2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. SKLB-0124

SKLB-0124 是一种有效的 PRMT6 降解剂，在 HCC827 和 MDA-MB-435 细胞中的 DC50 分别为 15.4 μM 和 16.4 μM。SKLB-0124 不降解 PRMT1 或 PRMT8。SKLB-0124 对 PRMT6 的 IC50 值为 1.6 μM。SKLB-0124 可诱导蛋白酶体依赖性的 PRMT6 降解，并显著抑制细胞增殖。SKLB-0124 可有效诱导细胞凋亡 (apoptosis) 和细胞周期停滞。SKLB-0124 可用于肺癌和乳腺癌的研究。

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SKLB-0124

SKLB-0124 Chemical Structure

CAS No. : 3065966-31-3

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SKLB-0124 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

SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer[1].

IC50 & Target[1]

PRMT6

15.4 nM (DC50)

体外研究
(In Vitro)

SKLB-0124 (1.25-20 μM, 0.5-7 d) 表现出非急性降解动力学，通过泛素蛋白酶体系统 (UPS) 通路在 MDA-MB-435 细胞和 HCC827 细胞中以适当的速率降解 PRMT6，且不产生钩状效应[1]。
SKLB-0124 (0-10 μM, 6 d) 抑制细胞增殖，对 HCC827 和 MDA-MB-435 细胞的 IC50 分别为 6.66 和 5.68 μM[1]。
SKLB-0124 (10-20 μM, 3 d) 以浓度依赖性方式导致 MDA-MB-435 细胞和 HCC827 细胞的 G0/G1 期阻滞[1]。
SKLB-0124 (15-90 μM, 9 d) 对正常 HEK293 和 HEK293T 细胞的毒性较低[1]。

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

SKLB-0124 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MDA-MB-435 cells and HCC827 cells
Concentration: 10 and 20 μM
Incubation Time: 3 d
Result: Caused the G0/G1 arrest pattern in a concentration dependent manner, with a concomitant decrease of cells in other phases of the cell cycle.

Apoptosis Analysis[1]

Cell Line: MDA-MB-435 cells and HCC827 cells
Concentration: 10 and 20 μM
Incubation Time: 6 d
Result: Induced apoptosis in 78.41% of the HCC827 cells and 90.1% of the MDA-MB-435 cells at 20 μM.

Western Blot Analysis[1]

Cell Line: MDA-MB-435 cells and HCC827 cells
Concentration: 1.25, 2.5, 5, 10 and 20 μM
Incubation Time: 0.5, 1, 3, 5 and 7 d
Result: Significantly and dose-dependently reduced the expression of PRMT6 protein.
Observed that after 5 days of PRMT6 degradation, there was a significant degradation after 7 days.
Significantly degraded PRMT6 but did not degrade PRMT1 or PRMT8.
分子量

531.73

Formula

C32H45N5O2
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

SKLB-0124 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:

SKLB-01243065966-31-3SKLB0124SKLB 0124Histone MethyltransferaseApoptosisAnticancer agentsHistone methylationHydrophobic tagging methodPRMT6Protein degraderInhibitorinhibitorinhibit

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目录号：
HY-178114
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