2. Epigenetics
  3. Histone Methyltransferase
  4. NSD2-IN-6

NSD2-IN-6 是一种选择性 NSD2 抑制剂，对 NSD2 和 NSD1 的IC50 分别为3.8 nM和274 nM。NSD2-IN-6 可降低 H3K36me2 水平，并通过恢复雄激素受体 (AR) 信号通路来逆转细胞可塑性。NSD2-IN-6在类器官模型中能诱导细胞状态从簇 2 和簇 3 向簇 1 转变。NSD2-IN-6 在体内通过逆转肿瘤细胞可塑性、抑制生长并促进细胞凋亡 (apoptosis) 来发挥抗肿瘤活性。NSD2-IN-6 可用于前列腺癌的研究。

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NSD2-IN-6

NSD2-IN-6 Chemical Structure

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Other Forms of NSD2-IN-6:

NSD2-IN-6 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NSD2-IN-6 is a selective and orally active NSD2 inhibitor with IC50s of 3.8  and 274 nM for NSD2 and NSD1 respectively. NSD2-IN-6 reduces H3K36me2 levels, reverses cell plasticity by restoring the androgen receptor (AR) signaling pathway. NSD2-IN-6 reduces a shift from cluster 2 and 3 states towards the cluster 1 state in organoids. NSD2-IN-6 exerts antitumor activity by reversing tumor cell plasticity, suppressing growth, and promoting apoptosis in vivo. NSD2-IN-6 can be used for prostate cancer research[1].

IC50 & Target[1]

EZH1

3.8 nM (IC50)

EZH1

274 nM (IC50)

体外研究
(In Vitro)

NSD2-IN-6 (compound NSD2i) 能在 NPPO-1NE 类器官中显著降低 H3K36me2 结构域水平[1]。
NSD2-IN-6 处理 NPPO-1NE 类器官，可导致细胞状态从簇 2 和簇 3 显著向簇 1 转变，并富集经典雄激素受体靶基因的表达[1]。
NSD2-IN-6在联合 Enzalutamide (HY-70002) 的情况下对非神经内分泌类器官的 AR 表达影响甚微或没有影响[1]。
NSD2-IN-6 (1 µM, 17 天) 能增强 NPPO-1NE、NPPO-2、NPPO-4 和 NPPO-6 类器官对 Enzalutamide 的敏感性，其 EC50 分别为 0.34、2.7、1.6 和 20 µM[1]。
NSD2-IN-6 (0.3-10 µM, 26天) 对 NSD2 敲除的 NPPO-1 和 NPPO-2 类器官无效，对 NSD2 敲除的 MSKPCa10 类器官有轻微效果[1]。
NSD2-IN-6 (10 µM, 21 天) 可降低 MSKPCa10、MSKPCa14、WCM154、WCM1262 和 MSKPCa2 人源 CRPC 类器官细胞系中的 H3K36me2 表达并轻微上调 H3K27me3；在 WCM1262 细胞系中导致谱系标志物 CD56 丢失并上调 AR；在 MSKPCa2 类器官中则引起类器官尺寸减小及 cleaved caspase 3 免疫染色阳性[1]。
NSD2-IN-6 (0.3-10 µM, 21 天) 在 MSKPCa10、MSKPCa14、WCM154、WCM1262 和 MSKPCa2 人源 CRPC 类器官细胞系中，经 Enzalutamide 处理后能导致细胞活力下降，产生高的布利斯协同评分，并浓度依赖性地诱导细胞凋亡[1]。

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

NSD2-IN-6 相关抗体:

Cell Viability Assay[1]

Cell Line: H3K27me3 in MSKPCa10, MSKPCa14, WCM154, WCM1262 and MSKPCa2 human CRPC organoid lines
Concentration: 0.3, 1, 3 and 10 μM
Incubation Time: 21 days
Result: Progressively decreased cell viability after enzalutamide treatment.

Apoptosis Analysis[1]

Cell Line: H3K27me3 in MSKPCa10, MSKPCa14, WCM154, WCM1262 and MSKPCa2 human CRPC organoid lines
Concentration: 0.3, 1, 3 and 10 μM
Incubation Time: 21 days
Result: Significantly increased caspase 3 and caspase 7 activity in a concentration-dependent manner.
体内研究
(In Vivo)

NSD2-IN-6 (compound NSD2i) (75-300 mg/kg，口服，一日一次 5 天) 可降低人源性前列腺癌类器官小鼠移植瘤中的 H3K36me2 水平[1]。
NSD2-IN-6 (150 mg/kg，口服，每日一次，一日一次持续 42 天) 通过逆转肿瘤细胞可塑性、抑制生长并促进肿瘤细胞凋亡，在小鼠人源性前列腺癌类器官移植瘤模型中发挥抗肿瘤活性[1]。

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

Animal Model: Subcutaneous grafts of human CRPC organoids in NOD/SCID mice[1]
Dosage: 75, 150 and 300 mg/kg
Administration: p.o., daily for 5 days
Result: Reduced H3K36me2 levels at each con centration without any adverse effects on mouse body weights.
Animal Model: Subcutaneous grafts of human CRPC organoids in NOD/SCID mice[1]
Dosage: 150 mg/kg
Administration: p.o., daily for 42 days
Result: Had modest effects on tumour growth for MSKPCa10, MSKPCa14 and WCM1262 xenografts.
Resulted strong growth suppression when combined with Enzalutamide.
Displayed a strong responses when combined with or with not Enzalutamide.
Showed loss of neuroendocrine phenotypes accompanied by overt necrosis and fibrosis, and increased adenocarcinoma features in MSKPCa10, MSKPCa14 and WCM1262 xenografts when combine with Enzalutamide.
Showed Loss of H3K36me2 , neuroendocrine markers CHGA and SYP in MSKPCa10 and MSKPCa14, and loss of CD56 in WCM1262 when combined with Enzalutamide.
Displayed strong downregulation of Ki67 and upregulation of CC3 when combine with Enzalutamide.
分子量

546.52

Formula

C25H26F4N8O2
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

NSD2-IN-6 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

NSD2-IN-6Histone Methyltransferaseorganoidsprostate cancerNSD2NSD1H3K36me2ARInhibitorinhibitorinhibit

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