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  4. XRK3F2 free base

XRK3F2 free base is a p62 (sequestosome-1) ZZ domain inhibitor that has specificity for the p62-ZZ domain over other p62 signaling domains. XRK3F2 free base blocks TNFα effects and upregulation in bone marrow stromal cells, and induces multiple myeloma cell apoptosis. XRK3F2 free base can be used for the research of multiple myeloma bone disease, acute myeloid leukemia, and multiple myeloma.

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CAS No. : 2375193-42-1

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XRK3F2 free base Related Antibodies

Top Publications Citing Use of Products

    XRK3F2 free base purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 May 27;31(1):209.  [Abstract]

    Cell viability (live cells counted using hemocytometer after trypan blue exclusion) and intracellular Caspase3 activity (Caspase 3/7 Activity Apoptosis Assay) were assessed after treating cabozantinib-resistant HCC cells with XRK3F2.

    XRK3F2 free base purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2020 Dec 17:8:593890.  [Abstract]

    The infarct volume was significantly decreased compared with that of the ND13 group.after treatment with XRK3F2 (2.5 μg/μL).

    XRK3F2 free base purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2020 Dec 17:8:593890.  [Abstract]

    HE staining showed that after treatment with XRK3F2 (2.5 μg/μL), the injuries condition improved.

    XRK3F2 free base purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2020 Dec 17:8:593890.  [Abstract]

    After combined treatment with XRK3F2 (2.5 μg/μL) and ND13, the expression levels of IL-10 and IL-4 were higher and the expression levels of TNF-α and IL-1β were lower than those of the ND13 group.

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    Description

    XRK3F2 free base is a p62 (sequestosome-1) ZZ domain inhibitor that has specificity for the p62-ZZ domain over other p62 signaling domains. XRK3F2 free base blocks TNFα effects and upregulation in bone marrow stromal cells, and induces multiple myeloma cell apoptosis. XRK3F2 free base can be used for the research of multiple myeloma bone disease, acute myeloid leukemia, and multiple myeloma[1][2][3].

    In Vitro

    XRK3F2 free base (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 free base (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 free base (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 free base (5 μM; 5 days) rescues Runx2 mRNA expression in MM-exposed HD-hBMSC during osteogenic differentiation[1].
    XRK3F2 free base (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 free base (5 μM) induces apoptosis of primary human AML CD34+CD38− cells (LIC-like population) at 5 μM[2].
    XRK3F2 free base (0.1-10 μM, 48 h ) inhibits TNFα-induced differentiation of human CD116+ OCL precursors[3].
    XRK3F2 free base (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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    XRK3F2 free base Related Antibodies

    Cell Differentiation Assay[1]

    Cell Line: murine pre-osteoblast MC4 cells
    Concentration: 3 μM
    Incubation Time: 48 h (mRNA analysis); 7 days (alkaline phosphatase staining)
    Result: Prevented TNFα-induced Gfi1 mRNA upregulation and Runx2 mRNA repression; rescued alkaline phosphatase staining (a marker of osteogenic differentiation) in TNFα-treated MC4 cells

    Cell Differentiation Assay[1]

    Cell Line: murine pre-osteoblast MC4 cells, 5TGM1 multiple myeloma (MM) cells
    Concentration: 2.5-5 μM
    Incubation Time: 4 days (osteogenic media culture)
    Result: Significantly elevated Runx2 mRNA and downstream osteogenic target genes (Ocn, Bsp, Osx); reduced GFI1 binding at the Runx2-P1 promoter; increased H3K9ac levels at the Runx2-P1 promoter; rescued alkaline phosphatase staining

    Cell Differentiation Assay[1]

    Cell Line: healthy donor human BMSC (HD-hBMSC), MM1.S cells
    Concentration: 5 μM
    Incubation Time: 5 days (osteogenic media culture after MM removal)
    Result: Rescued Runx2 mRNA levels in MM-exposed HD-hBMSC; decreased Gfi1 mRNA (difference not significant)

    Cell Cytotoxicity Assay[2]

    Cell Line: K562, HL-60, K562/A02, HL60/ADR
    Concentration: 0-20 μM
    Incubation Time: 72 h
    Result: Exhibited cytotoxicity toward K562 (IC50 = 6.41 μM), HL-60 (IC50 = 8.23 μM), K562/A02 (IC50 = 6.42 μM), and HL60/ADR (IC50 = 8.76 μM) cells, with comparable sensitivity between parental and drug-resistant lines.

    Cell Proliferation Assay[3]

    Cell Line: human MM cell lines, primary MM cells, murine 5TGM1-gfp cells
    Concentration: 10 μM
    Incubation Time: 48 h (human MM cell lines, primary MM cells); 72 h (murine 5TGM1-gfp cells)
    Result: Significantly inhibited growth of all 6 human MM cell lines and primary human MM cells; achieved an IC50 of 4.35 μM for 5TGM1 cells and 4.6 μM for MM1.S cells; induced cleavage of caspases 9, 7, and 3 in MM1.S cells after 16 hours.
    Parmacokinetics
    Species Dose Route T1/2
    Mice[3] 27 mg/kg i.p. 10.3
    Mice[3] 40 mg/kg i.p. 10.3 h
    In Vivo

    XRK3F2 free base (40 mg/kg; i.p.; daily; 10 consecutive days) has leukemia inhibitory potential in vivo in a PDX model, reducing leukemic burden[2].
    XRK3F2 free base (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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: NOG (sublethally irradiated 120 cGy; AML PDX model)[2]
    Dosage: 40 mg/kg
    Administration: i.p.; daily; 10 consecutive days
    Result: Markedly reduced leukemic burden of hCD45+ cells in the bone marrow compared to the vehicle group.
    Animal Model: C57BL/KaLwRij (male, 6-12 weeks of age, multiple myeloma model via tibial inoculation of 1×10⁵ 5TGM1-gfp cells)[3]
    Dosage: 27 mg/kg/day; 40 mg/kg/day
    Administration: i.p.; 5 consecutive days/week; 2 weeks
    Result: Increased cortical bone volume (measured by new bone volume to total bone volume ratio) in all treated mice; Observed greater cortical bone formation in treated mice with high tumor burden (high IgG₂b levels); Detected no new bone formation in non-MM-bearing legs; Confirmed new woven bone formation localized to MM-containing bones via histology, with active osteoblasts and osteoclasts present on new bone surfaces.
    Molecular Weight

    399.43

    Formula

    C23H23F2NO3
    CAS No.
    SMILES

    FC1=CC=C(COC2=CC=C(CNCCO)C=C2OCC3=CC=C(C=C3)F)C=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    XRK3F2 free base Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    XRK3F22375193-42-1p62Sequestosome-1SQSTM1HDAC1acute myeloid leukemiamultiple myeloma cellsMC4 pre-osteoblastsosteoclastsRunx2-P1 promoterp62 (sequestosome-1) ZZ domainbone marrow stromal cellsnormal hematopoietic stem cellsleukemia initiating cellsInhibitorinhibitorinhibit

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