Chemical Structure : DB008
CAS No.: 2991637-98-8
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.
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5 mg | ¥2580 | In stock | |
| 10 mg | ¥3980 | In stock | |
| 25 mg | ¥5980 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| 分子量 | 444.47 | |
| 分子式 | C25H21FN4O3 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
4-(3-(4-Acryloylpiperazine-1-carbonyl)-4-fluorobenzyl)-6-ethynylphthalazin-1(2H)-one |
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1. Bejan DS, et al. Chem Sci. 2022 Nov 16;13(46):13898-13906.
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