4=CC=C(S(=O)(N5CC6=C(C=CC=C6)CC5)=O)C=C4

References

1. Yonghui Zhang, et al. Cell Death Dis. 2023 Jun 27;14(6):378.

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