2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. SKLB06329

SKLB06329 是一种强效的选择性 I 型 PRMTs 抑制剂。SKLB06329 对 PRMT6 表现出良好的选择性 (IC50 = 3.86 nM)，且对 II/III 型 PRMTs (如 PRMT5/7) 以及多种赖氨酸甲基转移酶 (PKMTs) 均无显著抑制作用。SKLB06329 能显著抑制三阴性乳腺癌 (TNBC) 细胞的增殖，诱导细胞凋亡 (apoptosis)，并抑制细胞内不对称二甲基精氨酸 (ADMA) 的表达。SKLB06329 可用于三阴性乳腺癌的相关研究。

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SKLB06329

SKLB06329 Chemical Structure

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Customer Review

SKLB06329 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

SKLB06329 is a potent selective Type I PRMTs inhibitor. SKLB06329 shows good selectivity for PRMT6 (IC50 = 3.86 nM) over Type II/III PRMTs (PRMT5/7) and shows no significant inhibition against various lysine methyltransferases (PKMTs). SKLB06329 significantly inhibits the proliferation of triple-negative breast cancer (TNBC) cells, induces apoptosis, and suppresses the expression of asymmetric dimethylarginine (ADMA) within cells. SKLB06329 can be used for triple-negative breast cancer research[1].

IC50 & Target[1]

PRMT6

3.86 nM (IC50)

体外研究
(In Vitro)

SKLB06329 (compound B9) (6 天) 能抑制 TNBC 细胞的增殖，其对 MDA-MB-231 和 Hs578T 细胞的 IC50 值分别为 29.94 μM 和 3.93 μM，其效力与阳性对照 MS023 (HY-19615) 相当[1]。
SKLB06329 与PRMT1中的多个氨基酸 (包括Glu65、Met164 和 Tyr170) 形成氢键，因此能强效抑制 I 型PRMTs 的活性[1]。
SKLB06329 (5-40 μM) 能显著抑制 MDA-MB-231 和 Hs578T 细胞的集落形成，即使在最低测试浓度 5 μM 下也能减少集落数量并降低每个集落的细胞密度[1]。
SKLB06329 (10-80 μM，6 天) 能有效诱导细胞凋亡，并在 TNBC 细胞 (MDA-MB-231 和 Hs578T) 中以浓度依赖的方式抑制不对称二甲基精氨酸 (ADMA) 的表达，这表明它在细胞内抑制了 I 型 PRMTs 的甲基化功能[1]。
SKLB06329 (0-80 μM，6 天) 在 MDA-MB-231 细胞中展现出一种依赖于 PRMT1 的抗增殖效应[1]。

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

SKLB06329 相关抗体:

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 and Hs578T cells
Concentration: 10, 20, 40 and 80 μM
Incubation Time: 6 days
Result: Induced apoptosis of MDA-MB-231 and Hs578T cells.
The apoptosis inducing effect was more pronounced in Hs578T cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 and Hs578T cells
Concentration: 10, 20, 40 and 80 μM
Incubation Time: 6 days
Result: Significantly reduced ADMA expression compared with that in the control group.
Reduced ADMA expression in a concentration-dependent manner.
Significantly reduced levels of H4R3me2a and H3R2me2a in MDA-MB-231 and Hs578T cells.

Cell Viability Assay[1]

Cell Line: PRMT1-knockdown (shPRMT1) MDA-MB-231 cells
Concentration: 0, 20, 40 and 80 μM
Incubation Time: 6 days
Result: Showed a significant sensitivity decrease in PRMT1-knockdown (shPRMT1) MDA-MB-231 cells compared to the control group.
分子量

399.51

Formula

C20H25N5O2S
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

SKLB06329 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:

SKLB06329SKLB 06329SKLB-06329Histone MethyltransferaseApoptosisPRMTlysine methyltransferasesPRMT6TNBCADMAMDA-MB-231Hs578TInhibitorinhibitorinhibit

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目录号：
HY-178274
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