XRK3F2
CAS No. : 2375193-43-2
| Size | Price | Stock |
|---|---|---|
| 5mg | $100 | In-stock |
| 10mg | $150 | In-stock |
| 50mg | $520 | In-stock |
| 100mg | $800 | In-stock |
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| Cat. No. : | HY-112904 |
| M.Wt: | 435.89 |
| Formula: | C23H24ClF2NO3 |
| Purity: | >98 % |
| Solubility: | DMSO : 150 mg/mL (ultrasonic);H2O : 0.91 mg/mL (ultrasonic) |
XRK3F2 is a p62 (sequestosome-1) ZZ domain inhibitor that has specificity for the p62-ZZ domain over other p62 signaling domains. XRK3F2 blocks TNFα effects and upregulation in bone marrow stromal cells, and induces multiple myeloma cell apoptosis. XRK3F2 can be used for the research of multiple myeloma bone disease, acute myeloid leukemia, and multiple myeloma[1][2][3].
IC50 & Target:P62-ZZ domain[1].
In Vitro:XRK3F2 (5 μM; 48 h co-culture + 4 days osteogenic culture) prevents MM-induced Runx2 suppression and Gfi1 upregulation in MC4 pre-osteoblasts during co-culture and subsequent osteogenic differentiation. XRK3F2 also rescues alkaline phosphatase activity in MC4 pre-osteoblasts[1].
XRK3F2 (5 μM; 48 h) blocks Gfi1 upregulation, Runx2 repression, and IL6 induction in primary murine BMSC treated with MM1.S conditioned media or TNFα plus IL7. XRK3F2 prevents MM-induced GFI1 and HDAC1 recruitment to the Runx2-P1 promoter and preserves H3K9ac marks in MC4 pre-osteoblasts[1].
XRK3F2 (2.5-5 μM; 4 days) rescues Runx2 expression, osteogenic target gene expression, and H3K9ac marks, and reduces GFI1 binding at the Runx2-P1 promoter in MM-exposed MC4 pre-osteoblasts[1].
XRK3F2 (5 μM; 5 days) rescues Runx2 mRNA expression in MM-exposed HD-hBMSC during osteogenic differentiation[1].
XRK3F2 (0-20 μM; 72 h) inhibits the viability of K562, HL-60, K562/A02, and HL60/ADR leukemia cells with IC50 values ranging from 6.41 to 8.76 μM[2].
XRK3F2 (5 μM) induces apoptosis of primary human AML CD34+CD38− cells (LIC-like population) at 5 μM[2].
XRK3F2 (0.1-10 μM, 48 h ) inhibits TNFα-induced differentiation of human CD116+ OCL precursors[3].
XRK3F2 (10 μM; 48 h, 72 h) directly inhibits growth of human MM cell lines, primary MM cells, and murine 5TGM1-gfp cells by inducing apoptosis, with an IC50 of 4.35 μM for 5TGM1 cells[3].
In Vivo:XRK3F2 (40 mg/kg; i.p.; daily; 10 consecutive days) has leukemia inhibitory potential in vivo in a PDX model, reducing leukemic burden[2].
XRK3F2 (27, 40 mg/kg/day; i.p.; 5 consecutive days/week; 2 weeks) induces significant new cortical bone formation restricted to MM-containing bones in an immunocompetent multiple myeloma model[3].
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