For research use only. Not for therapeutic Use.
BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay[1].
BRD0539 dose-dependently blocks the formation of the DNA-bound state in a dose-dependent fashion. BRD0539 impairs the perturbation induced by the 4PAM DNA[1].
BRD0539 does not interfere with the SpCas9:gRNA interaction[1].
BRD0539 is able to inhibit SpCas9 in the eGFP-disruption assay, BRD0539 is unable to inhibit FnCpf1, a structurally different CRISPR-associated nuclease, in the same assay, further highlighting the specificity of BRD0539[1].
| Catalog Number | I015231 |
| CAS Number | 1403838-79-8 |
| Synonyms | [(3aR,4R,9bR)-8-(2-fluorophenyl)-1-(4-methylphenyl)sulfonyl-2,3,3a,4,5,9b-hexahydropyrrolo[3,2-c]quinolin-4-yl]methanol |
| Molecular Formula | C25H25FN2O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C25H25FN2O3S/c1-16-6-9-18(10-7-16)32(30,31)28-13-12-20-24(15-29)27-23-11-8-17(14-21(23)25(20)28)19-4-2-3-5-22(19)26/h2-11,14,20,24-25,27,29H,12-13,15H2,1H3/t20-,24+,25-/m1/s1 |
| InChIKey | CZOIXFMISSBIJL-DCEDVJGZSA-N |
| SMILES | CC1=CC=C(C=C1)S(=O)(=O)N2CCC3C2C4=C(C=CC(=C4)C5=CC=CC=C5F)NC3CO |
| Reference | [1]. Basudeb Maji, et al. A High-Throughput Platform to Identify Small-Molecule Inhibitors of CRISPR-Cas9. Cell. 2019 May 2;177(4):1067-1079.e19. |
