For research use only. Not for therapeutic Use.
DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively[1]. DB008 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
DB008 (0-1μM; 0-120 min; HEK 293T cells) covalently modifies Cys169 of PARP16 and exhibits excellent proteome-wide selectivity in the irreversible binding mode[1].
DB008 (100 nM; 16 h; HAP1 WT and HAP1 PARP16 KO cells) rescues nutrient starvation-induced loss of soluble PARP16[1].
| Catalog Number | I042059 |
| CAS Number | 2991637-98-8 |
| Synonyms | 6-ethynyl-4-[[4-fluoro-3-(4-prop-2-enoylpiperazine-1-carbonyl)phenyl]methyl]-2H-phthalazin-1-one |
| Molecular Formula | C25H21FN4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H21FN4O3/c1-3-16-5-7-18-19(13-16)22(27-28-24(18)32)15-17-6-8-21(26)20(14-17)25(33)30-11-9-29(10-12-30)23(31)4-2/h1,4-8,13-14H,2,9-12,15H2,(H,28,32) |
| InChIKey | FDHSVRMVJBTBMG-UHFFFAOYSA-N |
| SMILES | C=CC(=O)N1CCN(CC1)C(=O)C2=C(C=CC(=C2)CC3=NNC(=O)C4=C3C=C(C=C4)C#C)F |
| Reference | [1]. Bejan DS, et, al. Structure-guided design and characterization of a clickable, covalent PARP16 inhibitor. Chem Sci. 2022 Nov 16;13(46):13898-13906. |
