DB008 | PARP16 inhibitor | Probechem Biochemicals

Chemical Structure : DB008

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DB008 (DB-008)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	444.47
分子式	C25H21FN4O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(3-(4-Acryloylpiperazine-1-carbonyl)-4-fluorobenzyl)-6-ethynylphthalazin-1(2H)-one

参考文献

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

DB008 (DB-008)

生物&药学活性

物理化学性质&存储条件

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DB008 (DB-008)

生物&药学活性

物理化学性质&存储条件

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