Chemical Structure : Y043-4427
CAS No.:
1574337-35-1
Y043-4427
(mDTX2i C22H24N4O2)
Catalog No.: PC-23661Not For Human Use, Lab Use Only.
Y043-4427 (mDTX2i, C22H24N4O2) is a potent small molecule inhibitor of Deltex E3 ubiquitin ligase 2 (DTX2) with IC50 of 30.83 uM in Hepa1-6 cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Y043-4427 (mDTX2i, C22H24N4O2) is a potent small molecule inhibitor of Deltex E3 ubiquitin ligase 2 (DTX2) with IC50 of 30.83 uM in Hepa1-6 cells.
Y043-4427 (mDTX2i) binds to the mouse DTX2 protein (SPK KD=5-10 uM) and form hydrogen bonds at asparagine 459, lysine 460, aspartate 461, lysine 476, and asparagine 576.
Y043-4427 (mDTX2i) inhibits the binding of DTX2 to histone H2B, and decreases H2BK120ub1, H3K4me3, and H3K79me3.
mDTX2i treatment inhibited the transcription and secretion of mouse CXCL2 and mouse CXCL6, inhibited neutrophil chemotaxis and ARG1 expression of neutrophils.
mDTX2i increased the infiltration of CD8+ T cells, decreased the infiltration of TANs, and decreased the expression of CXCL2 and CXCL6 in subcutaneous tumors.
mDTX2i treatment sensitizes HCC cells to PD1 antibody treatment in spontaneous HCC model.
Physicochemical Properties
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M.Wt
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376.46
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Formula
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C22H24N4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-[5-(1H-benzimidazol-2-YL) pentyl]-2-(3-oxo-2,3-dihydro-1H-isoindol-1-yl) acetamide
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References
1. Wu X, et al. Adv Sci (Weinh). 2024 Dec 29:e2408233.
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