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DB008

Chemical Structure : DB008

CAS No.: 2991637-98-8

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DB008 (DB-008)

Catalog No.: PC-26517Not For Human Use, Lab Use Only.

DB008 is a selective, covalent PARP16 inhibitor with IC50 of 0.275 uM, covalently reacts with a non-conserved cysteine (Cys169, human numbering) in the NAD+ binding pocket of PARP16.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DB008 is a selective, covalent PARP16 inhibitor with IC50 of 0.275 uM, covalently reacts with a non-conserved cysteine (Cys169, human numbering) in the NAD+ binding pocket of PARP16.
DB008 shows excellent selectivity profile among the MARylating PARPs, with one of the prominent off-targets as PARP2 (IC50=139 nM).
DB008 does not inhibit PARP1/2 in a covalent manner.
DB008 covalently modifies Cys169 of PARP16 and exhibits excellent proteome-wide selectivity in the irreversible binding mode.
DB008 stabilizes PARP16 levels during nutrient starvation.

Physicochemical Properties

M.Wt 444.47
Formula C25H21FN4O3
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

4-(3-(4-Acryloylpiperazine-1-carbonyl)-4-fluorobenzyl)-6-ethynylphthalazin-1(2H)-one

References

1. Bejan DS, et al. Chem Sci. 2022 Nov 16;13(46):13898-13906.

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