| Bioactivity | 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]. | |||||||||
| Target | IC50: 22 μM (SpCas9) | |||||||||
| Invitro | 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]. | |||||||||
| Name | BRD0539 | |||||||||
| CAS | 1403838-79-8 | |||||||||
| Formula | C25H25FN2O3S | |||||||||
| Molar Mass | 452.54 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| 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. |
BRD0539
CAS: 1403838-79-8 F: C25H25FN2O3S W: 452.54
BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9
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