2. Apoptosis
  3. Apoptosis
  4. MM927

MM927 是一种高效的 NVL 抑制剂，其 IC50 值为 0.053 μM。MM927 阻断核仁中 60S 核糖体亚基的生物合成。MM927 能诱导半核糖体多聚体的形成，使细胞在 G1/S 和 G2/M 期发生周期阻滞，并诱导细胞凋亡 (apoptosis)。MM927 在 MOLM-13 急性髓系白血病 (AML) 和 HCT116 结直肠癌 (CRC) 异种移植模型中展示了抗肿瘤活性。MM927 可用于研究急性髓系白血病 (AML) 和 HCT116 结直肠癌 (CRC)等癌症。

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MM927

MM927 Chemical Structure

CAS No. : 3065567-21-4

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MM927 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

MM927 is a potent NVL inhibitor, with an IC50 of 0.053 μM. MM927 blocks 60S ribosomal subunit biogenesis in the nucleolus. MM927 induces half-mer polysomes, cell cycle arrest at G1/S and G2/M and apoptosis in cells. MM927 demonstrates antitumor efficacy in MOLM-13 AML and HCT116 CRC xenograft models. MM927 can be used for the study of cancers such as acute myeloid leukemia (AML) and colorectal cancer (CRC)[1].

体外研究
(In Vitro)

MM927 (72 h) 抑制 HCT116 细胞 (IC50 = 53 nM) 和 MOLM-13 细胞 (IC50 = 92 nM) 的活性[1]。
MM927 (0.5 μM, 24 h) 在 HCT116 NVL WT 细胞的多核糖体图谱中诱导 half-mer 多核糖体，并减少游离的 60S/80S 峰[1]。
MM927 (3 μM, 6 h) 使新合成的 eL36-SNAP 转移至非核糖体组分，并在 HCT116 细胞中从 60S/80S/多核糖体组分中耗竭[1]。
MM927 (3 μM, 24 h) 导致新合成的 eL36-SNAP (60S) 在细胞质信号减少，并在 HCT116 NVL WT 细胞中滞留于核仁灶中[1]。
MM927 (0.5 μM, 24-48 h) 在 HCT116 mock 细胞中诱导 G1/S 和 G2/M 期的细胞周期阻滞[1]。
MM927 (3 μM, 2-3 days) 在 MOLM-13 细胞中诱导凋亡，表现为切割型 caspase-3 增加，以及 Annexin V 阳性细胞比例升高[1]。
MM927 (0.051 μM, 72 h) 抑制表达外源人源 NVL 的 HCT116 NVLAID/AID 细胞的活性，IC50 为 0.051 μM；并抑制表达外源小鼠 NVL 的 HCT116 NVLAID/AID 细胞，IC50 为 0.207 μM[1]。

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

MM927 相关抗体:

Apoptosis Analysis[1]

Cell Line: MOLM-13 cells
Concentration: 3 μM
Incubation Time: 2, 3 days
Result: Induced apoptosis in MOLM-13 cells.
Decreased procaspase-3.
Increased cleaved caspase-3 levels, and high Annexin V-positive cell rates.
体内研究
(In Vivo)

MM927 (35 mg/kg, 腹腔注射，每日两次，21 天) 可降低 HCT116 NVL WT 肿瘤异种移植瘤的生长，并减少 NSG 小鼠的肿瘤负荷，而对 HCT116 NVL R403WCRISPR 肿瘤异种移植瘤无影响[1]。
MM927 (35 mg/kg, 腹腔注射，每日两次，14 天) 可降低 NSG 小鼠的白血病疾病负荷[1]。
MM927 (35 mg/kg, 腹腔注射，每日两次，3 天) 可增加 HCT116 NVL WT 肿瘤异种移植瘤中细胞核 p53 染色，并减少 NSG 小鼠中 Ki-67 阳性细胞染色[1]。

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

Animal Model: HCT116 NVL WT cells or HCT116 NVL R403WCRISPR cells (5 × 106 in 100 µL) were subcutaneously implanted into the left and right flanks of 4-8-week-old NSG mice[1]
Dosage: 35 mg/kg
Administration: i.p., twice daily, 21 days
Result: Achieved tumor growth inhibition (TGI) in HCT116 NVL WT tumor xenografts of NSG mice.
Reduced tumor burden at the end of treatment.
Showed no effect on HCT116 NVL R403WCRISPR tumor xenografts.
Showed no significant changes in body weight, no significant alterations in hemoglobin, platelets, liver Enzymes (ALT, AST).
Animal Model: Luciferase-expressing MOLM-13 cells (1 × 106) were intravenously injected into the tail vein of 4-8-week-old NSG mice[1]
Dosage: 35 mg/kg
Administration: i.p., twice daily, 14 days
Result: Achieved a 7-fold reduction in leukemic disease burden.
Caused a 9-fold decrease in MOLM-13 cell percentage in bone marrow and a 15-fold decrease in peripheral blood.
Animal Model: HCT116 NVL WT cells or HCT116 NVL R403WCRISPR cells (5 × 106 in 100 µL) were subcutaneously implanted into the left and right flanks of 4-8-week-old NSG mice[1]
Dosage: 35 mg/kg
Administration: i.p., twice daily, 3 days
Result: Reduced Ki-67-positive (proliferating) cell staining in HCT116 NVL WT tumor xenografts of NSG mice, with few cells showing co-localization of p53 and Ki-67.
分子量

487.50

Formula

C26H18FN3O4S
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

MM927 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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:

MM9273065567-21-4MM 927MM-927Apoptosisacute myeloid leukemiacolorectal cancerNVLHCT116 cellsInhibitorinhibitorinhibit

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