| Bioactivity | XRK3F2 is an inhibitor of p62 (Sequestosome-1)-ZZ/ domain. |
| Target | P62-ZZ domain. |
| Invitro | The presence of XRK3F2 during MM-preOB co-cultures prevents Runx2 suppression at both d0 and d4. Furthermore, XRK3F2 blocks MM-induced upregulation of Gfi1. XRK3F2 blocks the induction of Gfi1 mRNA in BMSC in both treatment conditions. In contrast, XRK3F2 prevents both MM1.S CM and TNFα plus IL7-mediated Runx2 suppression. Further, the pro-inflammatory and myeloma pro-survival factor IL6 mRNA is also reduced by XRK3F2 treatment. In addition, XRK3F2 also prevents TNFα-mediated upregulation of Gfi1 and rescues inhibition of Runx2 in MC4 preOB. XRK3F2 prevents MM-induced GFI1 occupancy at the Runx2-P1 promoter. XRK3F2 treatment significantly rescues the H3K9ac levels at Runx2 in MM patient hBMSC and XRK3F2 can rescue early steps in osteogenesis[1]. |
| Name | XRK3F2 |
| CAS | 2375193-43-2 |
| Formula | C23H24ClF2NO3 |
| Molar Mass | 435.89 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Adamik J, et al. XRK3F2 Inhibition of p62-ZZ Domain Signaling Rescues Myeloma-Induced GFI1-Driven Epigenetic Repression of the Runx2 Gene in Pre-osteoblasts to Overcome Differentiation Suppression. Front Endocrinol (Lausanne). 2018 Jun 29;9:344. |