2. Autophagy
  3. p62
  4. XRK3F2 free base

XRK3F2 free base 是一种 p62(自噬衔接蛋白 1) ZZ 结构域抑制剂，相较于 p62 的其他信号结构域，它对 p62-ZZ 结构域具有特异性。XRK3F2 free base 可阻断 TNFα 在骨髓基质细胞中的作用与上调，并诱导多发性骨髓瘤细胞凋亡。XRK3F2 free base 可用于多发性骨髓瘤骨病、急性髓系白血病及多发性骨髓瘤的相关研究。

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XRK3F2 free base

XRK3F2 free base Chemical Structure

CAS No. : 2375193-42-1

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XRK3F2 free base 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

XRK3F2 free base (5 μM；共培养 48 h + 成骨培养 4 天) 可在共培养及后续成骨分化过程中，防止多发性骨髓瘤 (MM) 诱导的 MC4 前成骨细胞中Runx2表达受抑与Gfi1表达上调。XRK3F2 还可恢复 MC4 前成骨细胞中的碱性磷酸酶活性[1]。
XRK3F2 free base (5 μM；处理 48 小时) 可阻断经 MM1.S 条件培养基或 TNFα 联合 IL7 处理的原代小鼠骨髓间充质干细胞 (BMSC) 中Gfi1的上调、Runx2的抑制及IL6的诱导。XRK3F2 可阻止多发性骨髓瘤 (MM) 诱导的 GFI1 和 HDAC1 向 Runx2-P1 启动子的招募，并在 MC4 前成骨细胞中维持 H3K9ac 修饰[1]。
XRK3F2 free base (2.5-5 μM；处理 4 天) 可挽救经MM暴露的 MC4 前成骨细胞中Runx2的表达、成骨靶基因的表达及H3K9ac标记水平，并减少Runx2-P1 启动子上的 GFI1 结合[1]。
XRK3F2 free base (5 μM；5 天) 可挽救成骨分化过程中经 MM 处理的 HD-hBMSC 内Runx2的 mRNA 表达[1]。
XRK3F2 free base (0-20 μM；作用 72 小时) 可抑制 K562、HL-60、K562/A02 和 HL60/ADR 白血病细胞的活力，其 IC50 值范围为 6.41 至 8.76 μM[2]。
XRK3F2 free base (5 μM) 可在 5 μM 浓度下诱导原代人急性髓系白血病 CD34+CD38−细胞 (类白血病起始细胞群体) 发生凋亡[2]。
XRK3F2 free base (0.1-10 μM，作用 48 h) 可抑制 TNFα 诱导的人 CD116+破骨细胞 (OCL) 前体细胞分化[3]。
XRK3F2 free base (10 μM；作用 48 h、72 h) 可通过诱导细胞凋亡直接抑制人多发性骨髓瘤 (MM) 细胞系、原代 MM 细胞及小鼠 5TGM1-gfp 细胞的增殖，其对 5TGM1 细胞的 IC50为 4.35 μM[3]。

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

XRK3F2 free base 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

XRK3F2 free base (40 mg/kg；腹腔注射；每日一次；连续 10 天) 在 PDX 模型中具有体内白血病抑制活性，可降低白血病负荷[2]。
XRK3F2 free base (27、40 mg/kg/天；腹腔注射；每周连续给药 5 天；共 2 周) 在免疫健全的多发性骨髓瘤模型中可诱导显著的新皮质骨形成，且该形成仅局限于存在多发性骨髓瘤 (MM) 的骨骼中[3]。

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.
分子量

399.43

Formula

C23H23F2NO3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

XRK3F2 free base 相关分类

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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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